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.
|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.|
|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.|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
32nd National Medicinal Chemistry Symposium--medicinal chemistry developments for neurodegeneration, diabetes and cancer.
Gater D. IDrugs. 2010 Aug;13(8):514-6. PMID: 20721817.
GPR119 agonists for the treatment of type 2 diabetes.
Jones RM, et al. Expert Opin Ther Pat. 2009 Oct;19(10):1339-59. PMID: 19780700.
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