BMS-903452 is a potent and selective GRP119 agonist. BMS-903452 is efficacious in both acute and chronic in vivo rodent models of diabetes. Dosing of BMS-903452 in a single ascending dose study in normal healthy humans showed a dose dependent increase in exposure and a trend toward increased total GLP-1 plasma levels. G-protein-coupled receptor 119 (GPR119) is expressed predominantly in pancreatic β-cells and in enteroendocrine cells in the gastrointestinal tract. GPR119 agonists have been shown to stimulate glucose-dependent insulin release by direct action in the pancreas and to promote secretion of the incretin GLP-1 by action in the gastrointestinal tract. This dual mechanism of action has generated significant interest in the discovery of small molecule GPR119 agonists as a potential new treatment for type 2 diabetes.
MedKoo Cat#: 522370
Name: BMS-903452
CAS#: 1339944-47-6
Chemical Formula: C21H19Cl2FN4O4S
Exact Mass: 512.0488
Molecular Weight: 513.37
Elemental Analysis: C, 49.13; H, 3.73; Cl, 13.81; F, 3.70; N, 10.91; O, 12.47; S, 6.25
The following data is based on the product molecular weight 513.37 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 |
