Estradiol 3-sulfamate

Modify Date: 2025-08-24 20:45:47

Estradiol 3-sulfamate Structure
Estradiol 3-sulfamate structure
Common Name Estradiol 3-sulfamate
CAS Number 172377-52-5 Molecular Weight 351.46
Density N/A Boiling Point N/A
Molecular Formula C18H25NO4S Melting Point N/A
MSDS N/A Flash Point N/A

 Use of Estradiol 3-sulfamate


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.

 Names

Name Estradiol 3-sulfamate

 Estradiol 3-sulfamate Biological Activity

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
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.

 Chemical & Physical Properties

Molecular Formula C18H25NO4S
Molecular Weight 351.46
Storage condition 2-8℃
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