Mestranol

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Chemical Structure| 72-33-3 同义名 : EE 3-ME;Δ-MVE;Ethinyl Estradiol 3 Methyl Ether;Ovastol;Norquen;Devocin;SC-475;NSC 84032;Ethynyl Estradiol 3-methyl ether
CAS号 : 72-33-3
货号 : A923746
分子式 : C21H26O2
纯度 : 99%
分子量 : 310.43
MDL号 : MFCD00003689
存储条件：

Pure form Sealed in dry,2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 35 mg/mL(112.75 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 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[3]. When mestranol was tested in mice and rats (studies on dogs and monkeys are still in progress) orally in combination with a progestin, it produced pituitary tumors and vaginal and cervical squamous cell carcinomas. When used alone, mestranol, by the oral route, increased incidences of pituitary tumors in both sexes, mammary tumors in castrated males, and mammary tumors in females of another mouse species[4]. Pharmacokinetally, a 50 micrograms oral dose of mestranol (which itself is inactive) is bioequivalent to a 35 micrograms dose of ethinyl estradiol[5]. 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. 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[6].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00972439 Oral Contraceptive Not Applicable Completed - United States, California ... 展开 >> Los Angeles County Hospital Los Angeles, California, United States, 90033 收起 <<
NCT00504816 Type 2 Diabetes Mellitus ... 展开 >> Diabetes Mellitus, Type 2 收起 << Phase 1 Completed - United States, Florida ... 展开 >> GSK Investigational Site Miramar, Florida, United States, 33025 收起 <<
NCT00972439 - Completed - -
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.22mL

0.64mL

0.32mL

16.11mL

3.22mL

1.61mL

32.21mL

6.44mL

3.22mL
参考文献

[1]Dragan YP, Singh J, et al. Effect of the separate and combined administration of mestranol and phenobarbital on the development of altered hepatic foci expressing placental form of glutathione S-transferase in the rat. Carcinogenesis. 1996 Sep;17(9):2043-52.

[2]Shackelford DP Jr, McConnaughey MM, et al. The effects of estradiol and mestranol on alpha-adrenoceptors in select regions of the rat brain. Brain Res Bull. 1988 Aug;21(2):329-33.

[3]Kappus H, Bolt HM, Remmer H. 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

[4]Mestranol. IARC Monogr Eval Carcinog Risk Chem Hum. 1979 Dec;21:257-78

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

[6]Jiang SY, Shyu RY, Yeh MY, Jordan VC. Tamoxifen inhibits hepatoma cell growth through an estrogen receptor independent mechanism. J Hepatol. 1995 Dec;23(6):712-9