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LY2881835 

Cat. No. M28122
LY2881835  Structure
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Biological Activity

LY2881835 is a potent and selective agonist of G protein-coupled receptor 40 (GPR40). LY2881835 has efficacious and durable dose-dependent reductions in glucose levels along with significant increases in insulin and GLP-1 secretion. LY2881835 has the potential for the research of type 2 diabetes mellitus.

Chemical Information
Molecular Weight 491.62
Formula C33H33NO3
CAS Number 1292290-38-0
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] Tingting Chen, et al. Eur J Med Chem. Design, synthesis and structure-activity relationship studies of GPR40 agonists containing amide linker

[2] Yanyun Chen, et al. Pharmacol Res Perspect. A selective GPR40 (FFAR1) agonist LY2881835 provides immediate and durable glucose control in rodent models of type 2 diabetes

[3] Mikhail Krasavin, et al. Eur J Med Chem. Polar aromatic periphery increases agonist potency of spirocyclic free fatty acid receptor (GPR40) agonists inspired by LY2881835

[4] Chafiq Hamdouchi, et al. J Med Chem. The Discovery, Preclinical, and Early Clinical Development of Potent and Selective GPR40 Agonists for the Treatment of Type 2 Diabetes Mellitus (LY2881835, LY2922083, and LY2922470)

[5] Mikhail Krasavin, et al. Bioorg Med Chem. Free fatty acid receptor 1 (GPR40) agonists containing spirocyclic periphery inspired by LY2881835

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Keywords: LY2881835  supplier, GPR/FFAR, inhibitors, activators


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