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Cat. No. M3632
MBX-2982 Structure
Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
5mg USD 160 In stock
10mg USD 280 In stock
50mg USD 850 In stock
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Quality Control
Biological Activity

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.

Customer Product Validations & Biological Datas
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.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
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.

Chemical Information
Molecular Weight 448.54
Formula C22H24N8OS
CAS Number 1037792-44-1
Purity >99%
Solubility DMSO
Storage at -20°C

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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Keywords: MBX-2982 supplier, GPR, inhibitors

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