Estradiol 3-sulfamate

SKU: orb1709735

Description

Estradiol 3-sulfamate (BLE 00084) is a potent, orally bioavailable inhibitor of estrone sulfatase (ES), exhibiting a K(i) of 73 nM in human placental microsomes. Its application is primarily in breast cancer research, where it is used to study ES inhibition in both in vitro enzymatic assays and in vivo models of hormone-dependent tumors.

Research Area

Metabolism Research, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 172377-52-5
• MW: 351.46
• Purity: 99.63% (May vary between batches)
• Formula: C₁₈H₂₅NO₄S
• SMILES: [H][C@@]12CC[C@H](O)[C@@]1(C)CC[C@]1([H])c3ccc(OS(N)(=O)=O)cc3CC[C@@]21[H]
• Target: Others,Estrogen Receptor/ERR
• Solubility: DMSO:50 mg/mL (142.26 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (5.69 mM)

Bioactivity

• Target IC50:
  estrone sulfatase:251 nM|estrone sulfatase:133 nM(Ki)
• In Vivo:
  Estradiol 3-sulfamate readily transforms into its metabolite EMATE in the gut, making it a more effective STS inhibitor.
• In Vitro:
  Compared to the lead compound EMATE, Estradiol 3-sulfamate exhibits superior inhibitory activity against estrone sulfatase.

Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

E2MATE, BLE 00084, BLE00084, BLE-00084, Estrogen Receptor, estrogen receptor, estrone sulfatase, EstrogenReceptor, ES-J 995, ES-J995, ES-J-995, Estradiol 3 sulfamate, Estradiol 3sulfamate, Estradiol 3-sulfamate, ERR

Compound Identifiers

PubChem CID

6918339