Estradiol 3-sulfamate( —— )

Catalog No. M32917 CAS No. 172377-52-5

COA

Datasheet

HNMR

HPLC

MSDS

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Product Name

Estradiol 3-sulfamate
Note

Research use only, not for human use.
Brief Description

Estradiol 3-sulfamate (BLE 00084) is an orally active and highly potent steroidal estrone sulfatase (ES) inhibitor.
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.
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.
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.
Synonyms

——
Pathway

Endocrinology/Hormones
Target

Estrogen Receptor/ERR
Recptor

Estrogen Receptor/ERR
Research Area

——
Indication

——

CAS Number

172377-52-5
Formula Weight

351.46
Molecular Formula

C18H25NO4S
Purity

>98% (HPLC)
Solubility

In Vitro:?DMSO : 62.5 mg/mL (177.83 mM; Ultrasonic )
SMILES

[H][C@@]12CC[C@H](O)[C@@]1(C)CC[C@]1([H])c3ccc(OS(N)(=O)=O)cc3CC[C@@]21[H]
Chemical Name

——

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

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