Estradiol 3-sulfamate |
| Katalog-Nr.GC36010 |
Estradiol-3-sulfamat (BLE 00084; E2MATE; ES-J 995) ist ein potenter, lang wirkender und oral aktiver Steroidsulfatase-Hemmer; hemmt Östronsulfatase mit einem IC50 von 251 nM und einem Ki von 133 nM.
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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