172377-52-5

172377-52-5 structure

Name: Estradiol 3-sulfamate
Chemical Name: Estradiol 3-sulfamate
CAS Number: 172377-52-5
Molecular Formula: C₁₈H₂₅NO₄S
Molecular Weight: 351.46
Catalog: Research Areas Cancer
Create Date: 2018-03-15 12:06:37
Modify Date: 2024-01-08 12:57:02
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.

Name	Estradiol 3-sulfamate

Description	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.
Related Catalog	Signaling Pathways >> Others >> Others Research Areas >> Cancer
Target	IC50: 251 nM (estrone sulfatase)[1] Ki: 133 nM (estrone sulfatase)[1]
In Vitro	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].
In Vivo	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].
References	[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.