Estradiol 3-sulfamate
Names
[ CAS No. ]:
172377-52-5
[ Name ]:
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]
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Chemical & Physical Properties
[ Molecular Formula ]:
C18H25NO4S
[ Molecular Weight ]:
351.46
[ Storage condition ]:
2-8℃