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Description: BMS-816336 is a potent and orally bioactive inhibitor of human 11beta-hydroxysteroid dehydrogenase type 1 (11beta-HSD1) enzyme with an IC50 of 3.0 nM. BMS-816336 showed activity against human 11beta-hydroxysteroid dehydrogenase type 1 (11beta-HSD1) enzyme (IC50 3.0 nM) with > 10000 fold selectivity over human 11beta-hydroxysteroid dehydrogenase type 2 (11beta-HSD2). BMS-816336 exhibits a robust acute pharmacodynamic effects in cynomolgus monkeys (ED50 0.13 mpk) and in DIO mice. BMS-816336 was found to be well-tolerated in Phase 1 clinical studies and represents a potential new treatment for type 2 diabetes, metabolic syndrome, and other human diseases modulated by glucocorticoid control.
References: J Med Chem. 2017 Jun 22; 60(12):4932-4948.
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