上海卢湘仪毛细管血液离心机RG-120TX 24 根毛细管

上海卢湘仪毛细管血液离心机RG-120TX 24 根毛细管

  • 品牌 卢湘仪|BIORIDGE
  • 型号 RG-120TX
  • 商品详情

    技术性能 

    微机控制,直流无刷电机驱动,运行稳定、噪声低转速精度高, 触控面板,可编程操作,主机运行参数可根据需求设置自动存储, 数字屏显示,人性化界面操作简单便捷,实时RPM/RCF之读数换算和设定,方便快捷,配备电子门锁,设有门盖保护,超速等多种保护功能、确保仪器安全运行。采用食用级硅橡胶整体式密封圈,符合GMP认证。离心机获得美国FDA认证。

    技术参数 

    型号

    RG-120TX-12(含12根毛细管转子)

    RG-120TX-24(含24根毛细管转子)

    最高转速

    12000r/min

    最大相对离心力

    13500×g

    最大容量

    24根毛细血管

    转速精度

    ±30r/min

    整机噪音

    <65dB(A)

    定时范围

    1min~99min

    电源

    AC220V 50Hz 5A

    外形尺寸

    230×310×240mm(L×W×H)

     外包装尺寸

    290×400×330mm(L×W×H)

    重量

    9kg

  • 上海卢湘仪毛细管血液离心机RG-120TX 12 根毛细管

    上海卢湘仪毛细管血液离心机RG-120TX 12 根毛细管

  • 品牌 卢湘仪|BIORIDGE
  • 型号 RG-120TX
  • 商品详情

    技术性能 

    微机控制,直流无刷电机驱动,运行稳定、噪声低转速精度高, 触控面板,可编程操作,主机运行参数可根据需求设置自动存储, 数字屏显示,人性化界面操作简单便捷,实时RPM/RCF之读数换算和设定,方便快捷,配备电子门锁,设有门盖保护,超速等多种保护功能、确保仪器安全运行。采用食用级硅橡胶整体式密封圈,符合GMP认证。离心机获得美国FDA认证。

    技术参数

    型号

    RG-120TX-12(含12根毛细管转子)

    RG-120TX-24(含24根毛细管转子)

    最高转速

    12000r/min

    最大相对离心力

    13500×g

    最大容量

    24根毛细血管

    转速精度

    ±30r/min

    整机噪音

    <65dB(A)

    定时范围

    1min~99min

    电源

    AC220V 50Hz 5A

    外形尺寸

    230×310×240mm(L×W×H)

     外包装尺寸

    290×400×330mm(L×W×H)

    重量

    9kg

  • Vemurafenib(Synonyms: 维罗非尼; PLX4032; RG7204; RO5185426)

    上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

    Vemurafenib (Synonyms: 维罗非尼; PLX4032; RG7204; RO5185426) 纯度: 99.83%

    Vemurafenib (PLX4032; RG7204; RO5185426) 是首创的,有效的 B-RAF 选择性抑制剂,能够抑制 RAFV600E 和 c-RAF-1 的活性,IC50 分别为 31 nM 和 48 nM。Vemurafenib 可以诱导细胞自噬 (autophagy)。

    Vemurafenib(Synonyms: 维罗非尼; PLX4032;  RG7204;  RO5185426)

    Vemurafenib Chemical Structure

    CAS No. : 918504-65-1

    规格 价格 是否有货 数量
    Free Sample (0.1-0.5 mg)   Apply now  
    10 mM * 1 mL in DMSO ¥567 In-stock
    10 mg ¥515 In-stock
    50 mg ¥1300 In-stock
    100 mg ¥2300 In-stock
    200 mg ¥4100 In-stock
    500 mg ¥6890 In-stock
    1 g ¥11500 In-stock
    5 g   询价  
    10 g   询价  

    * Please select Quantity before adding items.

    Vemurafenib 相关产品

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    • MAPK Compound Library
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    • Autophagy Compound Library
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    • FDA Approved & Pharmacopeial Drug Library
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    • Anti-Pancreatic Cancer Compound Library
    • Targeted Therapy Drug Library
    • Anti-Liver Cancer Compound Library
    • Rare Diseases Drug Library
    • Anti-Colorectal Cancer Compound Library

    生物活性

    Vemurafenib (PLX4032) is a first-in-class, selective, potent inhibitor of B-RAF kinase, with IC50s of 31 and 48 nM for RAFV600E and c-RAF-1, respectively[1][4]. Vemurafenib induces cell autophagy[5].

    IC50 & Target[1]

    B-RafV600E

    31 nM (IC50)

    c-Raf-1

    48 nM (IC50)

    体外研究
    (In Vitro)

    Vemurafenib (PLX4032) selectively blocks the RAF/MEK/ERK pathway in BRAF mutant cells[1]. RG7204 is a potent inhibitor of proliferation in those expressing RAFV600E but not BRAFWT in 17 melanoma cell lines. Vemurafenib (RG7204) induces MEK and ERK phosphorylation at high concentrations in CHL-1 cells[2]. Ectopic expression of EGFR in melanoma cells is sufficient to cause resistance to PLX4032[3].

    上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

    体内研究
    (In Vivo)

    Vemurafenib (PLX4032, 20, 25, 75 mg/kg, p.o.) causes dose-dependent inhibition of tumor growth, with higher exposures resulting in tumor regression of BRAF mutant xenografts[1]. RG7204 (12.5, 25, and 75 mg/kg, p.o.) significantly inhibits tumor growth and induced tumor regression in mice bearing LOX tumor xenografts[2].

    上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

    Clinical Trial

    分子量

    489.92

    Formula

    C23H18ClF2N3O3S

    CAS 号

    918504-65-1

    中文名称

    维罗非尼;维罗菲尼;威罗菲尼;唯罗非尼

    运输条件

    Room temperature in continental US; may vary elsewhere.

    储存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    溶解性数据
    In Vitro: 

    DMSO : 50 mg/mL (102.06 mM; Need ultrasonic)

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 2.0411 mL 10.2057 mL 20.4115 mL
    5 mM 0.4082 mL 2.0411 mL 4.0823 mL
    10 mM 0.2041 mL 1.0206 mL 2.0411 mL

    *

    请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
    储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

    In Vivo:

    请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

    ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
    分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

    • 1.

      请依序添加每种溶剂: 1.5% CMC-Na/saline water

      Solubility: 3.33 mg/mL (6.80 mM); Suspended solution; Need ultrasonic

    • 2.

      请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.08 mg/mL (4.25 mM); Clear solution

      此方案可获得 ≥ 2.08 mg/mL (4.25 mM,饱和度未知) 的澄清溶液。

      以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

      将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

    • 3.

      请依序添加每种溶剂: 10% DMSO    90% corn oil

      Solubility: ≥ 2.08 mg/mL (4.25 mM); Clear solution

      此方案可获得 ≥ 2.08 mg/mL (4.25 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

      以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

    *以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
    参考文献
    • [1]. Bollag G, et al. Clinical efficacy of a RAF inhibitor needs broad target blockade in BRAF-mutant melanoma. Nature, 2010, 467(7315), 596-599.

      [2]. Yang H, et al. RG7204 (PLX4032), a selective BRAFV600E inhibitor, displays potent antitumor activity in preclinical melanoma models. Cancer Res, 2010, 70(13), 5518-5527.

      [3]. Prahallad A, et al. Unresponsiveness of colon cancer to BRAF(V600E) inhibition through feedback activation of EGFR. Nature, 2012, 483(7387), 100-103.

      [4]. Shelledy L, et al. Vemurafenib: First-in-Class BRAF-Mutated Inhibitor for the Treatment of Unresectable or MetastaticMelanoma. J Adv Pract Oncol. 2015 Jul-Aug;6(4):361-5.

      [5]. Wang W, et al. Targeting Autophagy Sensitizes BRAF-Mutant Thyroid Cancer to Vemurafenib.J Clin Endocrinol Metab. 2017 Feb 1;102(2):634-643.

    Cell Assay
    [2]

    Briefly, cells are plated in 96-well microtiter plates at a density of 1,000 to 5,000 cells per well in a volume of 180 μL. For the assay, Vemurafenib (RG7204) is prepared at 10 times the final assay concentration in media containing 1% DMSO. Twenty-four hours after cell plating, 20 μL of the appropriate dilution are added to plates in duplicate. The plates are assayed for proliferation 6 days after the cells are plated according to the procedure.

    上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [2]

    Athymic nude mice, are with ages 13 to 14 weeks, and weighing approximately 23 to 25 g. For the LOX xenografts, 2×106 cells in 0.2 mL of PBS are injected s.c. into the right lateral flank. Vemurafenib (RG7204), formulated as MBP, is suspended at the desired concentration as needed for each dose group in an aqueous vehicle containing 2% Klucel LF and adjusted to pH 4 with dilute HCl. NSC 362856 is of 250-mg capsules. Capsules are opened and combined into one bulk supply. To prepare the stock dosing material, NSC 362856 is first dissolved in 100% DMSO followed by dilution with saline to form a final milky white suspension in 10% DMSO/90% saline (pH 3.4).

    上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

    参考文献
    • [1]. Bollag G, et al. Clinical efficacy of a RAF inhibitor needs broad target blockade in BRAF-mutant melanoma. Nature, 2010, 467(7315), 596-599.

      [2]. Yang H, et al. RG7204 (PLX4032), a selective BRAFV600E inhibitor, displays potent antitumor activity in preclinical melanoma models. Cancer Res, 2010, 70(13), 5518-5527.

      [3]. Prahallad A, et al. Unresponsiveness of colon cancer to BRAF(V600E) inhibition through feedback activation of EGFR. Nature, 2012, 483(7387), 100-103.

      [4]. Shelledy L, et al. Vemurafenib: First-in-Class BRAF-Mutated Inhibitor for the Treatment of Unresectable or MetastaticMelanoma. J Adv Pract Oncol. 2015 Jul-Aug;6(4):361-5.

      [5]. Wang W, et al. Targeting Autophagy Sensitizes BRAF-Mutant Thyroid Cancer to Vemurafenib.J Clin Endocrinol Metab. 2017 Feb 1;102(2):634-643.

    所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

    Idasanutlin(Synonyms: RG7388)

    上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

    Idasanutlin (Synonyms: RG7388) 纯度: 99.90%

    Idasanutlin (RG7388) 是一种有效,选择性的 MDM2 拮抗剂,能够抑制 p53-MDM2 的结合,IC50 值为 6 nM。

    Idasanutlin(Synonyms: RG7388)

    Idasanutlin Chemical Structure

    CAS No. : 1229705-06-9

    规格 价格 是否有货 数量
    Free Sample (0.1-0.5 mg)   Apply now  
    10 mM * 1 mL in DMSO ¥1492 In-stock
    2 mg ¥750 In-stock
    5 mg ¥1100 In-stock
    10 mg ¥1500 In-stock
    50 mg ¥4500 In-stock
    100 mg ¥7200 In-stock
    200 mg   询价  
    500 mg   询价  

    * Please select Quantity before adding items.

    Idasanutlin 相关产品

    相关化合物库:

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    • Clinical Compound Library
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    • Anti-Aging Compound Library
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    • Oxygen Sensing Compound Library
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    • Anti-COVID-19 Compound Library
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    • Anti-Blood Cancer Compound Library
    • Transcription Factor Targeted Library
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    • Rare Diseases Drug Library
    • Anti-Colorectal Cancer Compound Library

    生物活性

    Idasanutlin (RG7388) is a potent and selective MDM2 antagonist, inhibiting p53-MDM2 binding, with an IC50 of 6 nM.

    IC50 & Target

    IC50: 6 nM (p53-MDM2)[1]

    体外研究
    (In Vitro)

    Idasanutlin (RG7388) inhibits cell proliferation with IC50 of 30 nM, and induces dose-dependent p53 stabilization, cell cycle arrest, as well as cell apoptosis in cancer cells expressing wild-type p53[1]. Idasanutlin (RG7388) (300 nM or 1.8 μM) induces apoptosis in SJSA osteosarcoma cells[2].

    上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

    体内研究
    (In Vivo)

    Idasanutlin (RG7388, 25 mg/kg p.o.) results in tumor growth inhibition and regression, in the mouse SJSA human osteosarcoma xenograft model[1]. Idasanutlin (RG7388) induces induction of apoptosis and antiproliferation, in the SJSA xenograft model[2].

    上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

    Clinical Trial

    分子量

    616.48

    Formula

    C31H29Cl2F2N3O4

    CAS 号

    1229705-06-9

    运输条件

    Room temperature in continental US; may vary elsewhere.

    储存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    溶解性数据
    In Vitro: 

    DMSO : ≥ 45 mg/mL (73.00 mM)

    * “≥” means soluble, but saturation unknown.

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 1.6221 mL 8.1106 mL 16.2211 mL
    5 mM 0.3244 mL 1.6221 mL 3.2442 mL
    10 mM 0.1622 mL 0.8111 mL 1.6221 mL

    *

    请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
    储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

    In Vivo:

    请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

    ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
    分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

    • 1.

      请依序添加每种溶剂: 0.5%HPMC  1%Tween80

      Solubility: 10 mg/mL (16.22 mM); Suspended solution; Need ultrasonic

    • 2.

      请依序添加每种溶剂: 10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (4.06 mM); Clear solution

      此方案可获得 ≥ 2.5 mg/mL (4.06 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

      以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

    *以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
    参考文献
    • [1]. Ding Q, et al. Discovery of RG7388, a potent and selective p53-MDM2 inhibitor in clinical development. J Med Chem. 2013 Jul 25;56(14):5979-83.

      [2]. Higgins B, et al. Preclinical optimization of MDM2 antagonist scheduling for cancer treatment by using a model-based approach. Clin Cancer Res. 2014, 20(14), 3742-3752.

    Cell Assay
    [1]

    Cell proliferation is evaluated by the tetrazolium dye assay. The concentration at which 50% inhibition (IC50) or 90% inhibition (IC90) of cell proliferation is determined from the linear regression of a plot of the logarithm of the concentration versus percent inhibition.

    上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [2]

    At 10 to 12 weeks of age, mice are implanted with a 1:1 mixture of human SJSA osteosarcoma cells (ATCC) suspended in phenol-free Matrigel and PBS. Mice are implanted in the right flank at a concentration of 5×106 cells in 0.2 mL total volume. At approximately day 10, animals are randomized according to tumor volume, so that all groups of 10 randomized mice have similar starting mean tumor volumes of 100 to 250 mm3. Idasanutlin (RG7388) is administered as an amorphous solid dispersion microbulk precipitate powder containing 30% drug substance and 70% hydroxypropyl methylcellulose acetate succinate polymer that is reconstituted immediately before administration as a suspension in Klucel/Tween, and remaining suspension is discarded after dosing.

    上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

    参考文献
    • [1]. Ding Q, et al. Discovery of RG7388, a potent and selective p53-MDM2 inhibitor in clinical development. J Med Chem. 2013 Jul 25;56(14):5979-83.

      [2]. Higgins B, et al. Preclinical optimization of MDM2 antagonist scheduling for cancer treatment by using a model-based approach. Clin Cancer Res. 2014, 20(14), 3742-3752.

    所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

    Inavolisib(Synonyms: GDC-0077; RG6114)

    上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

    Inavolisib (Synonyms: GDC-0077; RG6114) 纯度: 98.94%

    GDC-0077 (RG6114) 是一种有效的,口服的选择性 PI3Kα 抑制剂 (IC50=0.038 nM)。GDC-0077 (RG6114) 通过与 PI3K 的 ATP 结合位点结合而发挥其活性,从而抑制了 PIP2 到 PIP3 的磷酸化。与野生型 PI3Kα 相比,GDC-0077 (RG6114) 对突变体的选择性更高。

    Inavolisib(Synonyms: GDC-0077;  RG6114)

    Inavolisib Chemical Structure

    CAS No. : 2060571-02-8

    规格 价格 是否有货 数量
    10 mM * 1 mL in DMSO ¥4950 In-stock
    5 mg ¥4500 In-stock
    10 mg ¥7500 In-stock
    25 mg ¥10500 In-stock
    50 mg ¥16800 In-stock
    100 mg ¥27300 In-stock
    200 mg   询价  
    500 mg   询价  

    * Please select Quantity before adding items.

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    • Angiogenesis Related Compound Library
    • Glucose Metabolism Compound Library
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    生物活性

    GDC-0077 (RG6114) is a potent, orally available, and selective PI3Kα inhibitor (IC50=0.038 nM). GDC-0077 (RG6114) exerts its activity by binding to the ATP binding site of PI3K, thereby inhibiting the phosphorylation of PIP2 to PIP3. GDC-0077 (RG6114) is more selective for mutant versus wild-type PI3Kα[1].

    IC50 & Target[1]

    PI3Kα

    0.038 nM (IC50)

    体外研究
    (In Vitro)

    GDC-0077 (RG6114) is >300-fold more selective for PI3Kα over the other class I PI3K isoforms (β, δ, and γ) and >2000-fold more selective over PIK family members. GDC-0077 selectively degrades mutant PI3Kα in a proteasome-dependent fashion resulting in reduction of PI3K pathway activity biomarkers such as pAKT and pPRAS40, inhibition of cell proliferation, and increased apoptosis in human PIK3CA-mutant breast cancer cell lines to a greater extent when compared to PIK3CA wild-type cells[1].

    上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

    体内研究
    (In Vivo)

    GDC-0077 (p.o.) results in tumor regressions, induction of apoptosis, and a reduction of pAKT, pPRAS40, and pS6RP in a dose-dependent fashion in patient-derived PIK3CA-mutant breast cancer xenograft models[1].

    上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

    Clinical Trial

    分子量

    407.37

    Formula

    C18H19F2N5O4

    CAS 号

    2060571-02-8

    运输条件

    Room temperature in continental US; may vary elsewhere.

    储存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    溶解性数据
    In Vitro: 

    DMSO : 110 mg/mL (270.02 mM; Need ultrasonic)

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 2.4548 mL 12.2739 mL 24.5477 mL
    5 mM 0.4910 mL 2.4548 mL 4.9095 mL
    10 mM 0.2455 mL 1.2274 mL 2.4548 mL

    *

    请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
    储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

    In Vivo:

    请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

    ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
    分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

    • 1.

      请依序添加每种溶剂: 5% DMSO    40% PEG300    5% Tween-80    50% saline

      Solubility: ≥ 2.75 mg/mL (6.75 mM); Clear solution

    • 2.

      请依序添加每种溶剂: 5% DMSO    95% (20% SBE-β-CD in saline)

      Solubility: ≥ 2.75 mg/mL (6.75 mM); Clear solution

    • 3.

      请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.08 mg/mL (5.11 mM); Clear solution

      此方案可获得 ≥ 2.08 mg/mL (5.11 mM,饱和度未知) 的澄清溶液。

      以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

      将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

    • 4.

      请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: ≥ 2.08 mg/mL (5.11 mM); Clear solution

      此方案可获得 ≥ 2.08 mg/mL (5.11 mM,饱和度未知) 的澄清溶液。

      以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

      将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
    • 5.

      请依序添加每种溶剂: 1% DMSO    99% saline

      Solubility: ≥ 0.55 mg/mL (1.35 mM); Clear solution

    *以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
    参考文献
    • [1]. R Hong, Abstract PD4-14: GDC-0077 is a selective PI3Kalpha inhibitor that demonstrates robust efficacy in PIK3CA mutant breast cancer models as a single agent and in combination with standard of care therapies. 2017 San Antonio Breast Cancer Symposium.

    所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

    RO4929097(Synonyms: RG-4733)

    上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

    RO4929097 (Synonyms: RG-4733) 纯度: 98.11%

    RO4929097 (RG-4733) 是一种 γ secretase 抑制剂,IC50 值为 4 nM,能够抑制细胞内 Aβ40 的产生和 Notch 活性,EC50 值分别为 14 nM 和 5 nM。

    RO4929097(Synonyms: RG-4733)

    RO4929097 Chemical Structure

    CAS No. : 847925-91-1

    规格 价格 是否有货 数量
    Free Sample (0.1-0.5 mg)   Apply now  
    10 mM * 1 mL in DMSO ¥880 In-stock
    5 mg ¥800 In-stock
    10 mg ¥1440 In-stock
    50 mg ¥4480 In-stock
    100 mg ¥8400 In-stock
    200 mg   询价  
    500 mg   询价  

    * Please select Quantity before adding items.

    RO4929097 相关产品

    相关化合物库:

    • Drug Repurposing Compound Library Plus
    • Clinical Compound Library Plus
    • Bioactive Compound Library Plus
    • Neuronal Signaling Compound Library
    • Stem Cell Signaling Compound Library
    • Wnt/Hedgehog/Notch Compound Library
    • Anti-Cancer Compound Library
    • Clinical Compound Library
    • Anti-Aging Compound Library
    • Drug Repurposing Compound Library
    • Differentiation Inducing Compound Library
    • Reprogramming Compound Library
    • Anti-Breast Cancer Compound Library
    • Anti-Lung Cancer Compound Library
    • Anti-Pancreatic Cancer Compound Library
    • Neurodegenerative Disease-related Compound Library
    • Angiogenesis Related Compound Library
    • Transcription Factor Targeted Library
    • Anti-Liver Cancer Compound Library
    • Anti-Colorectal Cancer Compound Library

    生物活性

    RO4929097 (RG-4733) is a γ secretase inhibitor with IC50 of 4 nM, inhibiting cellular processing of Aβ40 and Notch with EC50 of 14 nM and 5 nM, respectively[1].

    IC50 & Target

    IC50: 4 nM (γ secretase)[1]

    体外研究
    (In Vitro)

    RO4929097 inhibits the production of ICN reducing the expression of the downstream Notch target, Hes1, producing a less transformed morphology in A549 cells. RO4929097 inhibits Notch processing in human tumor-derived cells[1]. RO4929097 (1 µM) inhibits the growth of breast cancer cells, and the inhibition is 20% for SUM149 and 10% for SUM190 cells. RO4929097 does not have a marked effect in invasiveness of SUM149 cells. RO4929097 significantly reduces colony formation by both cell lines with the effect being more notable in SUM149 than by SUM190 cells[2]. RO4929097 inhibits proliferation, anchorage independent growth, and sphere formation of primary melanoma cells in vitro[3].

    上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

    体内研究
    (In Vivo)

    RO4929097 (3-60 mg/kg, p.o.) results in significant tumor growth inhibition in nude mice bearing A549 NSCLC xenografts, compared with vehicle-treated animals. When mice are treated with 60 mg/kg RO4929097 twice daily with the 7+/14- schedule, treatment initially causes regression of established A549 tumors[1]. RO4929097 impairs the growth of primary melanoma cells in vivo. The percentage of secondary tumors formed by RO4929097-treated cells is lower; the secondary tumors formed by RO4929097-treated cells are smaller; a significant delay in tumor formation by the RO4929097-treated cells compared to the vehicle-treated ones is observed in mice injected with 104 cells in vivo[3].

    上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

    Clinical Trial

    分子量

    469.40

    Formula

    C22H20F5N3O3

    CAS 号

    847925-91-1

    运输条件

    Room temperature in continental US; may vary elsewhere.

    储存方式

    4°C, stored under nitrogen

    *In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

    溶解性数据
    In Vitro: 

    DMSO : ≥ 49 mg/mL (104.39 mM)

    * “≥” means soluble, but saturation unknown.

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 2.1304 mL 10.6519 mL 21.3038 mL
    5 mM 0.4261 mL 2.1304 mL 4.2608 mL
    10 mM 0.2130 mL 1.0652 mL 2.1304 mL

    *

    请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
    储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (stored under nitrogen)。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

    In Vivo:

    请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

    ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
    分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

    • 1.

      请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.5 mg/mL (5.33 mM); Clear solution

      此方案可获得 ≥ 2.5 mg/mL (5.33 mM,饱和度未知) 的澄清溶液。

      以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

      将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

    • 2.

      请依序添加每种溶剂: 10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (5.33 mM); Clear solution

      此方案可获得 ≥ 2.5 mg/mL (5.33 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

      以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

    *以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
    参考文献
    • [1]. Luistro L, et al. Preclinical profile of a potent gamma-secretase inhibitor targeting notch signaling with in vivo efficacy and pharmacodynamic properties. Cancer Res. 2009, 69(19), 7672-7680.

      [2]. Debeb BG, et al. Pre-clinical studies of Notch signaling inhibitor RO4929097 in inflammatory breast cancer cells. Breast Cancer Res Treat. 2012.

      [3]. Huynh C, et al. The novel gamma secretase inhibitor RO4929097 reduces the tumor initiating potential of melanoma. PLoS One. 2011, 6(9), e25264.

    Cell Assay
    [2]

    The IBC cell lines SUM149 and SUM190 are seeded at a density of 5 × 104 cells. The next day, they are treated with vehicle or increasing doses of RO4929097, ranging from 0.1 nM to 10 μM. After 72 hrs, cells are trypsinized and viable cells counted with a hemocytometer.

    上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [1]

    Mice: RO4929097-treated mice are orally dosed with suspensions at 3 to 60 mg/kg RO4929097 according to the indicated regimens. In the Calu-6 xenograft model, RO4929097 is dosed at 60 mg/kg/d every other week for 4 weeks (7+/7- × 2 cycles). For all other xenograft models, RO4929097 is dosed once daily at 10 mg/kg for 21 days. Statistical analysis is determined by Mann-Whitney rank-sum test, one-way ANOVA, and post hoc Bonferroni t test. Differences between groups are considered significant when P ≤ 0.05. A549 tumors from vehicle-treated and selected RO4929097-treated groups are collected and fixed in 10% zinc-formalin overnight, processed, paraffin-embedded, sectioned at 5 μM, and stained with H&E for histopathology assessment. An Olympus BX51 microscope (×40 objective) mounted with a Nikon DS-Fi1 using the NIS-Elements F2.20 program collected the histology pictures. For Western blot analysis, three A549 tumors from each group, 7 (60 mg/kg) or 21 days (3 and 30 mg/kg), are flash-frozen. Collagen type V is detected using the H-200 antibody at a dilution of 1:1,000, and MFAP5 is detected using the antibody at a dilution of 1:1,000.

    上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

    参考文献
    • [1]. Luistro L, et al. Preclinical profile of a potent gamma-secretase inhibitor targeting notch signaling with in vivo efficacy and pharmacodynamic properties. Cancer Res. 2009, 69(19), 7672-7680.

      [2]. Debeb BG, et al. Pre-clinical studies of Notch signaling inhibitor RO4929097 in inflammatory breast cancer cells. Breast Cancer Res Treat. 2012.

      [3]. Huynh C, et al. The novel gamma secretase inhibitor RO4929097 reduces the tumor initiating potential of melanoma. PLoS One. 2011, 6(9), e25264.

    所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

    (20R)-Ginsenoside Rg3(Synonyms: (20R)-人参皂苷Rg3; (20R)-Propanaxadiol; R-ginsenoside Rg3)

    上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

    (20R)-Ginsenoside Rg3 (Synonyms: (20R)-人参皂苷Rg3; (20R)-Propanaxadiol; R-ginsenoside Rg3) 纯度: ≥98.0%

    (20R)-ginsenoside Rg3 ((20R)-Propanaxadiol),人参根中的一种活性化合物,具有抑制血管内皮细胞增生(IC50= 10 nM)和抗肿瘤活性。

    (20R)-Ginsenoside Rg3(Synonyms: (20R)-人参皂苷Rg3; (20R)-Propanaxadiol;  R-ginsenoside Rg3)

    (20R)-Ginsenoside Rg3 Chemical Structure

    CAS No. : 38243-03-7

    规格 价格 是否有货 数量
    10 mM * 1 mL in DMSO ¥691 In-stock
    5 mg ¥500 In-stock
    10 mg ¥800 In-stock
    20 mg ¥1400 In-stock
    50 mg   询价  
    100 mg   询价  

    * Please select Quantity before adding items.

    (20R)-Ginsenoside Rg3 相关产品

    相关化合物库:

    • Natural Product Library Plus
    • Bioactive Compound Library Plus
    • Natural Product Library
    • Anti-Cancer Compound Library
    • Glycoside Compound Library
    • Medicine Food Homology Compound Library
    • Terpenoids Library
    • Traditional Chinese Medicine Monomer Library

    生物活性

    (20R)-ginsenoside Rg3 ((20R)-Propanaxadiol), one of the active compounds present in ginseng root, inhibits vascular endothelial growth factor (VEGF)(IC50=10 nM) and antitumor activities[1][2].

    分子量

    785.01

    Formula

    C42H72O13

    CAS 号

    38243-03-7

    中文名称

    (20R)-人参皂苷Rg3

    运输条件

    Room temperature in continental US; may vary elsewhere.

    储存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    溶解性数据
    In Vitro: 

    DMSO : 41.67 mg/mL (53.08 mM; Need ultrasonic)

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 1.2739 mL 6.3693 mL 12.7387 mL
    5 mM 0.2548 mL 1.2739 mL 2.5477 mL
    10 mM 0.1274 mL 0.6369 mL 1.2739 mL

    *

    请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
    储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

    In Vivo:

    请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

    ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
    分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

    • 1.

      请依序添加每种溶剂: 10% DMSO    90% corn oil

      Solubility: ≥ 4.17 mg/mL (5.31 mM); Clear solution

      此方案可获得 ≥ 4.17 mg/mL (5.31 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

      以 1 mL 工作液为例,取 100 μL 41.7 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

    *以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
    参考文献
    • [1]. Liu L, et al. Enzymatic preparation of 20(S, R)-protopanaxadiol by transformation of 20(S, R)-Rg3 from blackginseng. Phytochemistry. 2010 Sep;71(13):1514-20.

      [2]. Yue PY, et al. The angiosuppressive effects of 20(R)- ginsenoside Rg3. Biochem Pharmacol. 2006 Aug 14;72(4):437-45.

    所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

    RGLS4326(Synonyms: RG4326)

    上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

    RGLS4326 (Synonyms: RG4326)

    RGLS4326 (RG4326) 是一种首创的 microRNA-17 (miR-17) 寡核苷酸抑制剂。RGLS4326 可用于常染色体显性多囊肾病 (ADPKD) 的研究。RGLS4326 作用于 HeLa 细胞,抑制 miR-17 功能,EC50 值为 28.3 nM。

    RGLS4326(Synonyms: RG4326)

    RGLS4326 Chemical Structure

    CAS No. : 2229964-07-0

    规格 是否有货
    100 mg   询价  
    250 mg   询价  
    500 mg   询价  

    * Please select Quantity before adding items.

    生物活性

    RGLS4326 (RG4326) is a first-in-class, short oligonucleotide inhibitor of microRNA-17 (miR-17). RGLS4326 can be used for the research of autosomal dominant polycystic kidney disease (ADPKD). RGLS4326 inhibits miR-17 function in HeLa cells with an EC50 value of 28.3 nM[1].

    IC50 & Target

    MicroRNA[1]

    体外研究
    (In Vitro)

    RGLS4326, a single-stranded, chemically modified, short oligonucleotide of 9-nt with full complementarity to the miR-17 seed sequence. RGLS4326 inhibits the pathologic functions of the miR-17 family of miRNAs in ADPKD[1].
    RGLS4326 treatment inhibits miR-17 function in kidney collecting duct cells in culture as measured by miR-17 PD-Sig, with an EC50 value of 77.2 ± 20.2 nM[1].
    RGLS4326 suppresses the growth of primary human autosomal dominant polycystic kidney disease (ADPKD) cysts[1].

    Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

    Cell Proliferation Assay[1]

    Cell Line: Primary cysts in 3D Matrigel
    Concentration: 5, 20, 100, and 300  nM
    Incubation Time: 9 days
    Result: Decreased in cyst epithelial cell proliferation.

    体内研究
    (In Vivo)

    RGLS4326 preferentially distributes to kidney tubules and cysts. RGLS4326 (a single 30 mg/kg SC injection) is rapidly absorbed into plasma, showing Tmax of ≤1 h, Cmax of 8.5 µg/mL, and half-life of <4 h in wild-type mice[1].
    In vivo administration of RGLS4326 also upregulates the expression of the direct miR-17 target genes Pkd1 and Pkd2[1].

    Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Model: Pkd2-KO mice[1]
    Dosage: 20 mg/kg
    Administration: SC injection
    Result: Compared to non-cystic control kidneys, polycystic kidneys of PBS-treated Pkd2-KO mice exhibit an age-dependent progressive decline in miR-17 PD-Sig, indicative of increasing miR-17 activity with disease progression.
    Administration of RGLS4326 reversed this decline in miR-17 PD-Sig, indicating a sustained functional inhibition of miR-17.

    分子量

    3082.42

    Formula

    C95H115F3N32O51P8S8

    CAS 号

    2229964-07-0

    运输条件

    Room temperature in continental US; may vary elsewhere.

    储存方式

    Please store the product under the recommended conditions in the Certificate of Analysis.

    参考文献
    • [1]. Edmund C Lee, et al. Discovery and preclinical evaluation of anti-miR-17 oligonucleotide RGLS4326 for the treatment of polycystic kidney disease. Nat Commun. 2019 Sep 12;10(1):4148.

    所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

    RG108(Synonyms: N-Phthalyl-L-tryptophan)

    上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

    RG108 (Synonyms: N-Phthalyl-L-tryptophan) 纯度: 99.61%

    RG108 (N-Phthalyl-L-tryptophan) 是一种非核苷的 DNA 甲基转移酶 (DNMTs) 抑制剂 (IC50=115 nM),RG108 (N-Phthalyl-L-tryptophan) 阻断 DNA 甲基转移酶的活性位点。RG108 (N-Phthalyl-L-tryptophan) 引起抑癌基因的去甲基化和再激活,但不影响着丝粒卫星序列的甲基化。

    RG108(Synonyms: N-Phthalyl-L-tryptophan)

    RG108 Chemical Structure

    CAS No. : 48208-26-0

    规格 价格 是否有货 数量
    10 mM * 1 mL in DMSO ¥932 In-stock
    10 mg ¥847 In-stock
    50 mg ¥3530 In-stock
    100 mg   询价  
    200 mg   询价  

    * Please select Quantity before adding items.

    RG108 相关产品

    相关化合物库:

    • Bioactive Compound Library Plus
    • Epigenetics Compound Library
    • Anti-Cancer Compound Library
    • Peptidomimetic Library
    • Reprogramming Compound Library
    • Anti-Blood Cancer Compound Library
    • Transcription Factor Targeted Library

    生物活性

    RG108 (N-Phthalyl-L-tryptophan) is a non-nucleoside DNA methyltransferases (DNMTs) inhibitor (IC50=115 nM) that blocks the DNMTs active site. RG108 (N-Phthalyl-L-tryptophan) causes demethylation and reactivation of tumor suppressor genes, but it does not affect the methylation of centromeric satellite sequences[1][2][3].

    IC50 & Target[1]

    CpG methylase M.SssI

    115 nM (IC50)

    体外研究
    (In Vitro)

    RG108 effectively blocks DNA methyltransferases in vitro and does not cause covalent enzyme trapping in human cell lines. Incubation of cells with low micromolar concentrations of RG108 results in significant demethylation of genomic DNA without any detectable toxicity. Intriguingly, RG108 causes demethylation and reactivation of tumor suppressor genes, but it does not affect the methylation of centromeric satellite sequences[1]. In another study, the synthesis and in vitro analysis of a biotinylated RG108 conjugate is investigated to evaluate the interactions with DNA methyltransferase enzymes[2]. In a recent study, it is shown RG108 can significantly reduce the DNA methyltransferases activity in SM derived iPS cells as compared to the native SMs[3].

    上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

    分子量

    334.33

    Formula

    C19H14N2O4

    CAS 号

    48208-26-0

    运输条件

    Room temperature in continental US; may vary elsewhere.

    储存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    溶解性数据
    In Vitro: 

    DMSO : 100 mg/mL (299.11 mM; Need ultrasonic)

    H2O : < 0.1 mg/mL (insoluble)

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 2.9911 mL 14.9553 mL 29.9106 mL
    5 mM 0.5982 mL 2.9911 mL 5.9821 mL
    10 mM 0.2991 mL 1.4955 mL 2.9911 mL

    *

    请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
    储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

    In Vivo:

    请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

    ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
    分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

    • 1.

      请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.08 mg/mL (6.22 mM); Clear solution

      此方案可获得 ≥ 2.08 mg/mL (6.22 mM,饱和度未知) 的澄清溶液。

      以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

      将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

    • 2.

      请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: ≥ 2.08 mg/mL (6.22 mM); Clear solution

      此方案可获得 ≥ 2.08 mg/mL (6.22 mM,饱和度未知) 的澄清溶液。

      以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

      将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
    • 3.

      请依序添加每种溶剂: 10% DMSO    90% corn oil

      Solubility: ≥ 2.08 mg/mL (6.22 mM); Clear solution

      此方案可获得 ≥ 2.08 mg/mL (6.22 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

      以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

    • 4.

      请依序添加每种溶剂: PBS

      Solubility: 1 mg/mL (2.99 mM); Clear solution; Need ultrasonic and warming and heat to 70°C

    *以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
    参考文献
    • [1]. Brueckner B, et al. Epigenetic reactivation of tumor suppressor genes by a novel small-molecule inhibitor of human DNA methyltransferases. Cancer Res. 2005 Jul 15;65(14):6305-11.

      [2]. Schirrmacher E, et al. Synthesis and in vitro evaluation of biotinylated RG108: a high affinity compound for studying binding interactions with human DNA methyltransferases. Bioconjug Chem. 2006 Mar-Apr;17(2):261-6.

      [3]. Pasha Z, et al. Efficient non-viral reprogramming of myoblasts to stemness with a single small molecule to generate cardiac progenitor cells. PLoS One. 2011;6(8):e23667.

    Kinase Assay
    [1]

    The substrate DNA for the in vitro methylation assay is a 798 bp fragment (−423/+375 relative to the initiation codon) from the promoter region of the human p16Ink4a gene. The methylation reaction contains 350 to 400 ng substrate DNA and 4 units of M.SssI methylase (0.5 μM) in a final volume of 50 μL. Inhibitors are added to final concentrations of 10, 100, 200, and 500 μM, respectively. Reactions are done at 37°C for 2 hours. After completion, the reaction is inactivated at 65°C for 15 minutes and the DNA is purified using PCR Purification kit. Three hundred nanograms of purified DNA is digested for 3 hours at 60°C with 30 units of BstUI and analyzed on 2% Tris-borate EDTA agarose gels.

    上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

    参考文献
    • [1]. Brueckner B, et al. Epigenetic reactivation of tumor suppressor genes by a novel small-molecule inhibitor of human DNA methyltransferases. Cancer Res. 2005 Jul 15;65(14):6305-11.

      [2]. Schirrmacher E, et al. Synthesis and in vitro evaluation of biotinylated RG108: a high affinity compound for studying binding interactions with human DNA methyltransferases. Bioconjug Chem. 2006 Mar-Apr;17(2):261-6.

      [3]. Pasha Z, et al. Efficient non-viral reprogramming of myoblasts to stemness with a single small molecule to generate cardiac progenitor cells. PLoS One. 2011;6(8):e23667.

    所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

    RG7112(Synonyms: RO5045337)

    上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

    RG7112 (Synonyms: RO5045337) 纯度: 99.86%

    RG7112 是有效的、选择性的、第一个用于临床的、可口服的、可透过血脑屏障的、 MDM2-p53 抑制剂,IC50 值为 18 nM,结合到MDM2 的KD 值为 11 nM.

    RG7112(Synonyms: RO5045337)

    RG7112 Chemical Structure

    CAS No. : 939981-39-2

    规格 价格 是否有货 数量
    Free Sample (0.1-0.5 mg)   Apply now  
    10 mM * 1 mL in DMSO ¥1761 In-stock
    5 mg ¥1100 In-stock
    10 mg ¥1900 In-stock
    25 mg ¥3800 In-stock
    50 mg ¥5700 In-stock
    100 mg ¥8500 In-stock
    200 mg   询价  
    500 mg   询价  

    * Please select Quantity before adding items.

    RG7112 相关产品

    相关化合物库:

    • Clinical Compound Library Plus
    • Bioactive Compound Library Plus
    • Apoptosis Compound Library
    • Metabolism/Protease Compound Library
    • Anti-Cancer Compound Library
    • Clinical Compound Library
    • CNS-Penetrant Compound Library
    • Autophagy Compound Library
    • Anti-Aging Compound Library
    • Oxygen Sensing Compound Library
    • Ubiquitination Compound Library
    • Ferroptosis Compound Library
    • Pyroptosis Compound Library
    • Orally Active Compound Library
    • Chemical Probe Library
    • Glutamine Metabolism Compound Library
    • Anti-Pancreatic Cancer Compound Library
    • Anti-Blood Cancer Compound Library
    • Transcription Factor Targeted Library
    • Anti-Liver Cancer Compound Library
    • Anti-Colorectal Cancer Compound Library

    生物活性

    RG7112 is a potent, selective, first clinical, orally active and blood-brain barrier crossed MDM2-p53 inhibitor, with an IC50 of 18 nM and a KD of 11 nM for binding to MDM2[1].

    IC50 & Target

    Kd: 11 nM (MDM2)[1]

    体外研究
    (In Vitro)

    RG7112 (0-5 μM) stabilizes wild-type p53 and induces p53 signaling in cancer cells. RG7112 effectively activates p53 functions in cancer cells[1][2].

    上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

    Cell Proliferation Assay[2]

    Cell Line: SJSA1 osteosarcoma cells.
    Concentration: 0-5 μM.
    Incubation Time: 0-60 hours.
    Result: Dose-dependently inhibited the growth and killed SJSA1 osteosarcoma cells expressing high levels of MDM2 protein due to MDM2 gene amplification.

    Cell Cycle Analysis[2]

    Cell Line: HCT116 and SJSA1 cells.
    Concentration: 0-5 μM.
    Incubation Time: 48 hours.
    Result: Induced a dose-dependent cell cycle block in G1 and G2/M phase and depletion of the S phase compartment.

    体内研究
    (In Vivo)

    RG7112 (25-200 mg/kg, single oral dose) activates p53 pathway and induces apoptosis in tumor cells in vivo[2].
    RG7112 (100 mg/kg, gavage once per day, 5 days/week for 3 weeks ) reduces tumor growth rate and increases survival in GBM models[3].

    上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Model: Female Balb/c nude mice[2].
    Dosage: 25-200 mg/kg.
    Administration: Orally, single dose.
    Result: At the highest dose level of RG7112 (200 mg/kg) only 1.2% (± 0.89 SD) of cells incorporated BrdU at 24 h post-dosing, vs. 14% (± 1.83 SD) of vehicle treated tumors.
    Animal Model: GBM cells were implanted into the brain of Athymic Nude mice (7 weeks old females, 10 animals/group)[3].
    Dosage: 100 mg/kg.
    Administration: Oral gavage, once per day, 5 days/week for 3 weeks.
    Result: Reduced tumor growth rate and increases survival in heterotopic and orthotopic animal models bearing MDM2-amplified GBM.

    Clinical Trial

    分子量

    727.78

    Formula

    C38H48Cl2N4O4S

    CAS 号

    939981-39-2

    运输条件

    Room temperature in continental US; may vary elsewhere.

    储存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    溶解性数据
    In Vitro: 

    DMSO : 200 mg/mL (274.81 mM; Need ultrasonic)

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 1.3740 mL 6.8702 mL 13.7404 mL
    5 mM 0.2748 mL 1.3740 mL 2.7481 mL
    10 mM 0.1374 mL 0.6870 mL 1.3740 mL

    *

    请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
    储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

    In Vivo:

    请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

    ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
    分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

    • 1.

      请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 10 mg/mL (13.74 mM); Clear solution

      此方案可获得 ≥ 10 mg/mL (13.74 mM,饱和度未知) 的澄清溶液。

      以 1 mL 工作液为例,取 100 μL 100.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

      将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

    • 2.

      请依序添加每种溶剂: 10% DMSO    90% corn oil

      Solubility: ≥ 10 mg/mL (13.74 mM); Clear solution

      此方案可获得 ≥ 10 mg/mL (13.74 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

      以 1 mL 工作液为例,取 100 μL 100.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

    • 3.

      请依序添加每种溶剂: 5% DMSO    40% PEG300    5% Tween-80    50% saline

      Solubility: ≥ 5 mg/mL (6.87 mM); Clear solution

    • 4.

      请依序添加每种溶剂: 5% DMSO    95% (20% SBE-β-CD in saline)

      Solubility: ≥ 2.5 mg/mL (3.44 mM); Clear solution

    *以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
    参考文献
    • [1]. Vu B, et al. Discovery of RG7112: A Small-Molecule MDM2 Inhibitor in Clinical Development. ACS Med Chem Lett. 2013 Apr 2;4(5):466-9.

      [2]. Tovar C, et al. MDM2 small-molecule antagonist RG7112 activates p53 signaling and regresses human tumors in preclinical cancer models. Cancer Res. 2013 Apr 15;73(8):2587-97.

      [3]. Verreault M, et al. Preclinical Efficacy of the MDM2 Inhibitor RG7112 in MDM2-Amplified and TP53 Wild-type Glioblastomas. Clin Cancer Res. 2016 Mar 1;22(5):1185-96.

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    Lavendustin A(Synonyms: 薰草菌素; RG-14355)

    上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

    Lavendustin A (Synonyms: 薰草菌素; RG-14355)

    Lavendustin A (RG-14355), 可从Streptomyces Griseolavendus 中分离得到,是一种有效的、特异性的、ATP竞争性的酪氨酸激酶抑制剂,对表皮生长因子受体 (EGFR) 相关酪氨酸激酶的 IC50 值为 11 ng/mL。 能抑制血管内皮生长因子诱导的血管生成,阻断LTPGABA-A的诱导。

    Lavendustin A(Synonyms: 薰草菌素; RG-14355)

    Lavendustin A Chemical Structure

    CAS No. : 125697-92-9

    规格 价格 是否有货
    1 mg ¥2800 询问价格 & 货期
    5 mg ¥7200 询问价格 & 货期
    10 mg ¥10800 询问价格 & 货期

    * Please select Quantity before adding items.

    生物活性

    Lavendustin A (RG-14355), isolated from Streptomyces Griseolavendus, is a potent, specific and ATP-competitive inhibitor of tyrosine kinase, with an IC50 of 11 ng/mL for EGFR-associated tyrosine kinase[1]. It suppresses VEGF-induced angiogenesis and blocks the induction of LTPGABA-A[2][3].

    IC50 & Target

    IC50: 11 ng/mL (EGFR-associated tyrosine kinase)[1].

    分子量

    381.38

    Formula

    C21H19NO6

    CAS 号

    125697-92-9

    中文名称

    薰草菌素

    运输条件

    Room temperature in continental US; may vary elsewhere.

    储存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    溶解性数据
    In Vitro: 

    DMSO : ≥ 250 mg/mL (655.51 mM)

    * “≥” means soluble, but saturation unknown.

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 2.6221 mL 13.1103 mL 26.2206 mL
    5 mM 0.5244 mL 2.6221 mL 5.2441 mL
    10 mM 0.2622 mL 1.3110 mL 2.6221 mL

    *

    请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
    储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

    In Vivo:

    请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

    ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
    分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

    • 1.

      请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.08 mg/mL (5.45 mM); Clear solution

      此方案可获得 ≥ 2.08 mg/mL (5.45 mM,饱和度未知) 的澄清溶液。

      以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

      将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

    • 2.

      请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: ≥ 2.08 mg/mL (5.45 mM); Clear solution

      此方案可获得 ≥ 2.08 mg/mL (5.45 mM,饱和度未知) 的澄清溶液。

      以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

      将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
    *以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
    参考文献
    • [1]. Onoda T, et al. Isolation of a novel tyrosine kinase inhibitor, lavendustin A, from Streptomyces griseolavendus. J Nat Prod. 1989 Nov-Dec;52(6):1252-7.

      [2]. Hu DE, et al. Suppression of VEGF-induced angiogenesis by the protein tyrosine kinase inhibitor, lavendustin A. Br J Pharmacol. 1995 Jan;114(2):262-8.

      [3]. Gubellini P, et al. Endogenous neurotrophins are required for the induction of GABAergic long-term potentiation in the neonatal rat hippocampus. J Neurosci. 2005 Jun 15;25(24):5796-802.

    所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

    Ginsenoside Rg5(Synonyms: 人参皂甙 Rg5)

    上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

    Ginsenoside Rg5 (Synonyms: 人参皂甙 Rg5) 纯度: 99.86%

    Ginsenoside Rg5 是红参的主要成分。Ginsenoside Rg5 阻断 IGF-1 与其受体的结合,IC50 约为90 nM。Ginsenoside Rg5 还通过抑制 NF-κB p65 的 DNA 结合活性来抑制 COX-2 的 mRNA 表达。

    Ginsenoside Rg5(Synonyms: 人参皂甙 Rg5)

    Ginsenoside Rg5 Chemical Structure

    CAS No. : 186763-78-0

    规格 价格 是否有货 数量
    10 mM * 1 mL in DMSO ¥3797 In-stock
    5 mg ¥2800 In-stock
    10 mg ¥4500 In-stock
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    100 mg   询价  

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    生物活性

    Ginsenoside Rg5 is the main component of Red ginseng. Ginsenoside blocks binding of IGF-1 to its receptor with an IC50 of ~90 nM. Ginsenoside Rg5 also inhibits the mRNA expression of COX-2 via suppression of the DNA binding activities of NF-κB p65.

    IC50 & Target[1][2]

    p65

     

    COX-2

     

    IGF-1R

    90 nM (IC50)

    体外研究
    (In Vitro)

    Ginsenoside Rg5 plays a novel role as an IGF-1R agonist. Ginsenoside Rg5 binds to IGF-1R with an IC50 value of ~90 and its angiogenic activity is inhibited by IGF-1R knockdown. To investigate the possible interaction of Ginsenoside Rg5 with IGF-1R, a docking analysis is performed. Docking results show that Ginsenoside Rg5 binds strongly at two sites, A and B, with Kd values of 20 and 27 nM, respectively, to the cysteine-rich domain of IGF-1R. Pretreatment with Rg5 blocks the binding of radiolabeled IGF-1 to HUVECs with an IC50 value of ~90 μM, which is greater than an IC50 value of ~1.4 nM for unlabeled IGF-1[1]. The results from MTT assay show that MCF-7 cell proliferation is inhibited by Ginsenoside Rg5 treatment for 24, 48 and 72 h in a dose-dependent manner. Ginsenoside Rg5 at different concentrations (0, 25, 50 and 100 μM), induce cell cycle arrest in G0/G1 phase through regulation of cell cycle-related proteins in MCF-7 cells[3].

    上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

    体内研究
    (In Vivo)

    Ginsenoside Rg5 inhibits the mRNA expression of COX-2 via suppression of the DNA binding activities of NF-κB p65 in lipopolysaccharides (LPS)-stimulated BV2 microglial cells. Rg5 pretreated group mice show declined expression of NF-κB p65 and COX-2. In the group treated with low dose of Ginsenoside Rg5 (10 mg/kg), there is remarkable tubular damage and infiltration of inflammatory cells. However, at the higher dose of Ginsenoside Rg5 (20 mg/kg), tubules markedly appeare histologically normal and no inflammation and cast formation is observed in kidney tissues[2].

    上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

    分子量

    767.00

    Formula

    C42H70O12

    CAS 号

    186763-78-0

    中文名称

    人参皂甙 Rg5

    运输条件

    Room temperature in continental US; may vary elsewhere.

    储存方式
    Powder -20°C 3 years
    In solvent -80°C 6 months
    -20°C 1 month
    溶解性数据
    In Vitro: 

    DMSO : 100 mg/mL (130.38 mM; Need ultrasonic)

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 1.3038 mL 6.5189 mL 13.0378 mL
    5 mM 0.2608 mL 1.3038 mL 2.6076 mL
    10 mM 0.1304 mL 0.6519 mL 1.3038 mL

    *

    请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
    储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

    In Vivo:

    请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

    ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
    分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

    • 1.

      请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.5 mg/mL (3.26 mM); Clear solution

      此方案可获得 ≥ 2.5 mg/mL (3.26 mM,饱和度未知) 的澄清溶液。

      以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

      将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

    • 2.

      请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: ≥ 2.5 mg/mL (3.26 mM); Clear solution

      此方案可获得 ≥ 2.5 mg/mL (3.26 mM,饱和度未知) 的澄清溶液。

      以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

      将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
    • 3.

      请依序添加每种溶剂: 10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (3.26 mM); Clear solution

      此方案可获得 ≥ 2.5 mg/mL (3.26 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

      以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

    *以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
    参考文献
    • [1]. Cho YL, et al. Specific activation of insulin-like growth factor-1 receptor by ginsenoside Rg5 promotes angiogenesis and vasorelaxation. J Biol Chem. 2015 Jan 2;290(1):467-77.

      [2]. Li W, et al. Ginsenoside Rg5 Ameliorates Cisplatin-Induced Nephrotoxicity in Mice through Inhibition of Inflammation, Oxidative Stress, and Apoptosis. Nutrients. 2016 Sep 13;8(9). pii: E566.

      [3]. Kim SJ, et al. Anti-breast cancer activity of Fine Black ginseng (Panax ginseng Meyer) and ginsenoside Rg5. J Ginseng Res. 2015 Apr;39(2):125-34.

    Kinase Assay
    [1]

    HUVECs are cultured in 24-well plates overnight. The cells are changed to serum-free M199 and incubated for 1 h. The medium is removed, and cells are incubated with fresh serum-free medium containing 0.1 μM-50 mM Ginsenoside Rg5 at 37°C for 20 min followed by the addition of 50 μL (1 μCi) of [125I]IGF-1 and then further incubated for 10 min. The medium is decanted, and cell plates are washed twice with serum-free medium. Cells are lysed in 300 μL of 0.1 N NaOH solution containing 0.1% SDS, transferred to scintillation vials, and mixed with 1 mL of Ultima Gold mixture solution. Cell-associated [125I]IGF-1 is analyzed in a scintillation counter. The nonspecific binding is determined by coincubation with unlabeled IGF-1 (50 nM)[1].

    上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

    Cell Assay
    [3]

    MCF-7 (HER2/ER+) and MDA-MB-453 (HER2+/ER) human breast cancer cell lines are maintained using RPMI 1640 medium supplemented with 10% (vol/vol) FBS plus 100 units/mL Penicillin and Streptomycin in a 5% carbon dioxide air incubator at 37°C. Cell cytotoxicity is measured by MTT assay. Cells are seeded in 96-well tissue culture plates at the density of 0.2×104 cells per well with 100 μL medium, and are allowed to become attached for 24 h. One hundred microliters of the medium with different concentrations of Ginsenoside Rg5 (e.g., 0 μM, 25 μM, 50 μM, and 100 μM) are added to each well. At indicated times, 30 μL MTT stock solution (3 mg/mL) are added to each well. After culturing the cells at 37°C for 2 h, DMSO is added to dissolve the formazan crystals. The absorbance is read at the wavelength of 540 nm with a microplate reader[3].

    上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [2]

    Mice[2]
    Male ICR mice (6 to 8 weeks old), weighing 25-27 g, are used. After acclimation for one week, mice are randomly assigned into 4 experimental groups with 8 mice in each group: normal control, Cisplatin control, and Cisplatin+Ginsenoside Rg5 groups (10 and 20 mg/kg, respectively). Ginsenoside Rg5 is administered intragastrically at the dose of 10 and 20 mg/kg for 10 days. On the 7th day, animals in Cisplatin control and Ginsenoside Rg5-treated groups receive a single intraperitoneal injection of Cisplatin (25 mg/kg) to induce nephrotoxicity in mice. Mice are anaesthetized with pentobarbital, subsequently sacrificed at 72 h after Cisplatin injection (Day 10). Blood samples are collected and then centrifuged at 3000 rpm to separate the serum and stored at -20 °C for determining blood urea nitrogen (BUN) and creatinine (CRE) levels.

    上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

    参考文献
    • [1]. Cho YL, et al. Specific activation of insulin-like growth factor-1 receptor by ginsenoside Rg5 promotes angiogenesis and vasorelaxation. J Biol Chem. 2015 Jan 2;290(1):467-77.

      [2]. Li W, et al. Ginsenoside Rg5 Ameliorates Cisplatin-Induced Nephrotoxicity in Mice through Inhibition of Inflammation, Oxidative Stress, and Apoptosis. Nutrients. 2016 Sep 13;8(9). pii: E566.

      [3]. Kim SJ, et al. Anti-breast cancer activity of Fine Black ginseng (Panax ginseng Meyer) and ginsenoside Rg5. J Ginseng Res. 2015 Apr;39(2):125-34.

    所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

    20(S)-Ginsenoside Rg3(Synonyms: 20(S)-人参皂苷 Rg3; 20(S)-Propanaxadiol; S-ginsenoside Rg3)

    上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

    20(S)-Ginsenoside Rg3 (Synonyms: 20(S)-人参皂苷 Rg3; 20(S)-Propanaxadiol; S-ginsenoside Rg3) 纯度: 98.10%

    20(S)-Ginsenoside Rg3 是红参的主要成分。20(S)-Ginsenoside Rg3 抑制 Na+hKv1.4 通道,IC50 分别为 32.2±4.5 和 32.6±2.2 μM。20(S)-Ginsenoside Rg3 还抑制 NF-κB 活性和 COX-2 表达。

    20(S)-Ginsenoside Rg3(Synonyms: 20(S)-人参皂苷 Rg3; 20(S)-Propanaxadiol;  S-ginsenoside Rg3)

    20(S)-Ginsenoside Rg3 Chemical Structure

    CAS No. : 14197-60-5

    规格 价格 是否有货 数量
    10 mM * 1 mL in DMSO ¥563 In-stock
    10 mg ¥512 In-stock
    50 mg ¥1097 In-stock
    100 mg ¥1953 In-stock
    200 mg   询价  
    500 mg   询价  

    * Please select Quantity before adding items.

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    生物活性

    20(S)-Ginsenoside Rg3 is the main component of Red ginseng. Ginsenoside Rg3 inhibits Na+ and hKv1.4 channel with IC50s of 32.2±4.5 and 32.6±2.2 μM, respectively. 20(S)-Ginsenoside Rg3 also inhibits levels, NF-κB activity, and COX-2 expression.

    IC50 & Target

    p65

     

    COX-2

     

    Human Endogenous Metabolite

     

    Na+ channel

    32.2 μM (IC50)

    hKv1.4 channel

    32.6 μM (IC50)

    Aβ40

     

    Aβ42

     

    体外研究
    (In Vitro)

    Ginsenoside Rg3 plays an important role in its effect on the Na+ channel. Treatment with Ginsenoside Rg3 reversibly inhibits the inward Na+ peak current (INa) with an IC50 of 32.2±4.5 μM, and the inhibition is voltage-dependent[1]. Ginsenoside Rg3 at 100 μM inhibits the hKv1.4 channel currents by an average of 65%.The Ginsenoside Rg3 effect is concentration-dependent and reversible. The IC50 value and Hill coefficient are 32.6±2.2 μM and 1.59±0.13, respectively[2]. Ginsenoside Rg3 shows the significant inhibition of NF-κB activity thereby reduced COX-2 expression. To examine the cytotoxicity of Ginsenoside Rg3 on IL-1β-induced inflamed A549 cells, the cells are firstly treated with IL-1β (10 ng/mL) for 4 h and treated with 100 to 900 ng/mL concentration of Ginsenoside Rg3 for 12 h. Cell viability is analyzed using an MTT assay. There is no observed cytotoxicity of Ginsenoside Rg3 in IL-1β-induced inflamed A549 cells compared to only PBS-treated cells (Con).To obtain the anti-inflammatory effects of Ginsenoside Rg3 on inflammation induced human lung epithelial cells, A549 cells inflammation is induced by IL-1β (10 ng/mL) and then treated by 5 μM of Dexamethasone (Dex) or 900 nM of Rg3. The NF-κB activation is analyzed by a western blot analysis to evaluate the effect of Ginsenoside Rg3 treatment on A549 cells. Phospho-NF-κB p65/total NF-κB p65 densitometry in the cells treated with Rg3 shows the significant decrease compared to IL-1β-induced inflamed A549 cells. The meaning of reducing the ratio of p-p65/p65 by Rg3 treatment is associated with NF-κB activation. Ginsenoside Rg3 also downregulates the expression of COX-2 effectively[3].

    上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

    体内研究
    (In Vivo)

    Ginsenoside Rg3 ((20S)-Rg3) is an Aβ-lowering Natural Compound. APP/PS1 mice are treated with Ginsenoside Rg3 once a day for 4 weeks by intraperitoneal injection (10 mg/kg/day). Aβ ELISA analysis of brain tissues reveal that Ginsenoside Rg3 treatment results in a significant reduction of Aβ40 and Aβ42 in the brain[4].

    上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

    分子量

    785.01

    Formula

    C42H72O13

    CAS 号

    14197-60-5

    中文名称

    20(S)-人参皂苷 Rg3

    运输条件

    Room temperature in continental US; may vary elsewhere.

    储存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    溶解性数据
    In Vitro: 

    DMSO : 100 mg/mL (127.39 mM; Need ultrasonic)

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 1.2739 mL 6.3693 mL 12.7387 mL
    5 mM 0.2548 mL 1.2739 mL 2.5477 mL
    10 mM 0.1274 mL 0.6369 mL 1.2739 mL

    *

    请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
    储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

    In Vivo:

    请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

    ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
    分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

    • 1.

      请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.5 mg/mL (3.18 mM); Clear solution

      此方案可获得 ≥ 2.5 mg/mL (3.18 mM,饱和度未知) 的澄清溶液。

      以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

      将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

    • 2.

      请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: ≥ 2.5 mg/mL (3.18 mM); Clear solution

      此方案可获得 ≥ 2.5 mg/mL (3.18 mM,饱和度未知) 的澄清溶液。

      以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

      将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
    • 3.

      请依序添加每种溶剂: 10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (3.18 mM); Clear solution

      此方案可获得 ≥ 2.5 mg/mL (3.18 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

      以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

    *以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
    参考文献
    • [1]. Kim JH, et al. A role for the carbohydrate portion of ginsenoside Rg3 in Na+ channel inhibition. Mol Cells. 2005 Feb 28;19(1):137-42.

      [2]. Lee JH, et al. Ginsenoside Rg3 inhibits human Kv1.4 channel currents by interacting with the Lys531 residue. Mol Pharmacol. 2008 Mar;73(3):619-26.

      [3]. Lee IS, et al. Anti-Inflammatory Effects of Ginsenoside Rg3 via NF-κB Pathway in A549 Cells and Human Asthmatic Lung Tissue. J Immunol Res. 2016;2016:7521601.

      [4]. Kang MS, et al. Modulation of lipid kinase PI4KIIα activity and lipid raft association of presenilin 1 underlies γ-secretase inhibition by ginsenoside (20S)-Rg3. J Biol Chem. 2013 Jul 19;288(29):20868-82.

    Cell Assay
    [3]

    MTT assays are performed to evaluate the cytotoxicity of Ginsenoside Rg3 on inflamed cells. Ten thousands of A549 cells cultured each well of 96-well plate and are incubated at 37°C and 5% CO2 overnight. After serum starvation using DMEM low glucose without FBS, the medium is changed into RPMI containing IL-1β (10 ng/mL) and the cells are incubated at 37°C and 5% CO2 for 4 h. After 4 h incubation, the cells are treated with Ginsenoside Rg3 (100-900 nM) for 12 h. Thirty microliters of MTT solution (5 mg/mL) is added to each well and the cells are incubated for 2 h. After 2 h incubation in cell culture incubator, the medium containing MTT solution of each well is removed and 50 μL of DMSO is added. Using an automated spectrophotometric plate reader at 570 nm, the optical density of formazan is measured[3].

    上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [4]

    Mice[4]
    The mice used are heterozygous, double transgenic animals expressing both human APP(K670N/M671L) and PS1(M146L) proteins. These Alzheimer disease model mice are age-matched (3 months old) in all experiments with wild-type littermates. Both sets of mice are produced by crossing heterozygous APP mice with heterozygous PS1 mice and are weaned at 3 weeks and genotyped by PCR of digested tail samples. Ginsenoside Rg3 is prepared in a saline solution containing 0.01% DMSO at a concentration of 10 mg/kg of body weight. Ginsenoside Rg3 (or saline with 0.01% DMSO for controls) is administered daily via intraperitoneal injection. After sacrifice, one hemibrain from each mouse is frozen on dry ice, homogenized in sucrose buffer, and extracted via formic acid for Aβ quantification using a commercial sandwich ELISA kit.

    上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

    参考文献
    • [1]. Kim JH, et al. A role for the carbohydrate portion of ginsenoside Rg3 in Na+ channel inhibition. Mol Cells. 2005 Feb 28;19(1):137-42.

      [2]. Lee JH, et al. Ginsenoside Rg3 inhibits human Kv1.4 channel currents by interacting with the Lys531 residue. Mol Pharmacol. 2008 Mar;73(3):619-26.

      [3]. Lee IS, et al. Anti-Inflammatory Effects of Ginsenoside Rg3 via NF-κB Pathway in A549 Cells and Human Asthmatic Lung Tissue. J Immunol Res. 2016;2016:7521601.

      [4]. Kang MS, et al. Modulation of lipid kinase PI4KIIα activity and lipid raft association of presenilin 1 underlies γ-secretase inhibition by ginsenoside (20S)-Rg3. J Biol Chem. 2013 Jul 19;288(29):20868-82.

    所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

    GDC-0623(Synonyms: RG 7421; MEK inhibitor 1)

    上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

    GDC-0623 (Synonyms: RG 7421; MEK inhibitor 1) 纯度: 99.15%

    GDC-0623 (RG 7421) 是一种有效的,ATP 竞争性的 MEK1 抑制剂,Ki值为 0.13 nM,对 HCT116 细胞中 KRAS (G13D)的 EC50 值为 42 nM,而对 A375 细胞中 BRAFV600E的 EC50 值为 7 nM。

    GDC-0623(Synonyms: RG 7421;  MEK inhibitor 1)

    GDC-0623 Chemical Structure

    CAS No. : 1168091-68-6

    规格 价格 是否有货 数量
    Free Sample (0.1-0.5 mg)   Apply now  
    10 mM * 1 mL in DMSO ¥1405 In-stock
    2 mg ¥950 In-stock
    5 mg ¥1400 In-stock
    10 mg ¥2450 In-stock
    50 mg ¥6050 In-stock
    100 mg ¥8150 In-stock
    200 mg   询价  
    500 mg   询价  

    * Please select Quantity before adding items.

    GDC-0623 相关产品

    相关化合物库:

    • Clinical Compound Library Plus
    • Bioactive Compound Library Plus
    • Apoptosis Compound Library
    • Immunology/Inflammation Compound Library
    • Kinase Inhibitor Library
    • MAPK Compound Library
    • Anti-Cancer Compound Library
    • Clinical Compound Library
    • Reprogramming Compound Library
    • Oxygen Sensing Compound Library
    • Ferroptosis Compound Library
    • Anti-Pancreatic Cancer Compound Library
    • Angiogenesis Related Compound Library
    • Anti-Liver Cancer Compound Library
    • Anti-Colorectal Cancer Compound Library

    生物活性

    GDC-0623 (RG 7421) is a potent, ATP-uncompetitive inhibitor of MEK1 (Ki=0.13 nM, +ATP), and displays 6-fold weaker potency against HCT116 (KRAS (G13D), EC50=42 nM) versus A375 (BRAFV600E, EC50=7 nM).

    IC50 & Target

    MEK1

    0.13 nM (Ki, +ATP)

    体外研究
    (In Vitro)

    GDC-0623 (RG 7421) and G-573 are able to prevent MEK phosphorylation by CRAF in vitro, and able to block MEK phosphorylation by BRAF(V600E)[1]. GDC-0623 (RG 7421) is potent, ATP-uncompetitive inhibitors of MEK1 but shows distinct shifts in cellular activity compared with the other two inhibitors, only 6-fold half-maximum effective concentration (EC50) decreases[2].

    上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

    体内研究
    (In Vivo)

    GDC-0623 (RG 7421) (40 mg/kg, p.o.) shows percent tumour growth inhibition (%TGI) in MiaPaCa-2 xenograft model. GDC-0623 (RG 7421) and G-573 show superior antitumour activity compared to GDC-0623 (RG 7421) in all three KRAS models[1].

    上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

    Clinical Trial

    分子量

    456.21

    Formula

    C16H14FIN4O3

    CAS 号

    1168091-68-6

    运输条件

    Room temperature in continental US; may vary elsewhere.

    储存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    溶解性数据
    In Vitro: 

    DMSO : 50 mg/mL (109.60 mM; Need ultrasonic)

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 2.1920 mL 10.9599 mL 21.9197 mL
    5 mM 0.4384 mL 2.1920 mL 4.3839 mL
    10 mM 0.2192 mL 1.0960 mL 2.1920 mL

    *

    请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
    储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

    In Vivo:

    请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

    ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
    分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

    • 1.

      请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.5 mg/mL (5.48 mM); Clear solution

      此方案可获得 ≥ 2.5 mg/mL (5.48 mM,饱和度未知) 的澄清溶液。

      以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

      将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

    • 2.

      请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: ≥ 2.5 mg/mL (5.48 mM); Clear solution

      此方案可获得 ≥ 2.5 mg/mL (5.48 mM,饱和度未知) 的澄清溶液。

      以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

      将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
    *以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
    参考文献
    • [1]. Hatzivassiliou G, et al. Mechanism of MEK inhibition determines efficacy in mutant KRAS- versus BRAF-driven cancers. Nature. 2013 Sep 12;501(7466):232-6.

      [2]. Takahashi RH, et al. Elucidating the Mechanisms of Formation for Two Unusual Cytochrome P450-Mediated Fused Ring Metabolites of GDC-0623, a MAPK/ERK Kinase Inhibitor. Drug Metab Dispos. 2015 Dec;43(12):1929-1933.

    Cell Assay
    [1]

    Flag-MEK1 mutants, S212P and S212A, are generated using the QuickChange site directed mutagenesis kit. Mammalian expression vectors for N-terminal Flag tagged MEK-1 are expressed in HCT116 cells. 1.8×106 HCT116 cells are plated in 10 cm plate and transfected on the following day with 17 μg of expression constructs using lipofectamine 2000. After 48 hours cells are treated with inhibitors for the indicated times, harvested and lysed in 100 μL cell extraction buffer. Cell lysates from each sample are analyzed by SDS-PAGE. Membranes are incubated with phospho-MEK S221, phospho-ERK1/2 and MEK1 primary antibodies and immunoreactive proteins are analyzed by SuperSignal West Pico Chemiluminescent Substrate.

    上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [1]

    Colo205 xenografts are established by inoculating 5×106 cells resuspended in Hank’s Balanced Salt Solution (HBSS) subcutaneously (s.c.) in the rear right flank of 6-8 week old female nude (nu/nu) mice. NCI-H2122 xenografts are established by inoculating 1×107 cells resuspended in Hank’s Balanced Salt Solution (HBSS) plus matrigel (growth factor reduced) s.c. in the rear right flank of 6-8 week old female nu/nu mice. Both A375 and MiaPaca-2 xenografts are initiated by transplanting 1 mm3 tumor fragments from their respective passaged tumors s.c. into the flank of athymic nu/nu mice. When tumors reached appr 200 mm3, mice are randomized and treated with daily (QD) oral gavage (PO) with either vehicle [methylcellulose 0.1% tween 80 0.1% (MCT)], GDC-0973 (at 10 mg/kg), GDC-0623 (RG 7421) (40 mg/kg), or G-573 (100 mg/kg). All doses of MEK inhibitors represented maximal tolerated doses (MTDs), resulting in no more than 15-20% body weight loss. Tumor volumes are determined using digital calipers using the formula (L×W×W)/2. Tumor growth inhibition (%TGI) iscalculated as the percentage of the area under the fitted curve (AUC) for the respective dose group per day in relation to the vehicle. Animal weights are recorded twice per week and mice are removed from study if body weights dropped ≥20%. Partial responses (PRs) are defined as any tumor demonstrating a ≥ 50% decrease in tumor volume, whereas complete responses (CRs) are defined as any tumor demonstrating 100% reduction in tumor volume at any point during the study.

    上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

    参考文献
    • [1]. Hatzivassiliou G, et al. Mechanism of MEK inhibition determines efficacy in mutant KRAS- versus BRAF-driven cancers. Nature. 2013 Sep 12;501(7466):232-6.

      [2]. Takahashi RH, et al. Elucidating the Mechanisms of Formation for Two Unusual Cytochrome P450-Mediated Fused Ring Metabolites of GDC-0623, a MAPK/ERK Kinase Inhibitor. Drug Metab Dispos. 2015 Dec;43(12):1929-1933.

    所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

    RG-185T台式高速离心机

    【简单介绍】

    品牌 其他品牌 加工定制
    结构类型 台式 布局形式 其他

    RG-185T台式高速离心机,微机控制,直流无刷电机驱动,运行稳定、噪音低、转速精度高。广泛应用于临床医学、生物化学、基因工程、免疫学等领域。是各级医院、科研单位、高等院校用于离心分离的*仪器。

    【详细说明】

    RG-185T台式高速离心机

    产品特点

      台式高速离心机广泛应用于临床医学、生物化学、基因工程、免疫学等领域。是各级医院、科研单位、高等院校用于离心分离的*仪器。

    主要技术性能
    1、数字屏(液晶屏)显示,人性化界面,操作简单便捷。

    2、微机控制,直流无刷电机驱动,运行稳定、噪音低、转速精度高。

    3、触摸面板,可编程操作,主机运行参数可根据需求设置且自动存储。

    4、配备电子门锁,设有门盖自锁、超速等多种保护功能;故障自动报警功能,安全可靠。

    5、具有9个程序的升/降速率曲线,可根据需要设置升/降速时间。

    6、实时rpm/RCF之间读数换算与设定,方便快捷。

    主要技术参数

    型号

    RG-185T

    转速可达

    18500r/min

    相对离心力可达

    23797xg

    容量可达

    100mlx4

    转速精度

    ± 30r/min

    时间设置范围

    1min~99min

    整机噪音

    <65dB(A)

    电源

    AC220V  50Hz  10A

    外形尺寸(Lx宽xH)

    330mmx420mmx280mm

    外包装尺寸(Lx宽xH)

    430mmx520mmx390mm

    净重

    20kg

    RG-185T台式高速离心机

    型号

    产品名称

    转速

    相对离心力

    容量

    备注

    RG-185T

    台式高速离心机

    18500

    23797

    LCD液晶显示

    主机带1号转子

    1号转子

    角转子

    18500

    23797

    1.5ml/2.2ml×12

    二选一

    NO.2

    角转子

    13000

    11400

    5ml×10/12

    二选一

    NO.3

    角转子

    12000

    14800

    10ml×12

     

    角转子

    12000

    14800

    15ml×8

     

    NO.4

    角转子

    12000

    13000

    50ml×6

    适用圆底管

    角转子

    12000

    13000

    50ml×6

    适用尖底管

    角转子

    12000

    13000

    100ml×4

     

    NO.5

    水平转子

    6000

    3200

    10ml×4

     

    NO.6

    水平酶标转子

    3000

    1400

    2×48 孔

     

    NO.7

    角转子

    13200

    16110

    1.5ml/2.2ml×24

    二选一

    NO.8

    角转子

    16000

    23669

    0.5ml×36/48

    二选一

    RG2833(Synonyms: RGFP109)

    上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

    RG2833 (Synonyms: RGFP109) 纯度: 99.71%

    RG2833 是一种可透过血脑屏障的 HDAC 抑制剂,抑制 HDAC1 和 HDAC3 的活性,IC50 值分别为 60 nM 和 50 nM,Ki 值分别为 32 和 5 nM。

    RG2833(Synonyms: RGFP109)

    RG2833 Chemical Structure

    CAS No. : 1215493-56-3

    规格 价格 是否有货 数量
    Free Sample (0.1-0.5 mg)   Apply now  
    10 mM * 1 mL in DMSO ¥500 In-stock
    5 mg ¥395 In-stock
    10 mg ¥714 In-stock
    50 mg ¥1500 In-stock
    100 mg ¥2500 In-stock
    500 mg ¥9500 In-stock
    1 g   询价  
    5 g   询价  

    * Please select Quantity before adding items.

    RG2833 相关产品

    相关化合物库:

    • Bioactive Compound Library Plus
    • Cell Cycle/DNA Damage Compound Library
    • Epigenetics Compound Library
    • Histone Modification Research Compound Library
    • Anti-Cancer Compound Library
    • CNS-Penetrant Compound Library
    • Anti-Aging Compound Library
    • Reprogramming Compound Library
    • Oxygen Sensing Compound Library
    • Anti-Breast Cancer Compound Library
    • Anti-Pancreatic Cancer Compound Library
    • Anti-Blood Cancer Compound Library
    • Anti-Liver Cancer Compound Library

    生物活性

    RG2833 is a brain-penetrant HDAC inhibitor with IC50s of 60 nM and 50 nM for HDAC1 and HDAC3, respectively. The Ki values for HDAC1 and HDAC3 are 32 and 5 nM, respectively[1].

    IC50 & Target

    HDAC3

    50 nM (IC50)

    HDAC1

    60 nM (IC50)

    HDAC1

    32 nM (Ki)

    HDAC3

    5 nM (Ki)

    体外研究
    (In Vitro)

    The Ki values of RG2833 for HDAC1 and HDAC3 are 32 nM and 5 nM, respectively. RG2833 is highly active in the whole tested concentration range from 1 to 10 µM. Continuous incubation with RG2833 slows the increase in frataxin protein, and when the compound is removed, frataxin protein levels rapidly increased in the cells from patient P13[1]. RG2833 produces significant increases in brain aconitase enzyme activity, together with reduction of neuronal pathology of the dorsal root ganglia (DRG)[2].

    上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

    体内研究
    (In Vivo)

    RG2833 (150 mg/kg) is able to correct frataxin deficiency in the brain and heart of KIKI mice 24 hours after a single injection, but not when lower doses are used. When followed in time, the frataxin mRNA increase induced by RG2833 in the KIKI mouse can be first detected at 12 hours and reach a maximum at 24 hours in both brain and heart[1]. RG2833 (100 mg/kg, s.c.) is well tolerated in chronic dosing of mice without toxicity. RG2833 improves motor coordination of YG8R FRDA mice. RG2833 increases frataxin protein expression in the brain of YG8R FRDA mice[2]. RGFP109 (30 mg/kg, p.o. once daily for 6 days) has no acute effects on dyskinesia after single or 6 days once-daily treatment. One week following cessation of RGFP109, dyskinesia and duration of ON-time with disabling dyskinesia are reduced by 37% and 50%, respectively[3].

    上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

    分子量

    339.43

    Formula

    C20H25N3O2

    CAS 号

    1215493-56-3

    运输条件

    Room temperature in continental US; may vary elsewhere.

    储存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    溶解性数据
    In Vitro: 

    DMSO : ≥ 50 mg/mL (147.31 mM)

    * “≥” means soluble, but saturation unknown.

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 2.9461 mL 14.7306 mL 29.4612 mL
    5 mM 0.5892 mL 2.9461 mL 5.8922 mL
    10 mM 0.2946 mL 1.4731 mL 2.9461 mL

    *

    请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
    储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

    In Vivo:

    请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

    ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
    分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

    • 1.

      请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.5 mg/mL (7.37 mM); Clear solution

      此方案可获得 ≥ 2.5 mg/mL (7.37 mM,饱和度未知) 的澄清溶液。

      以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

      将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

    • 2.

      请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: ≥ 2.5 mg/mL (7.37 mM); Clear solution

      此方案可获得 ≥ 2.5 mg/mL (7.37 mM,饱和度未知) 的澄清溶液。

      以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

      将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
    • 3.

      请依序添加每种溶剂: 10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (7.37 mM); Clear solution

      此方案可获得 ≥ 2.5 mg/mL (7.37 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

      以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

    • 4.

      请依序添加每种溶剂: 5% DMSO    40% PEG300    5% Tween-80    50% saline

      Solubility: ≥ 2.5 mg/mL (7.37 mM); Clear solution

    *以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
    参考文献
    • [1]. Rai M, et al. Two new pimelic diphenylamide HDAC inhibitors induce sustained frataxin upregulation in cells from Friedreich’s ataxia patients and in a mouse model. PLoS One. 2010, 5(1), e8825.

      [2]. Sandi C, et al. Prolonged treatment with pimelic o-aminobenzamide HDAC inhibitors ameliorates the disease phenotype of a Friedreich ataxia mouse model. Neurobiol Dis. 2011, 42(3), 496-505.

      [3]. Johnston TH, et al. RGFP109, a histone deacetylase inhibitor attenuates L-DOPA-induced dyskinesia in the MPTP-lesioned marmoset: a proof-of-concept study. Parkinsonism Relat Disord. 2013, 19(2), 260-264.

    Kinase Assay
    [2]

    Aconitase activities are determined by homogenization of mouse brain tissues on ice at 10% w/v in CellLytic MT Mammalian Tissue Lysis/Extraction buffer, followed by centrifugation at 800×g for 10 min at 4°C. Tissue lysates (50 μL) are then added to 200 μL of substrate mix (50 mM Tris/HCl pH 7.4, 0.4 mM NADP, 5 mM Na citrate, 0.6 mM MgCl2, 0.1% (v/v) Triton X-100 and 1U isocitrate dehydrogenase) and the reactions are incubated at 37°C for 15 min, followed by spectrophotometric absorbance measurements every minute for 15 min at 340 nm 37°C to determine the reaction slope. Aconitase activities of mouse brain tissues are then normalized to citrate synthase activities, which are determined using a citrate synthase assay kit.

    上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [2]

    Mice are housed in conventional open cages with Litaspen Premium 8/20 bedding, paper wool nesting and standard fun tunnel environmental enrichment, with 13 h light, 11 h dark, 20-23°C and 45-60% humidity. The mice are given a diet of SDS RM3 Expanded food pellets and standard drinking water. Mice are given subcutaneous injections of 150 mg/kg RG2833 three times per week for 4.5 months, or 50 mg/kg 136 or 100 mg/kg RG2833 five times per week for 5 months, followed by culling for tissue collection 24 h after the final injection.

    上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

    参考文献
    • [1]. Rai M, et al. Two new pimelic diphenylamide HDAC inhibitors induce sustained frataxin upregulation in cells from Friedreich’s ataxia patients and in a mouse model. PLoS One. 2010, 5(1), e8825.

      [2]. Sandi C, et al. Prolonged treatment with pimelic o-aminobenzamide HDAC inhibitors ameliorates the disease phenotype of a Friedreich ataxia mouse model. Neurobiol Dis. 2011, 42(3), 496-505.

      [3]. Johnston TH, et al. RGFP109, a histone deacetylase inhibitor attenuates L-DOPA-induced dyskinesia in the MPTP-lesioned marmoset: a proof-of-concept study. Parkinsonism Relat Disord. 2013, 19(2), 260-264.

    所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

    Ginsenoside Rg2(Synonyms: 人参皂苷 Rg2; Chikusetsusaponin I; Panaxoside Rg2; Prosapogenin C2)

    上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

    Ginsenoside Rg2 (Synonyms: 人参皂苷 Rg2; Chikusetsusaponin I; Panaxoside Rg2; Prosapogenin C2) 纯度: ≥98.0%

    Ginsenoside Rg2 是人参的主要活性成分之一。Ginsenoside Rg2抑制脂多糖介导的 VCAM-1ICAM-1 表达的增加。 Ginsenoside Rg2 还降低 1-42 积聚。

    Ginsenoside Rg2(Synonyms: 人参皂苷 Rg2; Chikusetsusaponin I;  Panaxoside Rg2;  Prosapogenin C2)

    Ginsenoside Rg2 Chemical Structure

    CAS No. : 52286-74-5

    规格 价格 是否有货 数量
    10 mM * 1 mL in DMSO ¥1036 In-stock
    5 mg ¥700 In-stock
    10 mg ¥1200 In-stock
    50 mg   询价  
    100 mg   询价  

    * Please select Quantity before adding items.

    Ginsenoside Rg2 相关产品

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    生物活性

    Ginsenoside Rg2 is one of the major active components of ginseng. Ginsenoside Rg2 inhibits VCAM-1 and ICAM-1 expressions stimulated with lipopolysaccharide (LPS). Ginsenoside Rg2 also reduces 1-42 accumulation.

    IC50 & Target[1][2]

    NF-κB

     

    1-42

     

    体外研究
    (In Vitro)

    Ginsenoside Rg2 prevents the decrease of IκB expression stimulated with lipopolysaccharide (LPS). IκB dissociation from RelA-p50 complex is crucial for NF-κB activity. Ginsenoside Rg2, protopanaxatriol, inhibits vascular cell adhesion molecule 1 (VCAM-1) and intercellular adhesion molecule 1 (ICAM-1) expression stimulated with LPS from human umbilical vein endothelial cell (HUVEC). The inhibition of VCAM-1 and ICAM-1 expression by Ginsenoside Rg2 is in a concentration-dependent manner, significantly. Treatment of endothelial cells with LPS (1µg/mL) decreases IκBα expression. By 1 hr after LPS treatment, significant decrease of IκBα is attained. To determine whether LPS-stimulated IκBα expression is affected by Ginsenoside Rg2, endothelial cells are treated for 1 hr with Ginsenoside Rg2 (1~50 µM) prior to LPS (1 µg/mL) stimulation for 1 hr. Ginsenoside Rg2 reverses the decrease of LPS-induced IκBα expression in a concentration-dependent manner, significantly. The adhesion of THP-1 cells to endothelial cells is measured using quantitative monolayer adhesion assay. The adhesion of THP-1 cells onto endothelial cells are increased to five folds by LPS (1 µg/mL) stimulation for 8 hrs. Ginsenoside Rg2 (1~50 µM) inhibits the adhesion of THP-1 cells to endothelial cells stimulated with LPS, in a concentration-dependent manner[1].

    上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

    体内研究
    (In Vivo)

    G-Rg1 and Ginsenoside Rg2 (G-Rg2) reduce the escape latencies on the last two training days compared to the Alzheimer’s disease (AD) model group (p<0.05). In the spatial exploration test, the total time spent in the target quadrant and the number of mice that exactly crossed the previous position of the platform are clearly shorter and lower, respectively, in the AD model group mice than in the normal control group mice (p<0.01), a trend that is reversed by treatment with G-Rg1 and Ginsenoside Rg2 (G-Rg1, p<0.01; Ginsenoside Rg2, p<0.05). Treatment with G-Rg1 and Ginsenoside Rg2 effectively improve cognitive function of the mice that have declined due to AD. G-Rg1 and Ginsenoside Rg2 reduce Aβ1-42 accumulation in APP/PS1 mice. In the G-Rg1 and Ginsenoside Rg2 treated mice, the pathological abnormalities observed in the APP/PS1 mice are gradually ameliorated. Clear nucleoli and light brown, sparsely scattered Aβ deposits are visible[2].

    上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

    分子量

    785.01

    Formula

    C42H72O13

    CAS 号

    52286-74-5

    中文名称

    人参皂苷 Rg2;人参皂苷 Rg2

    运输条件

    Room temperature in continental US; may vary elsewhere.

    储存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    溶解性数据
    In Vitro: 

    DMSO : 100 mg/mL (127.39 mM; ultrasonic and warming and heat to 60°C)

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 1.2739 mL 6.3693 mL 12.7387 mL
    5 mM 0.2548 mL 1.2739 mL 2.5477 mL
    10 mM 0.1274 mL 0.6369 mL 1.2739 mL

    *

    请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
    储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

    In Vivo:

    请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

    ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
    分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

    • 1.

      请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.5 mg/mL (3.18 mM); Clear solution

      此方案可获得 ≥ 2.5 mg/mL (3.18 mM,饱和度未知) 的澄清溶液。

      以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

      将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

    • 2.

      请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: ≥ 2.5 mg/mL (3.18 mM); Clear solution

      此方案可获得 ≥ 2.5 mg/mL (3.18 mM,饱和度未知) 的澄清溶液。

      以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

      将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
    • 3.

      请依序添加每种溶剂: 10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (3.18 mM); Clear solution

      此方案可获得 ≥ 2.5 mg/mL (3.18 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

      以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

    *以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
    参考文献
    • [1]. Cho YS, et al. Ginsenoside rg2 inhibits lipopolysaccharide-induced adhesion molecule expression in human umbilical vein endothelial cell. Korean J Physiol Pharmacol. 2013 Apr;17(2):133-7.

      [2]. Li N, et al. A UPLC/MS-based metabolomics investigation of the protective effect of ginsenosides Rg1 and Rg2 in mice with Alzheimer’s disease. J Ginseng Res. 2016 Jan;40(1):9-17.

      [3]. Cho YS, et al. Ginsenoside rg2 inhibits lipopolysaccharide-induced adhesion molecule expression in human umbilical vein endothelial cell. Korean J Physiol Pharmacol. 2013;17(2):133-137.

    Cell Assay

    HUVECs ares grown in EBM-2 containing 10% FBS at a density of 2.0×105 cells/well on 24-well plates. Endothelial cells at 90~95% confluence are treated with Ginsenoside Rg2 (1, 20, 50 µM) for 1 hr prior to 1 µg/mL of LPS stimulation for 8 hr. THP-1 cells are labeled with Calcein-AM (5 µM) in RPMI 1640 medium containing 10% FBS for 30 min. After extensive washing with PBS, the labeled THP-1 cells are seeded at a density of 5.0×105 cells/well onto endothelial cells which are treated with the Rg2 and/or LPS and, then, incubated for 1 hr at 37°C while gentle shaking. After incubation, non-adherent cells are removed by gentle washing two times with PBS. Photograph images are obtained at 485 nm excitation and 538 nm emission using a SPOT II digital camera-attached fluorescence microscope[1].

    上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [2]

    Mice[2]
    Male APP/PS1 mice, weighing 20±2 g, and male C57BL/6J mice, weighing 20±2 g, are used. The animals are maintained in an air-conditioned animal center at 23±2°C and a relative humidity of 50±10%, with a natural light-dark cycle. Food and water are available ad libitum. After acclimatization for 1 wk, the mice are divided into four groups (n=10 in each group): the normal control group, the AD model group, the G-Rg1 group, and the Ginsenoside Rg2 group. According to the concentration-response curves, the mice in the G-Rg1 and Ginsenoside Rg2 groups are injected intraperitoneally once daily with G-Rg1 and Ginsenoside Rg2 (30 mg/kg), respectively, dissolved in saline. The mice in the AD model group (APP/PS1 mice) and the normal control group (C57BL/6J nontransgenic littermates) are treated with isodose saline (0.9% w/v). All mice are treated for 1 mo before brain metabolite profiling.

    上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

    参考文献
    • [1]. Cho YS, et al. Ginsenoside rg2 inhibits lipopolysaccharide-induced adhesion molecule expression in human umbilical vein endothelial cell. Korean J Physiol Pharmacol. 2013 Apr;17(2):133-7.

      [2]. Li N, et al. A UPLC/MS-based metabolomics investigation of the protective effect of ginsenosides Rg1 and Rg2 in mice with Alzheimer’s disease. J Ginseng Res. 2016 Jan;40(1):9-17.

      [3]. Cho YS, et al. Ginsenoside rg2 inhibits lipopolysaccharide-induced adhesion molecule expression in human umbilical vein endothelial cell. Korean J Physiol Pharmacol. 2013;17(2):133-137.

    所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

    Nevirapine(Synonyms: 奈韦拉平; BI-RG 587; NSC 641530; NVP)

    Nevirapine (Synonyms: 奈韦拉平; BI-RG 587; NSC 641530; NVP) 纯度: 99.01%

    Nevirapine (BI-RG 587) 是用于研究 HIV/AIDS 的 HIV-1 逆转录酶非核苷抑制剂,Ki 值为 270 μM。

    Nevirapine(Synonyms: 奈韦拉平; BI-RG 587;  NSC 641530;  NVP)

    Nevirapine Chemical Structure

    CAS No. : 129618-40-2

    规格 价格 是否有货 数量
    Free Sample (0.1-0.5 mg)   Apply now  
    10 mM * 1 mL in DMSO ¥572 In-stock
    10 mg ¥520 In-stock
    50 mg ¥1100 In-stock
    100 mg ¥1600 In-stock
    200 mg ¥2600 In-stock
    500 mg   询价  
    1 g   询价  

    * Please select Quantity before adding items.

    Nevirapine 相关产品

    相关化合物库:

    • Drug Repurposing Compound Library Plus
    • FDA-Approved Drug Library Plus
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    • Bioactive Compound Library Plus
    • Anti-Infection Compound Library
    • FDA-Approved Drug Library
    • Anti-Cancer Compound Library
    • Antiviral Compound Library
    • CNS-Penetrant Compound Library
    • Drug Repurposing Compound Library
    • Anti-COVID-19 Compound Library
    • NMPA-Approved Drug Library
    • Orally Active Compound Library
    • FDA Approved & Pharmacopeial Drug Library
    • Drug-Induced Liver Injury (DILI) Compound Library
    • Rare Diseases Drug Library
    • Children’s Drug Library

    生物活性

    Nevirapine is a non-nucleoside inhibitor of HIV-1 reverse transcriptase used to treat and prevent HIV/AIDS; with a Ki of 270 μM[1].

    IC50 & Target

    Ki: 270 μM (HIV-1 reverse transcriptase)[1]

    体外研究
    (In Vitro)

    Nevirapine itself is an inhibitor of only CYP3A4 at concentrations that are well above those of therapeutic relevance (Ki=270 μM)[1]. Nevirapine has been used as a re-differentiation agent to treat cancers in several human cancer models. At all doses (100, 200, 350, 500 μM) tested, nevirapine significantly inhibits cell proliferation after 48 h treatment. At high dose (500 μM), nevirapine significantly increases the percentage of apoptotic cells compared with control[2]. Nevirapine is a potent and selective inhibitor (IC50=10-100 nM) of the replication of a wide variety of HIV-1 strains in several cellular assays[3].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    体内研究
    (In Vivo)

    Nevirapine is available for use in combination with nucleoside HIV-1 reverse transcriptase inhibitors (e.g., zidovudine, didanosine, etc.). Nevirapine has received FDA approval for use in combination with HIV-1 protease inhibitors (e.g., saquinavir, ritonavir, indinavir, etc.). In humans, nevirapine is eliminated primarily in the urine as glucuronide conjugates of 2-, 3-, 8-, and 12-hydroxynevirapine[1]. Nevirapine is completely absorbed in both sexes of mouse, rat, rabbit, monkey, and chimpanzee. Nevirapine is extensively metabolized in both sexes of all animal species studied[4]. Nevirapine (9 mg/kg, 18 mg/kg and 36 mg/kg) shows significant reduction in ulcer severity score and ulcer index as compared to the control[5]

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Clinical Trial

    分子量

    266.30

    Formula

    C15H14N4O

    CAS 号

    129618-40-2

    中文名称

    奈韦拉平;萘维拉平;那韦拉平;奈韦那平;萘韦拉平

    运输条件

    Room temperature in continental US; may vary elsewhere.

    储存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    溶解性数据
    In Vitro: 

    DMSO : 14.29 mg/mL (53.66 mM; Need ultrasonic)

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 3.7552 mL 18.7758 mL 37.5516 mL
    5 mM 0.7510 mL 3.7552 mL 7.5103 mL
    10 mM 0.3755 mL 1.8776 mL 3.7552 mL

    *

    请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
    储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

    In Vivo:

    请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

    ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
    分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

    • 1.

      请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 1.43 mg/mL (5.37 mM); Clear solution

      此方案可获得 ≥ 1.43 mg/mL (5.37 mM,饱和度未知) 的澄清溶液。

      以 1 mL 工作液为例,取 100 μL 14.3 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

      将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

    • 2.

      请依序添加每种溶剂: 10% DMSO    90% corn oil

      Solubility: ≥ 1.43 mg/mL (5.37 mM); Clear solution

      此方案可获得 ≥ 1.43 mg/mL (5.37 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

      以 1 mL 工作液为例,取 100 μL 14.3 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

    *以上所有助溶剂都可在 MCE 网站选购。
    参考文献
    • [1]. Erickson DA, et al. Characterization of the in vitro biotransformation of the HIV-1 reverse transcriptase inhibitornevirapine by human hepatic cytochromes P-450. Drug Metab Dispos. 1999 Dec;27(12):1488-95.

      [2]. Dong JJ, et al. In vitro evaluation of the therapeutic potential of nevirapine in treatment of human thyroid anaplastic carcinoma. Mol Cell Endocrinol. 2013 May 6;370(1-2):113-8.

      [3]. Merluzzi VJ, et al. Inhibition of HIV-1 replication by a nonnucleoside reverse transcriptase inhibitor. Science. 1990 Dec 7;250(4986):1411-3.

      [4]. Riska PS, et al. Biotransformation of nevirapine, a non-nucleoside HIV-1 reverse transcriptase inhibitor, in mice, rats, rabbits, dogs, monkeys, and chimpanzees. Drug Metab Dispos. 1999 Dec;27(12):1434-47.

      [5]. Onasanwo SA, et al. Evaluation of anti-ulcerogenic and ulcer-healing activities of nevirapine in rats. Afr J Med Med Sci. 2015 Sep;44(3):251-9.

    Cell Assay
    [2]

    FRO cells are seeded into 96-well culture plates at 10,000 cells/well. Cells are treated with different doses of nevirapine (0, 100, 200, 350 and 500 μM) for 48 h. MTT dye (5 mg/mL) is added to each well for additional 4 h, and the reaction is then stopped by the addition of DMSO. Optical density is measured at 490 nm on a multi-well plate reader[2].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [4]

    Rats: Nevirapine and [14C] Nevirapine are dissolved together in absolute ethanol and methylene chloride (1:1, v/v) with mild heating. The concentration of drug in suspension is 2 mg/mL (20 mg/kg, 26 μCi) for oral dosing to rats and 6.7 mg/mL (20.3 mg/kg, 10 μCi males, 8.9 μCi females) for intraduodenal administration to rats before bile collection. The i.v. dose is administered to rats (1.1 mg/kg, 20 μCi) as a solution in 20% ethanol/80% saline[4].

    Mice: Nevirapine and [14C] Nevirapine are dissolved together in absolute ethanol and methylene chloride (1:1, v/v) with mild heating. The concentration of drug in suspension is 2 mg/mL (20 mg/kg, 2.5 μCi) with a specific activity of 5.55 μCi/mg for oral dosing to mice[4].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    参考文献
    • [1]. Erickson DA, et al. Characterization of the in vitro biotransformation of the HIV-1 reverse transcriptase inhibitornevirapine by human hepatic cytochromes P-450. Drug Metab Dispos. 1999 Dec;27(12):1488-95.

      [2]. Dong JJ, et al. In vitro evaluation of the therapeutic potential of nevirapine in treatment of human thyroid anaplastic carcinoma. Mol Cell Endocrinol. 2013 May 6;370(1-2):113-8.

      [3]. Merluzzi VJ, et al. Inhibition of HIV-1 replication by a nonnucleoside reverse transcriptase inhibitor. Science. 1990 Dec 7;250(4986):1411-3.

      [4]. Riska PS, et al. Biotransformation of nevirapine, a non-nucleoside HIV-1 reverse transcriptase inhibitor, in mice, rats, rabbits, dogs, monkeys, and chimpanzees. Drug Metab Dispos. 1999 Dec;27(12):1434-47.

      [5]. Onasanwo SA, et al. Evaluation of anti-ulcerogenic and ulcer-healing activities of nevirapine in rats. Afr J Med Med Sci. 2015 Sep;44(3):251-9.

    所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

    Nevirapine(Synonyms: 奈韦拉平; BI-RG 587; NSC 641530; NVP)

    Nevirapine (Synonyms: 奈韦拉平; BI-RG 587; NSC 641530; NVP) 纯度: 99.01%

    Nevirapine (BI-RG 587) 是用于研究 HIV/AIDS 的 HIV-1 逆转录酶非核苷抑制剂,Ki 值为 270 μM。

    Nevirapine(Synonyms: 奈韦拉平; BI-RG 587;  NSC 641530;  NVP)

    Nevirapine Chemical Structure

    CAS No. : 129618-40-2

    规格 价格 是否有货 数量
    Free Sample (0.1-0.5 mg)   Apply now  
    10 mM * 1 mL in DMSO ¥572 In-stock
    10 mg ¥520 In-stock
    50 mg ¥1100 In-stock
    100 mg ¥1600 In-stock
    200 mg ¥2600 In-stock
    500 mg   询价  
    1 g   询价  

    * Please select Quantity before adding items.

    Nevirapine 相关产品

    相关化合物库:

    • Drug Repurposing Compound Library Plus
    • FDA-Approved Drug Library Plus
    • FDA-Approved Drug Library Mini
    • Bioactive Compound Library Plus
    • Anti-Infection Compound Library
    • FDA-Approved Drug Library
    • Anti-Cancer Compound Library
    • Antiviral Compound Library
    • CNS-Penetrant Compound Library
    • Drug Repurposing Compound Library
    • Anti-COVID-19 Compound Library
    • NMPA-Approved Drug Library
    • Orally Active Compound Library
    • FDA Approved & Pharmacopeial Drug Library
    • Drug-Induced Liver Injury (DILI) Compound Library
    • Rare Diseases Drug Library
    • Children’s Drug Library

    生物活性

    Nevirapine is a non-nucleoside inhibitor of HIV-1 reverse transcriptase used to treat and prevent HIV/AIDS; with a Ki of 270 μM[1].

    IC50 & Target

    Ki: 270 μM (HIV-1 reverse transcriptase)[1]

    体外研究
    (In Vitro)

    Nevirapine itself is an inhibitor of only CYP3A4 at concentrations that are well above those of therapeutic relevance (Ki=270 μM)[1]. Nevirapine has been used as a re-differentiation agent to treat cancers in several human cancer models. At all doses (100, 200, 350, 500 μM) tested, nevirapine significantly inhibits cell proliferation after 48 h treatment. At high dose (500 μM), nevirapine significantly increases the percentage of apoptotic cells compared with control[2]. Nevirapine is a potent and selective inhibitor (IC50=10-100 nM) of the replication of a wide variety of HIV-1 strains in several cellular assays[3].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    体内研究
    (In Vivo)

    Nevirapine is available for use in combination with nucleoside HIV-1 reverse transcriptase inhibitors (e.g., zidovudine, didanosine, etc.). Nevirapine has received FDA approval for use in combination with HIV-1 protease inhibitors (e.g., saquinavir, ritonavir, indinavir, etc.). In humans, nevirapine is eliminated primarily in the urine as glucuronide conjugates of 2-, 3-, 8-, and 12-hydroxynevirapine[1]. Nevirapine is completely absorbed in both sexes of mouse, rat, rabbit, monkey, and chimpanzee. Nevirapine is extensively metabolized in both sexes of all animal species studied[4]. Nevirapine (9 mg/kg, 18 mg/kg and 36 mg/kg) shows significant reduction in ulcer severity score and ulcer index as compared to the control[5]

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Clinical Trial

    分子量

    266.30

    Formula

    C15H14N4O

    CAS 号

    129618-40-2

    中文名称

    奈韦拉平;萘维拉平;那韦拉平;奈韦那平;萘韦拉平

    运输条件

    Room temperature in continental US; may vary elsewhere.

    储存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    溶解性数据
    In Vitro: 

    DMSO : 14.29 mg/mL (53.66 mM; Need ultrasonic)

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 3.7552 mL 18.7758 mL 37.5516 mL
    5 mM 0.7510 mL 3.7552 mL 7.5103 mL
    10 mM 0.3755 mL 1.8776 mL 3.7552 mL

    *

    请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
    储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

    In Vivo:

    请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

    ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
    分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

    • 1.

      请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 1.43 mg/mL (5.37 mM); Clear solution

      此方案可获得 ≥ 1.43 mg/mL (5.37 mM,饱和度未知) 的澄清溶液。

      以 1 mL 工作液为例,取 100 μL 14.3 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

      将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

    • 2.

      请依序添加每种溶剂: 10% DMSO    90% corn oil

      Solubility: ≥ 1.43 mg/mL (5.37 mM); Clear solution

      此方案可获得 ≥ 1.43 mg/mL (5.37 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

      以 1 mL 工作液为例,取 100 μL 14.3 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

    *以上所有助溶剂都可在 MCE 网站选购。
    参考文献
    • [1]. Erickson DA, et al. Characterization of the in vitro biotransformation of the HIV-1 reverse transcriptase inhibitornevirapine by human hepatic cytochromes P-450. Drug Metab Dispos. 1999 Dec;27(12):1488-95.

      [2]. Dong JJ, et al. In vitro evaluation of the therapeutic potential of nevirapine in treatment of human thyroid anaplastic carcinoma. Mol Cell Endocrinol. 2013 May 6;370(1-2):113-8.

      [3]. Merluzzi VJ, et al. Inhibition of HIV-1 replication by a nonnucleoside reverse transcriptase inhibitor. Science. 1990 Dec 7;250(4986):1411-3.

      [4]. Riska PS, et al. Biotransformation of nevirapine, a non-nucleoside HIV-1 reverse transcriptase inhibitor, in mice, rats, rabbits, dogs, monkeys, and chimpanzees. Drug Metab Dispos. 1999 Dec;27(12):1434-47.

      [5]. Onasanwo SA, et al. Evaluation of anti-ulcerogenic and ulcer-healing activities of nevirapine in rats. Afr J Med Med Sci. 2015 Sep;44(3):251-9.

    Cell Assay
    [2]

    FRO cells are seeded into 96-well culture plates at 10,000 cells/well. Cells are treated with different doses of nevirapine (0, 100, 200, 350 and 500 μM) for 48 h. MTT dye (5 mg/mL) is added to each well for additional 4 h, and the reaction is then stopped by the addition of DMSO. Optical density is measured at 490 nm on a multi-well plate reader[2].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [4]

    Rats: Nevirapine and [14C] Nevirapine are dissolved together in absolute ethanol and methylene chloride (1:1, v/v) with mild heating. The concentration of drug in suspension is 2 mg/mL (20 mg/kg, 26 μCi) for oral dosing to rats and 6.7 mg/mL (20.3 mg/kg, 10 μCi males, 8.9 μCi females) for intraduodenal administration to rats before bile collection. The i.v. dose is administered to rats (1.1 mg/kg, 20 μCi) as a solution in 20% ethanol/80% saline[4].

    Mice: Nevirapine and [14C] Nevirapine are dissolved together in absolute ethanol and methylene chloride (1:1, v/v) with mild heating. The concentration of drug in suspension is 2 mg/mL (20 mg/kg, 2.5 μCi) with a specific activity of 5.55 μCi/mg for oral dosing to mice[4].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    参考文献
    • [1]. Erickson DA, et al. Characterization of the in vitro biotransformation of the HIV-1 reverse transcriptase inhibitornevirapine by human hepatic cytochromes P-450. Drug Metab Dispos. 1999 Dec;27(12):1488-95.

      [2]. Dong JJ, et al. In vitro evaluation of the therapeutic potential of nevirapine in treatment of human thyroid anaplastic carcinoma. Mol Cell Endocrinol. 2013 May 6;370(1-2):113-8.

      [3]. Merluzzi VJ, et al. Inhibition of HIV-1 replication by a nonnucleoside reverse transcriptase inhibitor. Science. 1990 Dec 7;250(4986):1411-3.

      [4]. Riska PS, et al. Biotransformation of nevirapine, a non-nucleoside HIV-1 reverse transcriptase inhibitor, in mice, rats, rabbits, dogs, monkeys, and chimpanzees. Drug Metab Dispos. 1999 Dec;27(12):1434-47.

      [5]. Onasanwo SA, et al. Evaluation of anti-ulcerogenic and ulcer-healing activities of nevirapine in rats. Afr J Med Med Sci. 2015 Sep;44(3):251-9.

    所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

    RG14620(Synonyms: Tyrphostin RG14620)

    上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

    RG14620 (Synonyms: Tyrphostin RG14620) 纯度: 99.85%

    RG14620是 EGFR 抑制剂;IC50 值为3 μM。

    RG14620(Synonyms: Tyrphostin RG14620)

    RG14620 Chemical Structure

    CAS No. : 136831-49-7

    规格 价格 是否有货 数量
    10 mM * 1 mL in DMSO ¥605 In-stock
    5 mg ¥550 In-stock
    10 mg ¥800 In-stock
    50 mg ¥3000 In-stock
    100 mg ¥5000 In-stock
    200 mg   询价  
    500 mg   询价  

    * Please select Quantity before adding items.

    RG14620 相关产品

    相关化合物库:

    • Covalent Screening Library Plus
    • Bioactive Compound Library Plus
    • Immunology/Inflammation Compound Library
    • JAK/STAT Compound Library
    • Kinase Inhibitor Library
    • Protein Tyrosine Kinase Compound Library
    • Anti-Cancer Compound Library
    • Covalent Screening Library
    • Differentiation Inducing Compound Library
    • Anti-Hepatitis C Virus Compound Library
    • Anti-Lung Cancer Compound Library
    • Anti-Pancreatic Cancer Compound Library
    • Angiogenesis Related Compound Library
    • Anti-Liver Cancer Compound Library
    • Anti-Colorectal Cancer Compound Library

    生物活性

    RG14620 is an EGFR inhibitor with an IC50 of 3 μM.

    IC50 & Target

    EGFR

    3 μM (IC50, Cell Assay)

    体外研究
    (In Vitro)

    RG14620 inhibits colony formation (IC50=3 μM) and DNA synthesis (IC50=1 μM) by HER 14 cells, which are stimulated by 50 ng/mL EGF, in a dose-dependent manner. RG14620 also suppresses colony formation(IC50=4 μM) and DNA synthesis (IC50=1.25 μM) by EGF-stimulated MH-85 cells in a dose-dependent manner. The growth-inhibitory effect of RG14620 irreversible[2].

    上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

    体内研究
    (In Vivo)

    RG14620, at a dose of 200 g/mouse/day inhibits H-85 tumor growth in nude mice. Mice show less cachexia and hypercalcemia, eat more food, and are more active than untreated MH-85 tumor-bearing animals[2].

    上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

    分子量

    275.13

    Formula

    C14H8Cl2N2

    CAS 号

    136831-49-7

    运输条件

    Room temperature in continental US; may vary elsewhere.

    储存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    溶解性数据
    In Vitro: 

    DMSO : 33.33 mg/mL (121.14 mM; Need ultrasonic)

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 3.6346 mL 18.1732 mL 36.3465 mL
    5 mM 0.7269 mL 3.6346 mL 7.2693 mL
    10 mM 0.3635 mL 1.8173 mL 3.6346 mL

    *

    请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
    储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

    In Vivo:

    请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

    ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
    分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

    • 1.

      请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: 2.5 mg/mL (9.09 mM); Suspended solution; Need ultrasonic

      此方案可获得 2.5 mg/mL (9.09 mM) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。

      以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

      将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

    • 2.

      请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: 2.5 mg/mL (9.09 mM); Suspended solution; Need ultrasonic

      此方案可获得 2.5 mg/mL (9.09 mM) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。

      以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

      将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
    • 3.

      请依序添加每种溶剂: 10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (9.09 mM); Clear solution

      此方案可获得 ≥ 2.5 mg/mL (9.09 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

      以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

    *以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
    参考文献
    • [1]. Sagara Y, et al. Tyrphostins protect neuronal cells from oxidative stress. J Biol Chem. 2002 Sep 27;277(39):36204-15.

      [2]. Yoneda T, et al. The antiproliferative effects of tyrosine kinase inhibitors tyrphostins on a human squamous cell carcinoma in vitro and in nude mice. Cancer Res. 1991 Aug 15;51(16):4430-5.

    Cell Assay
    [2]

    MH-85 cells and HER 14 cells are plated in complete medium, either αMEM or DMEM, respectively, supplemented with 10% FCS. After overnight culture, the culture medium is switched to αMEM supplemented with 0.2% PCS and 50 ng/mL EGF (MH-85) or DMEM supplemented with 0.5% PCS and 50 ng/mL EGF (HER14). The cells are cultured in this medium in the presence or absence of increasing concentrations of RG-13022 or RG-14620 for 10 days. At the end of culture, the cells are fixed with 4% (v/v) formaldehyde in calcium-magnesium-free phosphate-buffered saline for 15 min at room temperature and stained with hematoxylin. Numbers of colonies including more than 20 cells in each well are counted under the microscope[2].

    上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [1]

    Mice: RG14620 in 0.1 mL 100% DMSO is injected i.p. twice a day from 1day after MH-85 tumor inoculation. Control animals are given the same vehicle[1].

    上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

    参考文献
    • [1]. Sagara Y, et al. Tyrphostins protect neuronal cells from oxidative stress. J Biol Chem. 2002 Sep 27;277(39):36204-15.

      [2]. Yoneda T, et al. The antiproliferative effects of tyrosine kinase inhibitors tyrphostins on a human squamous cell carcinoma in vitro and in nude mice. Cancer Res. 1991 Aug 15;51(16):4430-5.

    所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务