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.
|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.
|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.|
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.
|Related GPR Products|
NIBR189 is a small molecule antagonist of the Epstein-Barr virus-induced gene 2 (EBI2; GPR183) receptor with IC50 of 16 nM(Binding) and 11 nM (Functional).
Latanoprost is a prostaglandin F2alpha analogue and a prostanoid selective FP receptor agonist with an ocular hypertensive effect. Latanoprost increases uveoscleral outflow and thereby reduces intraocular pressure.
GPR120-IN-1 is a selective Gpr120 agonist with a logEC50 of 7.62.
GSK137647A is a selective FFA4 agonist for human, Mouse and Rat FFA4 with pEC50 values of 6.3, 6.2 and 6.1, respectively.
PSN375963 is a potent and selective agonist of GPR119 that shows similar potency to oleoyl ethanolamide (OEA) at both recombinant mouse and human GPR119 receptors, exhibiting EC50 values of 8.4 and 7.9 µM, respectively (EC50 values for OEA are 3.2 and 2.9 µM, respectively).
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2017 AbMole BioScience. All Rights Reserved.