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MBX-2982

Cat. No. M3632

MBX-2982 Structure
Size Price Availability Quantity
5mg USD 160 In stock
10mg USD 300 In stock
50mg USD 960 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.

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
References

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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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: MBX-2982 supplier, GPR, inhibitors

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