Estradiol 3-sulfamate, Inhibitor

Estradiol 3-sulfamate

Cat. Num. AAA5753112

• Purity: 98.00%
• Synonyms: Estradiol 3-sulfamate; BLE 00084; E2MATE; ES-J 995; inhibitor

• Purity/Purification: 98.00%
• Form/Format: Solid. Powder

• Solubility: DMSO: 62.5mg/mL (177.83mM) Need ultrasonic; (<1mg/ml refers to the product slightly soluble or insoluble)
• Formula: C18H25NO4S
• SMILES: C[C@@]1([C@H]2O)[C@](CC2)([H])[C@@](CCC3=C4C=CC(OS(N)(=O)=O)=C3)([H])[C@]4([H])CC1
• CAS Number: 172377-52-5
• Target & IC50: estrone sulfatase: ic50 251nM
• In Vitro: 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.
• Preparation and Storage: Store at -20 degree C for 3 years powder; -80 degree C for 2 years in solvent

Structure

Related Product Information for Estradiol 3-sulfamate, inhibitor

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

References

Numazawa M, et al. Inhibition of estrone sulfatase by aromatase inhibitor-based estrogen 3-sulfamates. Steroids. 2006 May;71(5):371-9.
Numazawa M, et al. Inhibition of estrone sulfatase by aromatase inhibitor-based estrogen 3-sulfamates. Steroids. 2006 May;71(5):371-9.
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.
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.