| Bioactivity | 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]. | ||||||||||||
| Invitro | 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]. | ||||||||||||
| Name | Mestranol | ||||||||||||
| CAS | 72-33-3 | ||||||||||||
| Formula | C21H26O2 | ||||||||||||
| Molar Mass | 310.43 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [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. |