Anamorelin Fumarate(Synonyms: 富马酸阿拉莫林; ONO-7643 Fumarate; RC1291 Fumarate)

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。

Anamorelin Fumarate (Synonyms: 富马酸阿拉莫林; ONO-7643 Fumarate; RC1291 Fumarate)

Anamorelin(RC1291; ONO-7643)延胡索酸盐是口服活性的饥饿素受体激动剂。

Anamorelin Fumarate(Synonyms: 富马酸阿拉莫林; ONO-7643 Fumarate;  RC1291 Fumarate)

Anamorelin Fumarate Chemical Structure

CAS No. : 339539-92-3

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Anamorelin Fumarate 的其他形式现货产品:

Anamorelin Anamorelin hydrochloride

生物活性

Anamorelin Fumarate is a novel ghrelin receptor agonist with EC50 value of 0.74 nM in the FLIPR assay.

IC50 & Target

Ki: 0.7 nM (ghrelin receptor)[1]
EC50: 0.74 nM (ghrelin receptor)[1]

体外研究
(In Vitro)

In the FLIPR assay, Anamorelin (ANAM) shows significant agonist activity on the ghrelin receptor, with EC50 value of 0.74 nM. No significant antagonist activity is observed with Anamorelin at concentrations of up to 1,000 nM. In the binding experiments, Anamorelin binds to the ghrelin receptor with a binding affinity constant (Ki) of 0.70 nM. In the competition assay with radiolabeled ibutamoren (35S-MK-677; another ghrelin receptor agonist) Anamorelin (ANAM) is also found to bind with high affinity to the ghrelin receptor (IC50=0.69 nM). In rat pituitary cells incubated with Anamorelin, there is a dose-dependent stimulatory effect on GH release and the potency (EC50) is 1.5 nM. Anamorelin is screened for activity against a set of over 100 receptors, ion channels, transporters, and enzymes. Anamorelin demonstrates binding to the tachykinin neurokinin 2 (NK2) site (IC50=0.021 μM); however, a subsequent NK2 functional assay demonstrates no functional activity[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)

In rats, Anamorelin (ANAM) at an oral dose of 3, 10, or 30 mg/kg once daily significantly increases both food intake and body weight from Day 2 to Day 7 of treatment compared with the vehicle control. The cumulative change in food intake and weight gain increases dose-dependently, and these changes are significant at all dose levels (P<0.05) compared to the control. Administration of Anamorelin at a single oral dose of 3, 10, or 30 mg/kg induces a dose-dependent increase in plasma GH levels and GH AUC0-6h in rats[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

662.78

Formula

C35H46N6O7

CAS 号

339539-92-3

中文名称

富马酸阿拉莫林

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]. Pietra C, et al. Anamorelin HCl (ONO-7643), a novel ghrelin receptor agonist, for the treatment of cancer anorexia-cachexiasyndrome: preclinical profile. J Cachexia Sarcopenia Muscle. 2014 Dec;5(4):329-37.

Kinase Assay
[1]

For the competition assay, Anamorelin (ANAM) concentrations (1 pM-10 μM) are added to the membranes together with 35S-MK-677. Nonspecific binding is determined by adding 10 μM nonlabeled MK-677. The mixture is incubated at 30°C for 60 min, followed by application of the samples to GF/B filters, which has been pretreated with 0.5 % PEI for 60 min. The filters are subsequently washed in 0.9 % NaCl and counted using an OptiPhase counter[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
[1]

Rats[1]
For the assessment of food intake and body weight, rats are divided into four groups: Anamorelin 3 mg/kg (n=7), 10 mg/kg (n=7), or 30 mg/kg (n=7), or vehicle control (n=8), and 100 μL blood samples are collected before and 0.25, 0.5, 1, 2, 3, 4, 5, and 6 h after single dosing. Rats are anesthetized with sodium pentobarbital 64.8 mg/kg. A catheter filled with heparinized saline solution is inserted in the left femoral artery for blood collection and fitted with an extension tube, 1 mL sampling syringe, and a three-way cock to allow excess blood to return. Plasma levels of GH are measured immunochemically using a Rat Growth Hormone EIA kit and microplate reader. Measurements are performed in duplicate. Area under the GH concentration curve from 0 to 6 h (AUC0-6h) postdose and the time course of GH plasma concentrations are evaluated.
Pig[1]
In pigs (n=6 per group), Anamorelin is dosed directly into the gastric lumen via the dosing catheter. Blood samples are collected for the stimulation profile of GH at 30 and 15 min before, and 0, 5, 15, 30, 45, 60, and 120 min following dosing. Animals received either a single dose (3.5 mg/kg), or once-daily administration (1 mg/kg) for 7 days and stimulation profiles are taken after the first and seventh dose of Anamorelin. To assess IGF-1 levels, pigs receive either placebo or Anamorelin for 7 days (1 mg/kg/day), and the following 7 days the two treatments are crossed over. A single blood sample is taken once a day immediately before 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]. Pietra C, et al. Anamorelin HCl (ONO-7643), a novel ghrelin receptor agonist, for the treatment of cancer anorexia-cachexiasyndrome: preclinical profile. J Cachexia Sarcopenia Muscle. 2014 Dec;5(4):329-37.

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Dimethyl fumarate(Synonyms: 富马酸二甲酯)

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。

Dimethyl fumarate (Synonyms: 富马酸二甲酯) 纯度: 99.88%

Dimethyl fumarate (DMF) 是一种具有口服活性且可透过血脑屏障的 Nrf2 激活剂,可诱导抗氧化剂基因表达上调。Dimethyl fumarate 通过 GSH 耗竭/ROS 升高/MAPKs 激活途径诱导结肠癌细胞坏死,并诱导细胞自噬 (autophagy)。Dimethyl fumarate 可用于多发性硬化症的研究。

Dimethyl fumarate(Synonyms: 富马酸二甲酯)

Dimethyl fumarate Chemical Structure

CAS No. : 624-49-7

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Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ¥550 In-stock
500 mg ¥400 In-stock
5 g ¥550 In-stock
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生物活性

Dimethyl fumarate (DMF) is an orally active and brain-penetrant Nrf2 activator and induces upregulation of antioxidant gene expression. Dimethyl fumarate induces necroptosis in colon cancer cells through GSH depletion/ROS increase/MAPKs activation pathway, and also induces cell autophagy. Dimethyl fumarate can be used for multiple sclerosis research[1][2].

IC50 & Target

Human Endogenous Metabolite

 

体外研究
(In Vitro)

Dimethyl fumarate (DMF; 20-200 μM; 24 hours) treatment dose-dependently reduces the viability of SGC-7901, HT29, HCT116 and CT26 cancer cells[1].
Dimethyl fumarate (DMF; 100 μM; 3-24 hours) significantly activates JNK, p38 and ERK in CT26 cells[1].
Dimethyl fumarate induces necroptosis in colon cancer cells and the mechanism involves GSH depletion, an increase in ROS and activation of MAPKs-mediated signalling[1].
Dimethyl fumarate inhibits dendritic cell (DC) maturation by reducing inflammatory cytokine production (IL-12 and IL-6) and the expression of MHC class II, CD80, and CD86. Dimethyl fumarate impairs NF-κB signaling via reduced p65 nuclear translocalization and phosphorylation. Dimethyl fumarate inhibits maturation of DCs and subsequently Th1 and Th17 cell differentiation by suppression of both NF-κB and ERK1/2-MSK1 signaling[2].
Dimethyl fumarate (DMF), an immune modulator and inducer of the antioxidant response, suppresses HIV replication and neurotoxin release[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.

Cell Viability Assay[1]

Cell Line: SGC-7901, HT29, HCT116 and CT26 cells
Concentration: 20 μM, 50 μM, 100 μM, 200 μM
Incubation Time: 24 hours
Result: Reduced cell viability in SGC-7901, HT29, HCT116 and CT26 cancer cells.

Western Blot Analysis[1]

Cell Line: CT26 cancer cells
Concentration: 100 μM
Incubation Time: 3 hours, 6 hours, 12 hours, 24 hours
Result: Significantly activated JNK, p38 and ERK in CT26 cells after treatment from 3 to 24 h.

体内研究
(In Vivo)

Dimethyl fumarate (DMF; 50 mg/kg; oral gavage; daily; for 7 days) treatment is shown to upregulate the mRNA and protein levels of Nrf2 and Nrf2-regulated cytoprotective genes, attenuate 6-OHDA induced striatal oxidative stress and inflammation in C57BL/6 mice[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.

Animal Model: Male C57BL/6 mice (8-week-old)[4]
Dosage: 50 mg/kg
Administration: Oral gavage; daily; for 7 days
Result: Was shown to upregulate mRNA and protein levels of Nrf2 and Nrf2-regulated cytoprotective genes.

Clinical Trial

分子量

144.13

Formula

C6H8O4

CAS 号

624-49-7

中文名称

富马酸二甲酯

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 : 62.5 mg/mL (433.64 mM; Need ultrasonic)

H2O : 8.33 mg/mL (57.80 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 6.9382 mL 34.6909 mL 69.3818 mL
5 mM 1.3876 mL 6.9382 mL 13.8764 mL
10 mM 0.6938 mL 3.4691 mL 6.9382 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: 50% PEG300    50% saline

    Solubility: 7.5 mg/mL (52.04 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 (14.43 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (14.43 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% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (14.43 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (14.43 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
  • 4.

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

    Solubility: ≥ 2.08 mg/mL (14.43 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (14.43 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]. Xin Xie, et al. Dimethyl fumarate induces necroptosis in colon cancer cells through GSH depletion/ROS increase/MAPKs activation pathway. Br J Pharmacol. 2015 Aug;172(15):3929-43.

    [2]. Peng H, et al. Dimethyl fumarate inhibits dendritic cell maturation via nuclear factor κB (NF-κB) and extracellular signal-regulated kinase 1 and 2 (ERK1/2) and mitogen stress-activated kinase 1 (MSK1) signaling. J Biol Chem. 2012 Aug 10;287(33):28017-26.

    [3]. Cross SA, et al. Dimethyl fumarate, an immune modulator and inducer of the antioxidant response, suppresses HIV replication and macrophage-mediated neurotoxicity: a novel candidate for HIV neuroprotection. J Immunol. 2011 Nov 15;187(10):5015-25.

    [4]. Jing X, et al. Dimethyl fumarate attenuates 6-OHDA-induced neurotoxicity in SH-SY5Y cells and in animal model of Parkinson’s disease by enhancing Nrf2 activity. Neuroscience. 2015 Feb 12;286:131-40

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Fumarate hydratase-IN-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。

Fumarate hydratase-IN-1  纯度: 99.93%

Fumarate hydratase-IN-1 (compound 2) 是一种细胞可渗透性的富马酸水合酶 (fumarate hydratase) 抑制剂。Fumarate hydratase-IN-1 对几种细胞系具有抗增殖活性,平均 IC50 为 2.2 μM。

Fumarate hydratase-IN-1

Fumarate hydratase-IN-1 Chemical Structure

CAS No. : 1644060-37-6

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥2161 In-stock
2 mg ¥1400 In-stock
5 mg ¥2200 In-stock
10 mg ¥3200 In-stock
50 mg ¥9800 In-stock
100 mg ¥16500 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

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生物活性

Fumarate hydratase-IN-1 (compound 2) is a cell-permeable fumarate hydratase inhibitor. Fumarate hydratase-IN-1 has antiproliferative activity against several cancer cell lines with a mean IC50 of 2.2 μM[1].

IC50 & Target

Fumarate hydratase[1]

体外研究
(In Vitro)

Fumarate hydratase-IN-1 inhibits SW620, ACHN, HCT-116, PC3, and SK-MEL-28 cell lines with a mean IC50 of 2.2 μM[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.

分子量

446.54

Formula

C27H30N2O4

CAS 号

1644060-37-6

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 (111.97 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.2394 mL 11.1972 mL 22.3944 mL
5 mM 0.4479 mL 2.2394 mL 4.4789 mL
10 mM 0.2239 mL 1.1197 mL 2.2394 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 (5.60 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.60 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 (5.60 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.60 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 (5.60 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.60 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]. Takeuchi T et al. Identification of Fumarate Hydratase Inhibitors with Nutrient-Dependent Cytotoxicity. J Am Chem Soc, 2015 Jan 21, 137(2): 564-567.

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Dofequidar fumarate(Synonyms: MS-209)

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。

Dofequidar fumarate (Synonyms: MS-209) 纯度: 98.40%

Dofequidar 延胡索酸盐(MS-209 延胡索酸盐)是口服活性的喹啉化合物,能抑制 ABCB1/P-gp,ABCC1/MDR-相关蛋白1。

Dofequidar fumarate(Synonyms: MS-209)

Dofequidar fumarate Chemical Structure

CAS No. : 153653-30-6

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 ¥1289 In-stock
5 mg ¥980 In-stock
10 mg ¥1560 In-stock
50 mg ¥5115 In-stock
100 mg ¥7905 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

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  • Orally Active Compound Library

生物活性

Dofequidar fumarate(MS-209 fumarate), an orally active quinoline compound, has been reported to overcome MDR by inhibiting ABCB1/P-gp, ABCC1/MDR-associated protein 1, or both. IC50 value: Target: P-gp in vitro: MS-209 at 3 microM effectively overcame docetaxel resistance in MDR cancer cells, and this concentration was achieved in blood plasma for > 7 h without serious toxicity [1]. MS-209 restored chemosensitivity of SBC-3 / ADM cells to VP-16, ADM, and VCR in a dose-dependent manner in vitro [2]. dofequidar inhibits the efflux of chemotherapeutic drugs and increases the sensitivity to anticancer drugs in CSC-like side population (SP) cells isolated from various cancer cell lines. Dofequidar treatment greatly reduced the cell number in the SP fraction [3]. In 4-1St cells, which are extremely resistant to ADM and VCR, MS-209 at a concentration of 3 microM enhanced the cytotoxicity of ADM and VCR, 88- and 350-fold, respectively [4]. in vivo: Treatment with docetaxel alone at the maximal tolerated dose (MTD) showed an apparent antitumor activity to an intrinsically resistant HCT-15 tumor xenograft, and MS-209 additionally potentiated the antitumor activity of docetaxel. Against a MCF-7/ADM tumor xenograft expressing larger amounts of P-gp, docetaxel alone at the MTD showed no antitumor activity, whereas the MTD of docetaxel combined with MS-209 greatly reduced MCF-7/ADM tumor growth [1]. Intravenous injection with SBC-3 or SBC-3 / ADM cells produced metastatic colonies in the liver, kidneys and lymph nodes in natural killer (NK) cell-depleted severe combined immunodeficiency (SCID) mice, though SBC-3 / ADM cells more rapidly produced metastases than did SBC-3 cells. Treatment with VP-16 and ADM reduced metastasis formation by SBC-3 cells, whereas the same treatment did not affect metastasis by SBC-3 / ADM cells. Although MS-209 alone had no effect on metastasis by SBC-3 or SBC-3 / ADM cells, combined use of MS-209 with VP-16 or ADM resulted in marked inhibition of metastasis formation by SBC-3 / ADM cells to multiple organs [2].

Clinical Trial

分子量

597.66

Formula

C34H35N3O7

CAS 号

153653-30-6

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
In Vitro: 

DMSO : 100 mg/mL (167.32 mM; Need ultrasonic)

H2O : 1 mg/mL (1.67 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.6732 mL 8.3660 mL 16.7319 mL
5 mM 0.3346 mL 1.6732 mL 3.3464 mL
10 mM 0.1673 mL 0.8366 mL 1.6732 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 (sealed storage, away from moisture)。-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 (4.18 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.18 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 (4.18 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.18 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 (4.18 mM); Suspended solution

    此方案可获得 ≥ 2.5 mg/mL (4.18 mM,饱和度未知) 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]. Nakanishi O, et al. Potentiation of the antitumor activity by a novel quinoline compound, MS-209, in multidrug-resistant solid tumor cell lines. Oncol Res. 1997;9(2):61-9.

    [2]. Naito M, et al. MS-209, a quinoline-type reversal agent, potentiates antitumor efficacy of docetaxel in multidrug-resistant solid tumor xenograft models. Clin Cancer Res. 2002 Feb;8(2):582-8.

    [3]. Nokihara H, et al. A new quinoline derivative MS-209 reverses multidrug resistance and inhibits multiorgan metastases by P-glycoprotein-expressing human small cell lung cancer cells. Jpn J Cancer Res. 2001 Jul;92(7):785-92.

    [4]. Katayama R, et al. Dofequidar fumarate sensitizes cancer stem-like side population cells to chemotherapeutic drugs by inhibiting ABCG2/BCRP-mediated drug export. Cancer Sci. 2009 Nov;100(11):2060-8.

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Tiamulin fumarate(Synonyms: 延胡索酸泰妙菌素; Thiamutilin fumarate)

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。

Tiamulin fumarate (Synonyms: 延胡索酸泰妙菌素; Thiamutilin fumarate) 纯度: ≥98.0%

Tiamulin fumarate (Thiamutilin fumarate) 是一类二萜,广泛用于控制猪的传染疾病,包括猪痢疾和地方性肺炎等。

Tiamulin fumarate(Synonyms: 延胡索酸泰妙菌素; Thiamutilin fumarate)

Tiamulin fumarate Chemical Structure

CAS No. : 55297-96-6

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 ¥550 In-stock
250 mg ¥500 In-stock
1 g ¥1000 In-stock
5 g   询价  
10 g   询价  

* Please select Quantity before adding items.

Tiamulin fumarate 相关产品

相关化合物库:

  • Bioactive Compound Library Plus
  • Anti-Infection Compound Library
  • Anti-Cancer Compound Library
  • Antibacterial Compound Library
  • FDA Approved & Pharmacopeial Drug Library
  • Antibiotics Library

生物活性

Tiamulin fumarate (Thiamutilin fumarate) is a diterpenic compound that widely used in swine for the control of infectious diseases, including swine dysentery and enzootic pneumonia.

分子量

609.81

Formula

C32H51NO8S

CAS 号

55297-96-6

中文名称

延胡索酸泰妙菌素

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
In Vitro: 

DMSO : ≥ 100 mg/mL (163.99 mM)

H2O : 100 mg/mL (163.99 mM; Need ultrasonic)

* “≥” 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 1.6399 mL 8.1993 mL 16.3986 mL
5 mM 0.3280 mL 1.6399 mL 3.2797 mL
10 mM 0.1640 mL 0.8199 mL 1.6399 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 (sealed storage, away from moisture)。-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 (4.10 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.10 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 (4.10 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.10 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 (4.10 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.10 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]. Noa M, et al. Tiamulin-nitrovin interaction in pigs: a case report and experimental reproduction. Vet Hum Toxicol. 2000 Oct;42(5):286-8.

    [2]. Dreyfuss J, et al. Metabolism of tritium- and carbon-14-labeled tiamulin in dogs, rats, and pigs. J Antibiot (Tokyo). 1979 May;32(5):496-503.

    [3]. Islam KM, et al. The activity and compatibility of the antibiotic tiamulin with other drugs in poultry medicine–A review. Poult Sci. 2009 Nov;88(11):2353-9.

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

Fumarate hydratase-IN-2 sodium salt

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。

Fumarate hydratase-IN-2 sodium salt  纯度: 98.02%

Fumarate hydratase-IN-2 sodium salt (compound 3) 是一种细胞可渗透性的,竞争性的富马酸水合酶 (fumarate hydratase) 抑制剂 (Ki=4.5 μM),具有营养依赖性细胞毒性。

Fumarate hydratase-IN-2 sodium salt

Fumarate hydratase-IN-2 sodium salt Chemical Structure

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥3392 In-stock
1 mg ¥1500 In-stock
5 mg ¥3500 In-stock
10 mg ¥5000 In-stock
25 mg ¥10000 In-stock
50 mg ¥16000 In-stock
100 mg   询价  
200 mg   询价  

* Please select Quantity before adding items.

Fumarate hydratase-IN-2 sodium salt 相关产品

相关化合物库:

  • Bioactive Compound Library Plus

生物活性

Fumarate hydratase-IN-2 sodium salt (compound 3) is a cell-permeable and competitive fumarate hydratase inhibitor (Ki=4.5 μM) with nutrient-dependent cytotoxicity [1].

IC50 & Target

Ki: 4.5 μM (Fumarate hydratase)[1]

分子量

440.47

Formula

C25H25N2NaO4

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
In Vitro: 

H2O : 25 mg/mL (56.76 mM; Need ultrasonic)

DMSO : 10.66 mg/mL (24.20 mM; Need ultrasonic and warming)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.2703 mL 11.3515 mL 22.7030 mL
5 mM 0.4541 mL 2.2703 mL 4.5406 mL
10 mM 0.2270 mL 1.1352 mL 2.2703 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 (sealed storage, away from moisture)。-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。

参考文献
  • [1]. Takeuchi T et al. Identification of fumarate hydratase inhibitors with nutrient-dependent cytotoxicity. J Am Chem Soc. 2015 Jan 21;137(2):564-7.

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

VUF11207 fumarate

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。

VUF11207 fumarate  纯度: 98.92%

VUF11207 fumarate (Compound 29) 是一种 CXCR7 激动剂和高效 CXCR7 (pKi 为 8.1) 配体,可诱导 CXCR7β-arrestin2 募集 (pEC50 为 8.8) 和随后的内在化 (pEC50 为 7.9)。

VUF11207 fumarate

VUF11207 fumarate Chemical Structure

CAS No. : 1785665-61-3

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥1290 In-stock
5 mg ¥1000 In-stock
10 mg ¥1700 In-stock
25 mg ¥3500 In-stock
50 mg ¥6000 In-stock
100 mg ¥10000 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

VUF11207 fumarate 相关产品

相关化合物库:

  • Bioactive Compound Library Plus
  • GPCR/G Protein Compound Library
  • Immunology/Inflammation Compound Library
  • Anti-Cancer Compound Library
  • Small Molecule Immuno-Oncology Compound Library
  • Targeted Diversity Library

生物活性

VUF11207 fumarate (Compound 29) is a CXCR7 agonist and a high-potency CXCR7 (pKi of 8.1) ligand that induces recruitment of β-arrestin2 (pEC50 of 8.8) and subsequent internalization (pEC50 of 7.9) of CXCR7[1].

IC50 & Target[1]

CXCR7

8.1 (pKi)

分子量

586.65

Formula

C31H39FN2O8

CAS 号

1785665-61-3

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
In Vitro: 

DMSO : 100 mg/mL (170.46 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.7046 mL 8.5230 mL 17.0459 mL
5 mM 0.3409 mL 1.7046 mL 3.4092 mL
10 mM 0.1705 mL 0.8523 mL 1.7046 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 (sealed storage, away from moisture)。-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 (3.55 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (3.55 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 (3.55 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (3.55 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 (3.55 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (3.55 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]. Wijtmans M, et al. Synthesis, modeling and functional activity of substituted styrene-amides as small-molecule CXCR7 agonists. Eur J Med Chem. 2012 May;51:184-92.

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

Aliskiren fumarate(Synonyms: CGP 60536 fumarate; CGP60536B fumarate; SPP 100 fumarate)

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。

Aliskiren fumarate (Synonyms: CGP 60536 fumarate; CGP60536B fumarate; SPP 100 fumarate)

Aliskiren fumarate 是一种口服有效的、选择性的肾素 (renin) 抑制剂,其 IC50 为 1.5 nM。Aliskiren fumarate 可用于高血压、心血管疾病和癌症恶病质的研究。

Aliskiren fumarate(Synonyms: CGP 60536 fumarate; CGP60536B fumarate; SPP 100 fumarate)

Aliskiren fumarate Chemical Structure

CAS No. : 1196835-68-3

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

* Please select Quantity before adding items.

Aliskiren fumarate 的其他形式现货产品:

Aliskiren

生物活性

Aliskiren fumarate is an orally active, highly potent and selective renin inhibitor, with IC50 of 1.5 nM. Aliskiren fumarate can be used for the research of hypertension, cardiovascular diseases and cancer cachexia[1][2][3].

IC50 & Target

IC50: 1.5 nM (renin)[1]

体内研究
(In Vivo)

Aliskiren fumarate (< 10 mg/kg, Orally, daily) inhibits plasma renin activity and lowers blood pressure in sodium-depleted marmosets[2].
Aliskiren fumarate (10 mg/kg, Intragastrically, once) significantly alleviates multiple cachexia‑associated symptoms in BALB/c mice bearing C26 mouse colon carcinoma cells, including BW loss, tumor burden, muscle wasting, muscular dysfunction, and shortened survival[3].

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

分子量

667.83

Formula

C34H57N3O10

CAS 号

1196835-68-3

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]. Yuji Nakamura, et al. Discovery of DS-8108b, a Novel Orally Bioavailable Renin Inhibitor. ACS Med. Chem. Lett., 2012, 3 (9), pp 754–758

    [2]. Wood JM, et al. Structure-based design of aliskiren, a novel orally effective renin inhibitor. Biochem Biophys Res Commun. 2003 Sep 5;308(4):698-705.

    [3]. Wang C, et al. Aliskiren targets multiple systems to alleviate cancer cachexia. Oncol Rep. 2016 Nov;36(5):3014-3022.

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Cevipabulin fumarate(Synonyms: TTI-237 fumarate)

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。

Cevipabulin fumarate (Synonyms: TTI-237 fumarate) 纯度: 99.08%

Cevipabulin fumarate (TTI-237 fumarate) 是一种微管活性的、口服有效的抗肿瘤化合物,可抑制 [3H]长春碱与微管蛋白的结合,对人癌细胞的 IC50 值为 18-40 nM。

Cevipabulin fumarate(Synonyms: TTI-237 fumarate)

Cevipabulin fumarate Chemical Structure

CAS No. : 849550-67-0

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 ¥2147 In-stock
5 mg ¥1680 In-stock
10 mg ¥2880 In-stock
50 mg ¥8880 In-stock
100 mg ¥12400 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

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生物活性

Cevipabulin fumarate (TTI-237 fumarate) is an oral, microtubule-active, antitumor compound and inhibits the binding of [3H]NSC 49842 to tubulin, with an IC50 of 18-40 nM for cytotoxicity in human tumor cell line[1][2].

IC50 & Target

IC50: 18-40 nM (microtubule in human tumor cells)[1].

体外研究
(In Vitro)

Cevipabulin (0-50 nM, 72 hours) shows good activity (between 18 and 40 nM IC50 values) on cell lines from ovarian, breast, prostate, and cervical tumors[1].
Flow cytometry experiments reveal that, Cevipabulin (TTI-237) at low concentrations (20-40 nM) produces sub-G1 nuclei and, at concentrations above 50 nM, it causes a strong G2-M block[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 Cytotoxicity Assay[1]

Cell Line: Human cancer cell lines (SK-OV-3, MDA-MB-435, MDA-MB-468, LnCaP, and Hela cells).
Concentration: 0-50 nM
Incubation Time: 72 hours
Result: The IC50 values are 24±8 nM, 21±4 nM, 18±6 nM, 22±7 nM and 40 nM in SK-OV-3, MDA-MB-435, MDA-MB-468, LnCaP and Hela cells.

体内研究
(In Vivo)

Cevipabulin (TTI-2370)( 5, 10, 15, and 20 mg/kg, every 4 days for 4 cycles, in mice) is active by i.v. and p.o. administration against human tumor xenografts, showing dose-dependent effects, with good antitumor activity at 20 and 15 mg/kg[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 Model: Athymic nu/nu female mice implanted s.c. in the flank with 1×107 LoVo human colon adenocarcinoma cells[1].
Dosage: 5, 10, 15, and 20 mg/kg
Administration: I.V. injection every 4 days for 4 cycles.
Result: The compound showed dose-dependent effects, with good antitumor activity at 20 and 15 mg/kg.
Animal Model: Athymic nu/nu female mice implanted s.c. in the flank with 1×106 U87-MG human glioblastoma cells[1].
Dosage: 25 mg/kg.
Administration: P.O. or I.V. on days 0, 7, 14.
Result: The compound was active by p.o. or i.v. administration against human tumor xenografts.

Clinical Trial

分子量

580.89

Formula

C22H22ClF5N6O5

CAS 号

849550-67-0

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
In Vitro: 

DMSO : 50 mg/mL (86.07 mM; Need ultrasonic)

H2O : 1.43 mg/mL (2.46 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 1.7215 mL 8.6075 mL 17.2150 mL
5 mM 0.3443 mL 1.7215 mL 3.4430 mL
10 mM 0.1721 mL 0.8607 mL 1.7215 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 (sealed storage, away from moisture)。-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。

参考文献
  • [1]. Beyer CF, et al. TTI-237: a novel microtubule-active compound with in vivo antitumor activity. Cancer Res. 2008 Apr 1;68(7):2292-300.

    [2]. Beyer CF, et al. The microtubule-active antitumor compound TTI-237 has both DB01229-like and Leurocristine-like properties. Cancer Chemother Pharmacol. 2009 Sep;64(4):681-9.

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Tesmilifene fumarate(Synonyms: DPPE fumarate)

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。

Tesmilifene fumarate (Synonyms: DPPE fumarate) 纯度: 99.69%

Tesmilifene fumarate (DPPE fumarate) 是 H1C 受体的拮抗剂,可广泛的增强化疗的细胞毒性,并保护正常细胞。

Tesmilifene fumarate(Synonyms: DPPE fumarate)

Tesmilifene fumarate Chemical Structure

CAS No. : 1185241-83-1

规格 价格 是否有货 数量
5 mg ¥850 In-stock
10 mg ¥1300 In-stock
25 mg ¥2400 In-stock
50 mg   询价  
100 mg   询价  

* Please select Quantity before adding items.

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生物活性

Tesmilifene fumarate (DPPE fumarate), an H1C receptor antagonist, potentiates a wide range of cytotoxics and even to offer some protection of normal cells[1][2].

体外研究
(In Vitro)

Tesmilifene may modulate the effects of 12(S)HETE in cancer cells, and indirectly, influence the susceptibility of cellular DNA to chemotherapy[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)

Tesmilifene (DPPE, 20 mg/kg (s.c.) and 20 μg (icv in 5 μL)) potentiated seizures induced by both convulsants[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 Model: Male BKTO mice (25-45 g)[2].
Dosage: 20 mg/kg (s.c.) and 20 μg (icv in 5 μL).
Administration: S.C. and icv.
Result: Potentiated seizures induced by both convulsants.

Clinical Trial

分子量

399.48

Formula

C23H29NO5

CAS 号

1185241-83-1

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 (625.81 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.5033 mL 12.5163 mL 25.0325 mL
5 mM 0.5007 mL 2.5033 mL 5.0065 mL
10 mM 0.2503 mL 1.2516 mL 2.5033 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 (5.21 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (5.21 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 (5.21 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (5.21 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 (5.21 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (5.21 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]. Mark Vincent, et al. Tesmilifene may enhance breast cancer chemotherapy by killing a clone of aggressive, multi-drug resistant cells through its action on the p-glycoprotein pump. Med Hypotheses. 2006;66(4):715-31.

    [2]. G Sturman, et al. Modulation of the intracellular and H3-histamine receptors and chemically-induced seizures in mice Agents Actions. 1994 Jun;41 Spec No:C68-9.

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VTP50469 fumarate

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。

VTP50469 fumarate  纯度: 98.84%

VTP50469 fumarate 是一种有效的,高选择性和口服活性的 Menin-MLL 相互作用抑制剂,Ki 为 104 pM。VTP50469 fumarate 具有高效的抗白血病活性。

VTP50469 fumarate

VTP50469 fumarate Chemical Structure

CAS No. : 2169919-29-1

规格 价格 是否有货 数量
5 mg ¥3400 In-stock
10 mg ¥5800 In-stock
50 mg   询价  
100 mg   询价  

* Please select Quantity before adding items.

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生物活性

VTP50469 fumarate is a potent, highly selective and orally active Menin-MLL interaction inhibitor with a Ki of 104 pM. VTP50469 fumarate has potently anti-leukemia activity[1][2].

IC50 & Target

Ki: 104 pM (Menin-MLL interaction)[1][2]

体外研究
(In Vitro)

VTP50469 more potently and rapidly inhibits cell proliferation in a concentration-dependent manner in MLL-r cell lines carrying (MOLM13 (IC50 of 13 nM), THP1 (IC50 of 37 nM), NOMO1 (IC50 of 30 nM), ML2 (IC50 of 16 nM), EOL1 (IC50 of 20 nM), and murine MLL-AF9 cells (IC50 of 15 nM)) and ALL (KOPN8 (IC50 of 15 nM), HB11;19 (IC50 of 36 nM), MV4;11 (IC50 of 17 nM), SEMK2 (IC50 of 27 nM), and RS4;11 (IC50 of 25 nM)) cell lines[1].
At early timepoints MLL-r B cell ALL (B-ALL) cell lines, but not MLL-r AML cell lines, underwent apoptosis in response to VTP50469 in a dose-dependent manner. MLL-r AML cell lines underwent dose-dependent differentiation starting at 4-6 days of exposure to VTP50469[1].
VTP50469 displaces Menin from protein complexes and inhibits chromatin occupancy of MLL at select genes. Loss of MLL binding led to changes in gene expression, differentiation, and apoptosis[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)

VTP50469 (15-60 mg/kg; oral administration; twice a day; for 28 days; NSG mice) treatment is highly efficacious across all dosage levels and all treatment groups have a significant survival advantage. Mice dosed at 30 and 60 mg/kg VTP50469 extends survival advantage[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 Model: Unconditioned immunodeficient (NSG) mice with MV4;11 cells[1]
Dosage: 15 mg/kg, 30 mg/kg, and 60 mg/kg
Administration: Oral administration; twice a day; for 28 days
Result: Was highly efficacious across all dosage levels and all treatment groups had a significant survival advantage over the control group.

分子量

804.93

Formula

C36H51FN6O8S

CAS 号

2169919-29-1

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

溶解性数据
In Vitro: 

DMSO : 220 mg/mL (273.32 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.2423 mL 6.2117 mL 12.4234 mL
5 mM 0.2485 mL 1.2423 mL 2.4847 mL
10 mM 0.1242 mL 0.6212 mL 1.2423 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 (sealed storage, away from moisture and light)。-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: ≥ 5.5 mg/mL (6.83 mM); Clear solution

    此方案可获得 ≥ 5.5 mg/mL (6.83 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 55.0 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: ≥ 5.5 mg/mL (6.83 mM); Clear solution

    此方案可获得 ≥ 5.5 mg/mL (6.83 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 55.0 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: ≥ 5.5 mg/mL (6.83 mM); Clear solution

    此方案可获得 ≥ 5.5 mg/mL (6.83 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 55.0 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]. Krivtsov AV, et al. A Menin-MLL Inhibitor Induces Specific Chromatin Changes and Eradicates Disease in Models of MLL-Rearranged Leukemia. Cancer Cell. 2019 Dec 9;36(6):660-673.e11.

    [2]. Andrei V. Krivtsov, et al. Abstract 4958: VTP50469 is a novel, orally available menin-MLL1 inhibitor effective against MLL-rearranged and NPM1-mutant leukemia. Cancer Resceach. July 2018.Volume 78, Issue 13 Supplement.

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