.Estradiol 3-sulfamate inhibits estrone sulfatase with an IC50 of 251 nM and a Ki of 133 nM. Estradiol 3-sulfamate is a potent, long-acting, and orally active steroid sulfatase inhibitor.

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.

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.

172377-52-5

C18H25NO4S

351.46

雌二醇 3-氨基磺酸;E2MATE;BLE 00084;ES-J 995;Estradiol 3-sulfamate

DMSO:62.5 mg/mL (177.83 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years