BI-135585 

BI-135585 is a potent, selective and orally active 11β-hydroxysteroid dehydrogenase 1 (11β-HSD1) inhibitor with an IC₅₀ of 13 nM. BI-135585 exhibits >1000-fold selectivity over other hydroxysteroid dehydrogenases. BI-135585 can be used for type 2 diabetes research^[1][2].

IC50: 13 nM (11β-HSD1)^[1]

BI-135585 binds in the substrate binding pocket of the active site of 11β-HSD1. Cellular activity of BI-135585 is examined by determining inhibition of 11β-HSD1 activity in human preadipocytes, the average IC₅₀ is 1 nM^[1].
In human adipose tissue ex vivo, BI-135585 inhibits the conversion of cortisone to cortisol with an average IC₅₀ of 11 nM^[1].
Abdominal subcutaneous and perirenal adipose tissue was harvested from one, male cynomolgus monkey. BI-135585 (20 hours) reduces enzyme activity in a dose-dependent manner with an IC50 of ~10 nM in perirenal adipose tissue and an IC50 of ~100 nM in abdominal subcutaneous adipose tissue^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

BI-135585 (compound 11j; 1-3 mg/kg; po) inhibits 67% and 90% of enzyme activity respectively in perirenal adipose tissue in cynomolgus monkey^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

460.56

C₂₈H₃₂N₂O₄

1114561-85-1

CC(C)(O)C[C@@]1(C2=CC=CC=C2)OC(N(CC1)[C@H](C3=CC=C(C4=CC(N(C=C4)C)=O)C=C3)C)=O

Room temperature in continental US; may vary elsewhere.

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

• [1]. Bradford S Hamilton, et al. Pharmacological characterization of the selective 11β-hydroxysteroid dehydrogenase 1 inhibitor, BI 135585, a clinical candidate for the treatment of type 2 diabetes. Eur J Pharmacol. 2015 Jan 5;746:50-5.  [Content Brief]

  [2]. Linghang Zhuang, et al. Discovery of BI 135585, an in vivo efficacious oxazinanone-based 11β hydroxysteroid dehydrogenase type 1 inhibitor. Bioorg Med Chem. 2017 Jul 15;25(14):3649-3657.  [Content Brief]