BMS-816336 is an orally active, potent and selective 11β-HSD1 inhibitor. BMS-816336 showed activity against human 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) enzyme (IC50 3.0 nM) with >10000 fold selectivity over human 11β-hydroxysteroid dehydrogenase type 2 (11β-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.
MedKoo Cat#: 530652
Name: BMS-816336
CAS#: 1009583-20-3
Chemical Formula: C21H27NO3
Exact Mass: 341.1991
Molecular Weight: 341.45
Elemental Analysis: C, 73.87; H, 7.97; N, 4.10; O, 14.06
The following data is based on the product molecular weight 341.45 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
