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Steroid sulfatase/17β-HSD1-IN-5

CAS: F: C21H22N2O6S W: 430.47

Steroid sulfatase/17β-HSD1-IN-5 is a irreversible inhibitor of steroid sulfatase (STS) .Steroid sulfatase/17β-HSD1-IN-
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Bioactivity Steroid sulfatase/17β-HSD1-IN-5 is a irreversible inhibitor of steroid sulfatase (STS) .Steroid sulfatase/17β-HSD1-IN-5 is a reversible and selective inhibitor of 7β-hydroxysteroid dehydrogenase type1 (17β-HSD1), with IC50s of 43 nM and 6.2μM for 17β-HSD1 and 17β-HSD2, respectively. Steroid sulfatase/17β-HSD1-IN-5 can be used for metabolic disease (especially for endometriosis) research[1].
Target IC50: 43 nM (17β-HSD 1)IC50: 6.3 μM (17β-HSD 2)IC50: 0.4 μM (Steroid sulfatase)
Invitro Steroid sulfatase/17β-HSD1-IN-5 (Compound 5) (0-40 μM;48-72 小时) 在浓度高达 31 μM (HEK293) 和 23 μM (HepG2)时,对细胞活力没有影响[1]。 Cell Viability Assay[1] Cell Line:
In Vivo Steroid sulfatase/17β-HSD1-IN-5 (Compound 5) (皮下注射,50 mg/kg,单次给药) 显示 T1/2 为 3.82 小时,和 Cmax obs 为 2824 nM[1]。 Animal Model:
Name Steroid sulfatase/17β-HSD1-IN-5
Formula C21H22N2O6S
Molar Mass 430.47
Transport Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Reference [1]. Mohamed Salah, et.al. Potent Dual Inhibitors of Steroid Sulfatase and 17β-Hydroxysteroid Dehydrogenase Type 1 with a Suitable Pharmacokinetic Profile for In Vivo Proof-of-Principle Studies in an Endometriosis Mouse Model.Journal of Medicinal Chemistry 2023 66 (13), 8975-8992.