BI 135585

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

BI 135585 (BI-135585, BI135585) 是一种有效的、选择性的、口服活性的 11β-HSD1 抑制剂，在人脂肪细胞和原代人脂肪组织中的 IC50 分别为 4.3 nM 和 53 nM。

BI 135585 (BI-135585, BI135585) is a potent, selective, orally active 11β-HSD1 inhibitor with IC50 of 4.3 nM and 53 nM in human adipocytes and primary human adipose tissue, respectively; exhibits >1,000-fold selectivity over other hydroxysteroid dehydrogenases; inhibits 11β HSD1 activity in adipose tissue, displays desirable pharmacodynamic properties in vivo.Diabetes Phase 1 Clinical.

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.In human adipose tissue ex vivo, BI-135585 inhibits the conversion of cortisone to cortisol with an average IC50 of 11 nM. 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.

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

BI-135585 | BI135585

Metabolic Enzyme/Protease

11β-HSD

11β-HSD

Metabolic Disease

Diabetes

1114561-85-1

460.574

C28H32N2O4

>98% (HPLC)

——

O=C1O[C@](C2=CC=CC=C2)(CC(C)(O)C)CCN1[C@H](C3=CC=C(C(C=CN4C)=CC4=O)C=C3)C

(S)-6-(2-hydroxy-2-methylpropyl)-3-((S)-1-(4-(1-methyl-2-oxo-1,2-dihydropyridin-4-yl)phenyl)ethyl)-6-phenyl-1,3-oxazinan-2-one

(-20℃)

With Ice Pack

≥ 2 years