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Tamoxifen(Synonyms: 他莫昔芬; ICI 47699; (Z)-Tamoxifen; trans-Tamoxifen)

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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。

Tamoxifen (Synonyms: 他莫昔芬; ICI 47699; (Z)-Tamoxifen; trans-Tamoxifen) 纯度: 99.92%

Tamoxifen (ICI 47699) 是一种口服有效的，选择性雌激素受体 (estrogen receptor) 调节剂 (SERM)，可阻断乳腺细胞中的雌激素作用，并可激活其他细胞，如骨骼，肝脏和子宫细胞中的雌激素活性。Tamoxifen 是一种有效的 Hsp90 激活剂，可增强 Hsp90 分子伴侣 ATPase 的活性。Tamoxifen 还可以有效抑制传染性 EBOV Zaire 和 Marburg (MARV)，IC50 分别为 0.1 µM 和 1.8 µM。Tamoxifen 可以激活自噬 (autophagy)，诱导凋亡 (apoptosis)。Tamoxifen 还可以诱导 CreER(T2) 转基因小鼠的基因敲除。

Tamoxifen(Synonyms: 他莫昔芬; ICI 47699; (Z)-Tamoxifen; trans-Tamoxifen)

Tamoxifen Chemical Structure

CAS No. : 10540-29-1

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10 mM * 1 mL in DMSO ￥550 In-stock
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1 g ￥690 In-stock
5 g ￥2750 In-stock
10 g ￥3500 In-stock
50 g   询价  

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Tamoxifen 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
  • Apoptosis Compound Library
  • Cell Cycle/DNA Damage Compound Library
  • Metabolism/Protease Compound Library
  • FDA-Approved Drug Library
  • Anti-Cancer Compound Library
  • CNS-Penetrant Compound Library
  • Autophagy Compound Library
  • Anti-Aging Compound Library
  • Drug Repurposing Compound Library
  • Anti-COVID-19 Compound Library
  • NMPA-Approved Drug Library
  • Endoplasmic Reticulum Stress Compound Library
  • Pyroptosis Compound Library
  • Cytoskeleton Compound Library
  • Orally Active Compound Library
  • FDA Approved & Pharmacopeial Drug Library
  • Drug-Induced Liver Injury (DILI) Compound Library
  • Targeted Therapy Drug Library
  • Tumorigenesis Related Compound Library
  • Rare Diseases Drug Library
  • Children’s Drug Library

生物活性

Tamoxifen (ICI 47699) is an orally active, selective estrogen receptor modulator (SERM) which blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells[1][2][3]. Tamoxifen is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.1 µM and 1.8 µM, respectively[5]. Tamoxifen activates autophagy and induces apoptosis[4]. Tamoxifen also can induce gene knockout of CreER(T2) transgenic mouse[6].

IC50 & Target[1][4]

Estrogen receptor

 

HSP90

 

体外研究
(In Vitro)

Tamoxifen (ICI 47699) shows strong inhibition of MCF-7 cells (EC50=1.41 μM) and to a lesser extent the T47D cells (EC50=2.5 μM) but does not affect the MDA-MB-231 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)

Injection of pre-mutant mice with Tamoxifen (75 mg/kg; injected for 5 days at 6 weeks of age) results in the excision of the floxed exon and, thus, in a gene knockout[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: Aldh1l1-cre/ERT2 x Ai95 mice[3]
Dosage: 75 mg/kg
Administration: Injected for 5 days at 6 weeks of age
Result: Resulted in the excision of the floxed exon and a gene knockout.

Clinical Trial

分子量

371.51

Formula

C26H29NO
CAS 号

10540-29-1
中文名称

他莫昔芬；三苯氧胺；它莫西芬
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
溶解性数据
In Vitro: 

DMSO : 62.5 mg/mL (168.23 mM; ultrasonic and warming and heat to 60°C)

Ethanol : 50 mg/mL (134.59 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.6917 mL 13.4586 mL 26.9172 mL
5 mM 0.5383 mL 2.6917 mL 5.3834 mL
10 mM 0.2692 mL 1.3459 mL 2.6917 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 (protect from 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： corn oil

    Solubility: 40 mg/mL (107.67 mM); Clear solution; Need ultrasonic

  • 2.

    请依序添加每种溶剂： 30% PEG400  0.5% Tween80  5% Propanediol  64.5%H2O

    Solubility: 5 mg/mL (13.46 mM); Suspended solution; Need ultrasonic

  • 3.

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

    Solubility: 2.5 mg/mL (6.73 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.5 mg/mL (6.73 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 EtOH 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% EtOH    90% corn oil

    Solubility: ≥ 2.5 mg/mL (6.73 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.73 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 EtOH 储备液加到 900 μL玉米油中，混合均匀。

  • 5.

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

    Solubility: ≥ 2.08 mg/mL (5.60 mM); Clear solution

    此方案可获得 ≥ 2.08 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 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

  • 6.

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

    Solubility: 2.08 mg/mL (5.60 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.08 mg/mL (5.60 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 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
  • 7.

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

    Solubility: ≥ 2.08 mg/mL (5.60 mM); Clear solution

    此方案可获得 ≥ 2.08 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 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

  • 8.

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

    Solubility: ≥ 0.83 mg/mL (2.23 mM); Clear solution

  • 9.

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

    Solubility: 0.83 mg/mL (2.23 mM); Suspended solution; Need ultrasonic

*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]. Osborne CK. Tamoxifen in the treatment of breast cancer. N Engl J Med. 1998 Nov 26;339(22):1609-18.

    [2]. Hawariah A, et al. In vitro response of human breast cancer cell lines to the growth-inhibitory effects of styrylpyrone derivative (SPD) and assessment of its antiestrogenicity. Anticancer Res. 1998 Nov-Dec;18(6A):4383-6.

    [3]. Jun Nagai, et al. Hyperactivity with Disrupted Attention by Activation of an Astrocyte Synaptogenic Cue. Cell. 2019 May 16;177(5):1280-1292.e20.

    [4]. Zhao R, et al. Tamoxifen enhances the Hsp90 molecular chaperone ATPase activity. PLoS One. 2010 Apr 1;5(4):e9934.

    [5]. Kedjouar B, et al. Molecular characterization of the microsomal tamoxifen binding site. J Biol Chem. 2004 Aug 6;279(32):34048-61.

    [6]. Feil S, et, al. Inducible Cre mice. Methods Mol Biol. 2009;530:343-63.

    [7]. Laura Cooper, et al. Screening and Reverse-Engineering of Estrogen Receptor Ligands as Potent Pan-Filovirus Inhibitors. J Med Chem. 2020 Sep 4.

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Fulvestrant(Synonyms: 氟维司群; ICI 182780; ZD 9238; ZM 182780)

发表于由

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。

Fulvestrant (Synonyms: 氟维司群; ICI 182780; ZD 9238; ZM 182780) 纯度: 99.95%

Fulvestrant (ICI 182780) 是一种纯抗雌激素，也是一种有效的雌激素受体 (ER) 拮抗剂，IC50 为 9.4 nM。Fulvestrant 还是一种 GPR30 的激动剂。Fulvestrant 有效抑制 ER 阳性 MCF-7 细胞的生长，IC50 为 0.29 nM。Fulvestrant 还可诱导细胞自噬 (autophagy) 和凋亡 (apoptosis)，并具有抗肿瘤功效。

Fulvestrant(Synonyms: 氟维司群; ICI 182780; ZD 9238; ZM 182780)

Fulvestrant Chemical Structure

CAS No. : 129453-61-8

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 ￥506 In-stock
10 mg ￥460 In-stock
50 mg ￥1130 In-stock
100 mg ￥1989 In-stock
500 mg ￥5960 In-stock
1 g   询价  
5 g   询价  

* Please select Quantity before adding items.

Fulvestrant 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
  • Apoptosis Compound Library
  • FDA-Approved Drug Library
  • Anti-Cancer Compound Library
  • Autophagy Compound Library
  • Drug Repurposing Compound Library
  • Lipid Compound Library
  • FDA Approved & Pharmacopeial Drug Library
  • Anti-Breast Cancer Compound Library
  • Drug-Induced Liver Injury (DILI) Compound Library
  • Targeted Therapy Drug Library
  • Rare Diseases Drug Library

生物活性

Fulvestrant (ICI 182780) is a pure antiestrogen and a potent estrogen receptor (ER) antagonist with an IC50 of 9.4 nM. Fulvestrant is also a GPR30 agonist. Fulvestrant effectively inhibits the growth of ER-positive MCF-7 cells with an IC50 of 0.29 nM. Fulvestrant also induces autophagy and has antitumor efficacy[1].

IC50 & Target

IC50: 9.4 nM (Estrogen Receptor)[1]
体外研究
(In Vitro)

Fulvestrant (ICI 182780; ZD 9238; ZM 182780) is a potent and specific inhibitor of estrogen action and demonstrates excellent growth-inhibitory effects in both cell and animal models of human breast cancer. Fulvestrant inhibits MCF-7 human breast cancer cells growth with the IC50 of 0.29 nM. The relative binding affinities of Fulvestrant is 0.89. Fulvestrant has significantly increased antiestrogenic potency and retains pure estrogen antagonist activity[1]. Fulvestrant is the first of a new type of endocrine treatment-an oestrogen receptor (ER) antagonist that downregulates the ER[3]. Treatment of MCF-7 cells with 1 µM ICI 47699 has no effect on the expression of ERα, whereas 100 nM Fulvestrant completely inhibits ERα expression[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.
体内研究
(In Vivo)

When administered alone, parenterally (s.c.), to immature female rats Fulvestrant (ICI 182,780) is devoid of uterotropic activity. Complete antagonism of Estrogen action is achieved with a dose of 0.5 mg Fulvestrant/kg/day s.c. The effects of Fulvestrant administered p.o. are qualitatively similar but potency is reduced by an order of magnitude compare with s.c. dosing (ED50 0.46 and complete antagonism at 5 mg/kg/day p.o.)[1]. The anti-tumor activity of Fulvestrant is first demonstrated in two models of human breast cancer in nude mice. In one of these models, the growth of MCF-7 tumor xenografts is completely blocked for at least 4 weeks following a single injection of Fulvestrant 5 mg. Similar reductions in growth are seen in the Br10 human tumor model. In other studies in nude mice bearing MCF-7 xenografts, Fulvestrant suppresses the growth of established tumours for twice as long and tumor growth is delayed to a greater extent than is observed with ICI 47699 treatment. ICI 47699-resistant breast tumors, which grow in nude mice after long-term treatment with ICI 47699, remain ensitive to growth inhibition by Fulvestrant[3]. These are comparable to the tumor growth inhibition (TGI) observed for ICI 47699 and Fulvestrant, which on day 40 are 86 and 88%, respectively[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.
Clinical Trial

分子量

606.77

Formula

C32H47F5O3S
CAS 号

129453-61-8
中文名称

氟维司群；氟维司琼
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 (412.02 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.6481 mL 8.2404 mL 16.4807 mL
5 mM 0.3296 mL 1.6481 mL 3.2961 mL
10 mM 0.1648 mL 0.8240 mL 1.6481 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 (4.53 mM); Suspended solution; Need ultrasonic

  • 2.

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

    Solubility: ≥ 2.5 mg/mL (4.12 mM); Suspended solution

    此方案可获得 ≥ 2.5 mg/mL (4.12 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 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： 15% Solutol HS 15  10% Cremophor EL  35% PEG 400   40% water

    Solubility: 2.5 mg/mL (4.12 mM); Suspended solution; Need ultrasonic

  • 4.

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

    Solubility: 2.08 mg/mL (3.43 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.08 mg/mL (3.43 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 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

  • 5.

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

    Solubility: ≥ 2.08 mg/mL (3.43 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (3.43 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]. Wakeling AE, et al. A potent specific pure antiestrogen with clinical potential. Cancer Res. 1991 Aug 1;51(15):3867-73.

    [2]. Yu X, et al.MiR-214 increases the sensitivity of breast cancer cells to tamoxifen and fulvestrant through inhibition of autophagy.Mol Cancer. 2015 Dec 15;14:208.

    [3]. Osborne CK, et al. Fulvestrant: an oestrogen receptor antagonist with a novel mechanism of action. Br J Cancer. 2004 Mar;90 Suppl 1:S2-6.

    [4]. Garner F, et al. RAD1901: a novel, orally bioavailable selective estrogen receptor degrader that demonstrates antitumor activity in breast cancer xenograft models. Anticancer Drugs. 2015 Oct;26(9):948-56

    [5]. Julia Kuhn, et al. GPR30 estrogen receptor agonists induce mechanical hyperalgesia in the rat. Eur J Neurosci. 2008 Apr;27(7):1700-9.
Cell Assay
[3]

MCF-7 or T47D cells are cultured in 10 cm dishes to ~75% confluence in EMEM growth medium. Twenty-four hours before treatment, the growth medium is replaced with phenol red-free RPMI-1640 growth medium. A stock solution of 10 mM RAD1901 is prepared in DMSO. Dilutions of RAD1901 are prepared in RPMI growth medium (doses ranging from 10 to 0.5 nM). Controls include 0.1% DMSO alone (vehicle), 100 nM Fulvestrant, and 1 µM ICI 47699. Plated cells are treated with RAD1901 or controls for 48 h, and then incubated for 15 min with ice-cold lysis buffer [1 mM EDTA, 0.5% Triton X-100, 5 mM NaF, 6 M urea, 1 mM sodium orthovanadate, 2.5 mM sodium pyrophosphate, and 1× HALT protease inhibitor cocktail]. Lysates are centrifuged at 2000g for 5 min, and the supernatant is diluted 1 : 1 in lysis buffer. Ninety-six-well plates are coated overnight with capture antibody (1 µg/mL), washed three times in the manufacturer’s wash buffer, blocked with blocking buffer for 2 h, and washed again. The prepared plates are incubated with 100 µL of the prepared cell lysate for 2 h, washed, incubated with biotinylated detection antibody for 2 h, and washed again. After a 20 min incubation with streptavidin-horseradish peroxidase, the plates are washed and incubated with substrate solution for 20 min. The reaction is stopped with stop solution, and the plates are analyzed on a microplate reader (OD450)[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
[1][3]

Rats[1]
In studies with OVX rats, surgical preparation is performed at least 2 weeks before treatment began. To measure the duration of action of a single large dose of Fulvestrant, OVX rats are treated with a daily s.c. dose of 0.5 μg of estradici benzoate beginning on the day of Fulvestrant administration and continued until vaginal smears showed evidence of cornification. At that point the experiment is terminated and uterine weight is recorded. The arachis oil formulation used in these single dose duration of action studies contained 50 mg Fulvestrant/mL.
Mice[3]
Female athymic nude mice [Crl:NU(NCr)-Foxn1nu] are used for tumor xenograft studies. Fourteen days after tumor cell implantation (designated as day 1 of the study), mice are 9 weeks of age, with body weights ranging from 21.4 to 32.5 g, individual tumor volumes ranging from 75 to 144 mm3, and a group mean tumor volume (MTV) of 108 mm3. The mice are randomized into nine groups of 15 animals each and treated with vehicle, ICI 47699 (1 mg/animal every other day), Fulvestrant (0.5 mg/animal daily), or RAD1901 (0.3, 1, 3, 10, 30, 60, 90, and 120 mg/kg daily). Tumor volumes are evaluated twice per week. The tumor endpoint is defined as an MTV of 1500 mm3 in the control group. Animals are also monitored for partial regression (PR) and complete regression responses.

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]. Wakeling AE, et al. A potent specific pure antiestrogen with clinical potential. Cancer Res. 1991 Aug 1;51(15):3867-73.

    [2]. Yu X, et al.MiR-214 increases the sensitivity of breast cancer cells to tamoxifen and fulvestrant through inhibition of autophagy.Mol Cancer. 2015 Dec 15;14:208.

    [3]. Osborne CK, et al. Fulvestrant: an oestrogen receptor antagonist with a novel mechanism of action. Br J Cancer. 2004 Mar;90 Suppl 1:S2-6.

    [4]. Garner F, et al. RAD1901: a novel, orally bioavailable selective estrogen receptor degrader that demonstrates antitumor activity in breast cancer xenograft models. Anticancer Drugs. 2015 Oct;26(9):948-56

    [5]. Julia Kuhn, et al. GPR30 estrogen receptor agonists induce mechanical hyperalgesia in the rat. Eur J Neurosci. 2008 Apr;27(7):1700-9.

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Goserelin acetate(Synonyms: 醋酸戈舍瑞林; ICI-118630 acetate)

发表于由

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。

Goserelin acetate (Synonyms: 醋酸戈舍瑞林; ICI-118630 acetate) 纯度: 99.23%

Goserelin acetate (ICI-118630 acetate) 是一种促性腺激素释放激素 (GnRH/LHRH) 十肽类似物，能作为 GnRH 激动剂。Goserelin acetate 可用于乳腺癌、上皮性卵巢癌和前列腺癌的研究。

Goserelin acetate(Synonyms: 醋酸戈舍瑞林; ICI-118630 acetate)

Goserelin acetate Chemical Structure

CAS No. : 145781-92-6

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥1930 In-stock
5 mg ￥910 In-stock
10 mg ￥1320 In-stock
50 mg ￥4620 In-stock
100 mg   询价  
200 mg   询价  

* Please select Quantity before adding items.

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•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
  • Apoptosis Compound Library
  • GPCR/G Protein Compound Library
  • FDA-Approved Drug Library
  • Anti-Cancer Compound Library
  • Drug Repurposing Compound Library
  • Endocrinology Compound Library
  • FDA Approved & Pharmacopeial Drug Library
  • Anti-Breast Cancer Compound Library
  • Drug-Induced Liver Injury (DILI) Compound Library
  • Targeted Diversity Library
  • Rare Diseases Drug Library
  • Peptide Library

生物活性

Goserelin acetate (ICI-118630 acetate), a decapeptide analogue of gonadotropin-releasing hormone (GnRH/LHRH), functions as a GnRH agonist. Goserelin acetate can be used for the research of breast cancer, epithelial ovarian cancer and prostate cancer[1][2].

IC50 & Target

GnRH[1]
体外研究
(In Vitro)

Goserelin (1 nM-1 mM; 48-72 hours) promotes EOC cell apoptosis[1].
Goserelin (100 μM; 24-72 hours) regulates the expression of human apoptosis-related genes in SKOV3-ip cells[1].
Goserelin (100 μM; 24-72 hours) promotes EOC cell apoptosis by upregulating FOXO1 through the PI3K/AKT signaling pathway[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.

Apoptosis Analysis[1]

Cell Line: SKOV3 cells, SKOV3-ip cells, A2780 cells (human EOC cell lines)
Concentration: 1 nM, 10 nM, 100 nM, 1 μM, 10 μM, 100 μM, 1 mM
Incubation Time: 48 hours, 72 hours
Result: Significantly increased the total apoptosis rate of SKOV3-ip, SKOV3 and A2780 cells.

Western Blot Analysis[1]

Cell Line: SKOV3 cells, SKOV3-ip cells, A2780 cells (human EOC cell lines)
Concentration: 1 nM, 10 nM, 100 nM, 1 μM, 10 μM, 100 μM, 1 mM
Incubation Time: 48 hours, 72 hours
Result: The expression of cleaved-caspase-3 and cleaved-PARP were observably increased at 100 μM.

RT-PCR[1]

Cell Line: SKOV3-ip cells
Concentration: 100 μM
Incubation Time: 24 hours, 48 hours, 72 hours
Result: Expression of human apoptosis-related genes regulated

体内研究
(In Vivo)

Goserelin (100 µg; s.c.; daily; for 19 days) significantly increases the proportion of apoptotic cells in the subcutaneous xenograft tumors[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: Five-week-old specific-pathogen free (SPF) female nude mice (18-20 g), subcutaneous xenograft tumor model[1]
Dosage: 100 µg/mice
Administration: Subcutaneous injection, daily, for 19 days
Result: Significantly increased the proportion of apoptotic cells in the subcutaneous xenograft tumors

Clinical Trial

分子量

1329.46

Formula

C61H88N18O16
CAS 号

145781-92-6
中文名称

醋酸戈舍瑞林
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Sealed storage, away from moisture

Powder -80°C 2 years
-20°C 1 year

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

H2O : 100 mg/mL (75.22 mM; Need ultrasonic)

DMSO : ≥ 28 mg/mL (21.06 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 0.7522 mL 3.7609 mL 7.5219 mL
5 mM 0.1504 mL 0.7522 mL 1.5044 mL
10 mM 0.0752 mL 0.3761 mL 0.7522 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 (1.56 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (1.56 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 (1.56 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (1.56 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 (1.56 mM); Clear solution; Need warming

    此方案可获得 2.08 mg/mL (1.56 mM) 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]. Ning Zhang, et al. Goserelin promotes the apoptosis of epithelial ovarian cancer cells by upregulating forkhead box O1 through the PI3K/AKT signaling pathway. Oncol Rep. 2018 Mar; 39(3): 1034–1042.

    [2]. Halle C F Moore, et al. Goserelin for ovarian protection during breast-cancer adjuvant chemotherapy. N Engl J Med. 2015 Mar 5;372(10):923-32.

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

Tamoxifen Citrate(Synonyms: 他莫昔芬柠檬酸盐; ICI 46474; (Z)-Tamoxifen Citrate; trans-Tamoxifen Citrate)

发表于由

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。

Tamoxifen Citrate (Synonyms: 他莫昔芬柠檬酸盐; ICI 46474; (Z)-Tamoxifen Citrate; trans-Tamoxifen Citrate) 纯度: 99.93%

Tamoxifen Citrate (ICI 46474) 是一种口服有效的，选择性雌激素受体调节剂 (SERM)，可阻断乳腺细胞中的雌激素作用，并可激活其他细胞，如骨骼，肝脏和子宫细胞中的雌激素活性。Tamoxifen Citrate 是一种有效的 Hsp90 激活剂，可增强 Hsp90 分子伴侣 ATPase 的活性。Tamoxifen Citrate 还可以有效抑制传染性 EBOV Zaire 和 Marburg (MARV)，IC50 分别为 0.1 µM 和 1.8 µM。Tamoxifen Citrate 可以激活自噬 (autophagy)，诱导凋亡 (apoptosis)。

Tamoxifen Citrate(Synonyms: 他莫昔芬柠檬酸盐; ICI 46474; (Z)-Tamoxifen Citrate; trans-Tamoxifen Citrate)

Tamoxifen Citrate Chemical Structure

CAS No. : 54965-24-1

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 ￥550 In-stock
500 mg ￥500 In-stock
1 g ￥690 In-stock
5 g ￥2750 In-stock
10 g   询价  
50 g   询价  

* Please select Quantity before adding items.

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生物活性

Tamoxifen Citrate (ICI 46474) is an orally active, selective estrogen receptor modulator (SERM) which blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells[1][2][3].Tamoxifen Citrate is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen Citrate also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.1 µM and 1.8 µM, respectively[5]. Tamoxifen Citrate activates autophagy and induces apoptosis[4].

IC50 & Target

HSP90

 

Estrogen receptor

 

体外研究
(In Vitro)

Tamoxifen Citrate (ICI 46474) shows strong inhibition of MCF-7 cells (EC50=1.41 μM) and to a lesser extent the T47D cells (EC50=2.5 μM) but does not affect the MDA-MB-231 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)

The Tamoxifen Citrate-inducible gene knockout strategy has clear advantages in that expression of a gene can be ablated in adult mice at will in a tissue specific manner. To study the role of Med1 in adult heart, 7-week old TmcsMed1-/- mice are given a daily Iintraperitoneal injection of Tamoxifen Citrate at a dose of 65 mg/kg for 5 days and killed at selected intervals thereafter. qPCR analysis of RNA shows that the Med1 expression begin to decrease after 3 days of Tamoxifen Citrate injection (about 70% decrease), and by 5 days of injection, Med1 expression is almost non-detectable in the heart. Tamoxifen Citrate-inducible cardiac-specific disruption of Med1 (TmcsMed1-/-) in adult mice causes dilated cardiomyopathy[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

563.64

Formula

C32H37NO8
CAS 号

54965-24-1
中文名称

他莫昔芬柠檬酸盐
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 (88.71 mM; Need ultrasonic)

Ethanol : 10 mg/mL (17.74 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 1.7742 mL 8.8709 mL 17.7418 mL
5 mM 0.3548 mL 1.7742 mL 3.5484 mL
10 mM 0.1774 mL 0.8871 mL 1.7742 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： corn oil

    Solubility: 10 mg/mL (17.74 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 (3.69 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (3.69 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 (3.69 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (3.69 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 (3.69 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (3.69 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]. Osborne CK. Tamoxifen in the treatment of breast cancer. N Engl J Med. 1998 Nov 26;339(22):1609-18.

    [2]. Hawariah A, et al. In vitro response of human breast cancer cell lines to the growth-inhibitory effects of styrylpyrone derivative (SPD) and assessment of its antiestrogenicity. Anticancer Res. 1998 Nov-Dec;18(6A):4383-6.

    [3]. Jia Y, et al. Cardiomyocyte-Specific Ablation of Med1 Subunit of the Mediator Complex Causes Lethal DilatedCardiomyopathy in Mice. PLoS One. 2016 Aug 22;11(8):e0160755.

    [4]. Zhao R, et al. Tamoxifen enhances the Hsp90 molecular chaperone ATPase activity. PLoS One. 2010 Apr 1;5(4):e9934.

    [5]. Laura Cooper, et al. Screening and Reverse-Engineering of Estrogen Receptor Ligands as Potent Pan-Filovirus Inhibitors. J Med Chem. 2020 Sep 4.
Animal Administration
[3]

Mice[3]
Seven-week old TmcsMed1-/- mice and the wild-type littermates are then administered Tamoxifen intraperitoneally at a daily dose of 65 mg/kg body weight for 5 days and then killed at selected intervals after initiation of Tamoxifen treatment. For each experiment 3 to 5 mice for control and csMed1-/- are used. To obtain survival curve 41 csMed1-/- and 41 csMed1fl/fl mice are used. Thirteen TmcsMed-/- mice and the same number of littermates are used for the survival curve experiments using Tamoxifen inducible model.

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]. Osborne CK. Tamoxifen in the treatment of breast cancer. N Engl J Med. 1998 Nov 26;339(22):1609-18.

    [2]. Hawariah A, et al. In vitro response of human breast cancer cell lines to the growth-inhibitory effects of styrylpyrone derivative (SPD) and assessment of its antiestrogenicity. Anticancer Res. 1998 Nov-Dec;18(6A):4383-6.

    [3]. Jia Y, et al. Cardiomyocyte-Specific Ablation of Med1 Subunit of the Mediator Complex Causes Lethal DilatedCardiomyopathy in Mice. PLoS One. 2016 Aug 22;11(8):e0160755.

    [4]. Zhao R, et al. Tamoxifen enhances the Hsp90 molecular chaperone ATPase activity. PLoS One. 2010 Apr 1;5(4):e9934.

    [5]. Laura Cooper, et al. Screening and Reverse-Engineering of Estrogen Receptor Ligands as Potent Pan-Filovirus Inhibitors. J Med Chem. 2020 Sep 4.

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

Goserelin(Synonyms: 戈舍瑞林; ICI 118630)

发表于由

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。

Goserelin (Synonyms: 戈舍瑞林; ICI 118630)

Goserelin (ICI 118630) 是一种促性腺激素释放激素 (GnRH/LHRH) 十肽类似物，能作为 GnRH 激动剂。Goserelin 可用于乳腺癌、上皮性卵巢癌和前列腺癌的研究。

Goserelin(Synonyms: 戈舍瑞林; ICI 118630)

Goserelin Chemical Structure

CAS No. : 65807-02-5

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

* Please select Quantity before adding items.

Goserelin 的其他形式现货产品:

Goserelin acetate

生物活性

Goserelin (ICI 118630), a decapeptide analogue of gonadotropin-releasing hormone (GnRH/LHRH), functions as a GnRH agonist. Goserelin can be used for the research of breast cancer, epithelial ovarian cancer and prostate cancer[1][2].

IC50 & Target

GnRH[1]
体外研究
(In Vitro)

Goserelin (1 nM-1 mM; 48-72 hours) promots EOC cell apoptosis[1].
Goserelin (100 μM; 24-72 hours) regulates the expression of human apoptosis-related genes in SKOV3-ip cells[1].
Goserelin (100 μM; 24-72 hours) influences EOC cell apoptosis by upregulating FOXO1 through the PI3K/AKT signaling pathway[1].

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

Apoptosis Analysis[1]

Cell Line: SKOV3 cells, SKOV3-ip cells, A2780 cells (human EOC cell lines)
Concentration: 1 nM, 10 nM, 100 nM, 1 μM, 10 μM, 100 μM, 1 mM
Incubation Time: 48 hours, 72 hours
Result: Significantly increased the total apoptosis rate of SKOV3-ip, SKOV3 and A2780 cells.

Western Blot Analysis[1]

Cell Line: SKOV3 cells, SKOV3-ip cells, A2780 cells (human EOC cell lines)
Concentration: 1 nM, 10 nM, 100 nM, 1μM , 10 μM, 100 μM, 1 mM
Incubation Time: 48 hours, 72 hours
Result: The expression of cleaved-caspase-3 and cleaved-PARP were observably increased at 100 μM.

RT-PCR[1]

Cell Line: SKOV3-ip cells
Concentration: 100 μM
Incubation Time: 24 hours, 48 hours, 72 hours
Result: Expression of human apoptosis-related genes regulated

体内研究
(In Vivo)

Goserelin (100 µg; s.c.; daily; for 19 days) significantly increases the proportion of apoptotic cells in the subcutaneous xenograft tumors[1].

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

Animal Model: Five-week-old specific-pathogen free (SPF) female nude mice (18-20 g), subcutaneous xenograft tumor model[1]
Dosage: 100 µg/mice
Administration: Subcutaneous injection, daily, for 19 days
Result: Significantly increased the proportion of apoptotic cells in the subcutaneous xenograft tumors

Clinical Trial

分子量

1269.41

Formula

C59H84N18O14
CAS 号

65807-02-5
中文名称

戈舍瑞林
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]. Ning Zhang, et al. Goserelin promotes the apoptosis of epithelial ovarian cancer cells by upregulating forkhead box O1 through the PI3K/AKT signaling pathway. Oncol Rep. 2018 Mar; 39(3): 1034–1042.

    [2]. Halle C F Moore, et al. Goserelin for ovarian protection during breast-cancer adjuvant chemotherapy. N Engl J Med. 2015 Mar 5;372(10):923-32.

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Pentagastrin(Synonyms: 五肽胃泌素; ICI-50123)

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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。

Pentagastrin (Synonyms: 五肽胃泌素; ICI-50123) 纯度: 98.02%

Pentagastrin (ICI-50123) 是胆囊收缩素 B (CCKB) 受体的选择性激动剂，IC50 为 11 nM。可增强胃粘膜对酸的防御机制，并保护胃粘膜免受损伤。

Pentagastrin(Synonyms: 五肽胃泌素; ICI-50123)

Pentagastrin Chemical Structure

CAS No. : 5534-95-2

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥676 In-stock
5 mg ￥550 In-stock
10 mg ￥800 In-stock
25 mg ￥1600 In-stock
50 mg ￥2600 In-stock
100 mg ￥4400 In-stock
200 mg   询价  
500 mg   询价  

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生物活性

Pentagastrin (ICI-50123) is a selective agonist of Cholecystokinin B (CCKB) receptor with an IC50 of 11 nM[1]. Pentagastrin enhances gastric mucosal defence mechanisms against acid and protects the gastric mucosa from experimental injury[2].

IC50 & Target

IC50: 11 nM (CCKB receptor)[1]
体外研究
(In Vitro)

Cholecystokinin receptors on GH3 rat anterior pituitary cells have been characterised using radioligand binding and Ca2+ mobilisation. Competition curve with Pentagastrin (IC50 of 25 nM) is consistent with a population predominantly of CCKB receptors. The selective CCKB receptor agonist, Pentagastrin, (0.1 nM-100 μM) dose dependently increased intracellular Ca2+ with a maximal increase of 2.77-fold. Binding of 50 pM [125I]BHCCK to GH 3 cells is dose dependently inhibited by Pentagastrin IC50 of 45 nM. Response to a submaximal dose of the CCKB receptor agonist Pentagastrin (100 nM) was dose dependently blocked by the CCKB receptor antagonist L-365,260[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)

Pentagastrin (80 µg/kg/h; intravenous injection; male Sprague-Dawley rats) treatment protects rat gastric mucosa from acidified aspirin injury. Pentagastrin induces a hyperaemic response to luminal acid challenge, increases mucus gel thickness, and elevates intracellular pH (pHi) during acid challenge[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 Sprague-Dawley rats (approximately 200 g)[2]
Dosage: 80 µg/kg/h
Administration: Intravenous injection
Result: Protected rat gastric mucosa from acidified aspirin injury. Induced a hyperaemic response to luminal acid challenge, increased mucus gel thickness, and elevated pHi during acid challenge.

分子量

767.89

Formula

C37H49N7O9S
CAS 号

5534-95-2
中文名称

五肽胃泌素；五肽胃必素；五肽促胃液素
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Protect from light

Powder -80°C 2 years
-20°C 1 year

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
溶解性数据
In Vitro: 

DMSO : ≥ 34 mg/mL (44.28 mM)

H2O : 1 mg/mL (1.30 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 1.3023 mL 6.5113 mL 13.0227 mL
5 mM 0.2605 mL 1.3023 mL 2.6045 mL
10 mM 0.1302 mL 0.6511 mL 1.3023 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 (protect from 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: ≥ 2.08 mg/mL (2.71 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (2.71 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% corn oil

    Solubility: ≥ 2.08 mg/mL (2.71 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (2.71 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]. Smith AJ, et al. Characterisation of CCKB receptors on GH3 pituitary cells: receptor activation is linked to Ca2+ mobilisation. Eur J Pharmacol. 1994 Apr 15;267(2):215-23.

    [2]. Tanaka S, et al. Pentagastrin gastroprotection against acid is related to H2 receptor activation but not acid secretion. Gut. 1998 Sep;43(3):334-41.

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Tamoxifen-​d5(Synonyms: ICI 47699-​d5; (Z)-Tamoxifen-​d5; trans-Tamoxifen-​d5)

发表于由

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。

Tamoxifen-​d5 (Synonyms: ICI 47699-​d5; (Z)-Tamoxifen-​d5; trans-Tamoxifen-​d5)

Tamoxifen-d5 (ICI 47699-d5) 是一种 Tamoxifen 氘代物。Tamoxifen (ICI 47699) 是一种口服有效的，选择性雌激素受体调节剂 (SERM)，可阻断乳腺细胞中的雌激素作用，并可激活其他细胞，如骨骼，肝脏和子宫细胞中的雌激素活性。Tamoxifen 是一种有效的 Hsp90 激活剂，可增强 Hsp90 分子伴侣 ATPase 的活性。

Tamoxifen-​d5(Synonyms: ICI 47699-​d5; (Z)-Tamoxifen-​d5; trans-Tamoxifen-​d5)

Tamoxifen-​d5 Chemical Structure

CAS No. : 157698-32-3

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

* Please select Quantity before adding items.

生物活性

Tamoxifen-d5 (ICI 47699-d5) is a deuterium labeled Tamoxifen. Tamoxifen (ICI 47699) is an orally active, selective estrogen receptor modulator (SERM). Tamoxifen is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity[1][2].

IC50 & Target

Estrogen receptor

 

HSP90

 

分子量

376.55

Formula

C26H24D5NO
CAS 号

157698-32-3
中文名称

他莫昔芬 ​d5
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]. Osborne CK. Tamoxifen in the treatment of breast cancer. N Engl J Med. 1998 Nov 26;339(22):1609-18.

    [2]. Zhao R, et al. Tamoxifen enhances the Hsp90 molecular chaperone ATPase activity. PLoS One. 2010 Apr 1;5(4):e9934.

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