产品
编 号：F662358
分子式：C28H32N2O4
分子量：460.56
分子式：C28H32N2O4
分子量：460.56
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CAS No: 1114561-85-1
产品详情
生物活性：
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.
体内研究：
BI-135585 (compound 11j; 1-3 mg/kg; po) inhibits 67% and 90% of enzyme activity respectively in perirenal adipose tissue in cynomolgus monkey.
体外研究：
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 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.
体内研究：
BI-135585 (compound 11j; 1-3 mg/kg; po) inhibits 67% and 90% of enzyme activity respectively in perirenal adipose tissue in cynomolgus monkey.
体外研究：
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.
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