Estradiol 3-sulfamate |
| Catalog No.GC36010 |
에스트라디올 3-설파메이트(BLE 00084; E2MATE; ES-J 995)는 강력하고 오래 지속되는 경구 활성 스테로이드 설파타제 억제제입니다. 251 nM의 IC50 및 133 nM의 Ki로 에스트론 설파타제를 억제합니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 172377-52-5
Sample solution is provided at 25 µL, 10mM.
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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.
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