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BMS-986118 

Cat. No. M28672
BMS-986118  Structure
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Quality Control & Documentation
Biological Activity

BMS-986118 is a potent, orally active, and selective GPR40 agonist with an EC50 of 0.07 µM. BMS-986118 has dual insulinotropic and GLP-1 secretory effects, resulting in robust plasma glucose lowering effects in acute animal models.

Chemical Information
Molecular Weight 540.96
Formula C25H28ClF3N4O4
CAS Number 1610562-74-7
Storage Please store the product under the recommended conditions in the Certificate of Analysis.
Conversion of different model animals based on BSA (PMID: 27057123)
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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.

References

[1] Jun Shi, et al. J Med Chem. Discovery of Potent and Orally Bioavailable Dihydropyrazole GPR40 Agonists

[2] Zheng Li, et al. Expert Opin Investig Drugs. Free fatty acid receptor agonists for the treatment of type 2 diabetes: drugs in preclinical to phase II clinical development

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  Catalog
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Keywords: BMS-986118  supplier, GPR/FFAR, inhibitors, activators


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