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MBX-2982 is a potent selective orally-active GPR119 agonist that functions through a unique dual mechanism of action. First, it acts directly on the beta cell to increase insulin secretion. In addition, MBX-2982 stimulates release of the incretin GLP-1 from the gut. Treatment with MBX-2982 increased insulin, active GLP-1, and total GLP-1 during an extended MMTT. Treatment with MBX-2982 also tended to increase fasting insulin and c-peptide, and decrease fasting triglycerides. MBX-2982 is a potential first-in-class treatment for type 2 diabetes that targets G protein-coupled receptor 119 (GPR119), a receptor that interacts with bioactive lipids known to stimulate glucose-dependent insulin secretion.
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Source | Eur J Pharmacol (2015). Figure 5. MBX-2982 |
| Method | Examining the longevity of wash-resistant cAMP responses to GPR119 agonists | |
| Cell Lines | HEK-GPR119 cells. | |
| Concentrations | 30 nM | |
| Incubation Time | 60 min | |
| Results | These data are consistent with a requirement for membrane deposition in the sustained wash-resistant effects for MBX-2982 and AZ1, but not AR-231, 453. |
| Molecular Weight | 448.54 |
| Formula | C22H24N8OS |
| CAS Number | 1037792-44-1 |
| Solubility (25°C) | DMSO ≥ 10 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
[2] Jones RM, et al. Expert Opin Ther Pat. GPR119 agonists for the treatment of type 2 diabetes.
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