BMS-816336 represents a potential new treatment for type 2 diabetes, metabolic syndrome, and other human diseases modulated by glucocorticoid control. BMS-816336 (6n-2) exhibits a robust acute pharmacodynamic effect in cynomolgus monkeys (ED50=0.12 mg/kg) and in DIO mice (1, 3, 10, 30, 100 mg/kg, 120 mintues). It is orally bioavailable (%F ranges from 20 to 72% in preclinical species) and has a predicted pharmacokinetic profile of a high peak to trough ratio and short half-life in humans.
| Animal Model: |
Nonfasting diet-induced obese male mice |
| Dosage: |
1, 3, 10, 30, 100 mg/kg |
| Administration: |
Oral, 120 mintues |
| Result: |
ED50=8.6 mg/kg and a plasma EC50 of 0.85 μM in this model. |