Estradiol 3-sulfamate (BLE 00084; E2MATE; ES-J 995) 是一种长效和有口服活性的类固醇硫酸酯酶 (steroid sulfatase) 抑制剂；抑制雌酮硫酸酯酶的 IC50 值为251 nM，Ki 值为133 nM。
CAS：172377-52-5
分子式：C18H25NO4S
分子量：351.46
纯度：98%
存储：Store at -20°C

Background:

Estradiol 3-sulfamate (BLE 00084; E2MATE; ES-J 995) is a potent, long-acting, and orally active steroid sulfatase inhibitor; inhibits estrone sulfatase with an IC50 of 251 nM and a Ki of 133 nM. IC50: 251 nM (estrone sulfatase)[1]Ki: 133 nM (estrone sulfatase)[1]

Introduction of a fluoro, chloro, or bromo moiety at the C-2 position of EMATE and Estradiol 3-sulfamate and that of a fluoro moiety at the C-4 position of the parent sulfamates markedly increase the estrone sulfatase inhibitory activity[1].

Estradiol 3-sulfamate is readily transformed and absorbed in the gut into its oxidative metabolite, EMATE, and both compounds have already been shown to be potent, long-acting, and orally active STS inhibitors[2].

[1]. Numazawa M, et al. Inhibition of estrone sulfatase by aromatase inhibitor-based estrogen 3-sulfamates. Steroids. 2006 May;71(5):371-9. [2]. Pohl O, et al. Synergistic effects of E2MATE and norethindrone acetate on steroid sulfatase inhibition: a randomized phase I proof-of-principle clinical study in women of reproductive age. Reprod Sci. 2014 Oct;21(10):1256-65.