BMS-903452 (BMS 903452) is a potent and selective GPR119 agonist with EC50 of 14 nM.
BMS-903452 exhibits an excellent profile in our vitro safety assays, no significant inhibition (IC50 > 40 μM) at nine different cytochrome P450 enzymes, does not activate PXR (EC50>50 μM), and exhibits no toxicity in a hepatic (HEPG2) cell line.
BMS-903452 displays high selectivity against a panel of 95 GPCRs and enzymes in a broad receptor screening panel.
BMS-903452 significantly increased active GLP-1 levels in cannulated Sprague-Dawley rat model.
BMS-903452 exhibited synergistic effect when combined with DPPIV inhibitor.
BMS-903452 is efficacious in both acute and chronic in vivo rodent models of diabetes.
