| Bioactivity | 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]. |
| Target | IC50: 13 nM (11β-HSD1) |
| Invitro | 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]. |
| In Vivo | 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]. |
| Name | BI-135585 |
| CAS | 1114561-85-1 |
| Formula | C28H32N2O4 |
| Molar Mass | 460.56 |
| 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]. 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. [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. |