标签归档：mestranol

Mestranol(Synonyms: 美雌醇；炔雌醇甲醚)

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。

Mestranol (Synonyms: 美雌醇；炔雌醇甲醚) 纯度: 99.97%

Mestranol 是一种非活性的前药，在转化为炔雌醇 (EE) 时具有生物活性。Mestranol是一种雌激素受体 (estrogen receptor) 激动剂。动物实验中，Mestranol 可以与黄体酮联合使用，Mestranol 可用于更年期激素或月经紊乱的研究。

Mestranol(Synonyms: 美雌醇；炔雌醇甲醚)

Mestranol Chemical Structure

CAS No. : 72-33-3

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥770 In-stock
100 mg ￥700 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Mestranol 相关产品

•相关化合物库:

  • Covalent Screening Library Plus
  • Drug Repurposing Compound Library Plus
  • FDA-Approved Drug Library Plus
  • FDA-Approved Drug Library Mini
  • Bioactive Compound Library Plus
  • FDA-Approved Drug Library
  • Anti-Cancer Compound Library
  • Drug Repurposing Compound Library
  • Covalent Screening Library
  • Lipid Compound Library
  • Endocrinology Compound Library
  • Anti-COVID-19 Compound Library
  • FDA Approved & Pharmacopeial Drug Library
  • Tumorigenesis Related Compound Library
  • Rare Diseases Drug Library

生物活性

Mestranol is an inactive prodrug and becomes biologically active on conversion to ethinyl estradiol (EE). Mestranol acts as an estrogen receptor agonist. Mestranol combines with a progestin in vivo and can be used for the research of menopausal hormone or menstrual disorders[1][2].

体外研究
(In Vitro)

Mestranol is a low potency synthetic estrogen that has been shown to be much more stable than 17β-Estradiol(HY-B0141) in hepatoma cell culture[3].
Mestranol (10 μM; 6 days) stimulates the growth of ERpositive MCF-7 WS8 cells up to 250% of control levels, growth stimulation could be partially reversed by tamoxifen[3].
However, in Hep G2 hepatoma cells, Mestranol (10 μM; 6 days) inhibits the growth of Hep 3B cells by 40% compared to control cells. Mestranol alone or cotreatment with tamoxifen both can inhibit cell growth. And cotreatment exhibits an additive effect with tamoxifen on growth inhibition[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

310.43

Formula

C21H26O2
CAS 号

72-33-3
中文名称

美雌醇；炔雌醇甲醚
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 (107.37 mM; Need ultrasonic)

H2O : 0.67 mg/mL (2.16 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.2213 mL 16.1067 mL 32.2134 mL
5 mM 0.6443 mL 3.2213 mL 6.4427 mL
10 mM 0.3221 mL 1.6107 mL 3.2213 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% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (6.70 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (6.70 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
  • 2.

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

    Solubility: ≥ 2.08 mg/mL (6.70 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (6.70 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]. H Kappus, et al. Affinity of ethynyl-estradiol and mestranol for the uterine estrogen receptor and for the microsomal mixed function oxidase of the liver. J Steroid Biochem. 1973 Mar;4(2):121-8.

    [2]. J W Goldzieher, et al. Pharmacokinetics of ethinyl estradiol and mestranol. Am J Obstet Gynecol. 1990 Dec;163(6 Pt 2):2114-9.

    [3]. S Y Jiang, et al. Tamoxifen inhibits hepatoma cell growth through an estrogen receptor independent mechanism. J Hepatol. 1995 Dec;23(6):712-9.

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

Mestranol-d2

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。

Mestranol-d2 

Mestranol-d2 是 Mestranol 氘代物。Mestranol 是一种非活性的前药，在转化为炔雌醇 (EE) 时具有生物活性。Mestranol是一种雌激素受体 (estrogen receptor) 激动剂。动物实验中，Mestranol 可以与黄体酮联合使用，Mestranol 可用于更年期激素或月经紊乱的研究。

Mestranol-d2

Mestranol-d2 Chemical Structure

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

Mestranol-d2 is the deuterium labeled Mestranol. Mestranol is an inactive prodrug and becomes biologically active on conversion to ethinyl estradiol (EE). Mestranol acts as an estrogen receptor agonist. Mestranol combines with a progestin in vivo and can be used for the research of menopausal hormone or menstrual disorders[1][2][3].

体外研究
(In Vitro)

Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].

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

312.44

Formula

C21H24D2O2
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]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.

    [2]. H Kappus, et al. Affinity of ethynyl-estradiol and mestranol for the uterine estrogen receptor and for the microsomal mixed function oxidase of the liver. J Steroid Biochem. 1973 Mar;4(2):121-8.

    [3]. J W Goldzieher, et al. Pharmacokinetics of ethinyl estradiol and mestranol. Am J Obstet Gynecol. 1990 Dec;163(6 Pt 2):2114-9.

    [4]. S Y Jiang, et al. Tamoxifen inhibits hepatoma cell growth through an estrogen receptor independent mechanism. J Hepatol. 1995 Dec;23(6):712-9.

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