1. GPCR/G Protein
  2. GPR40
  3. AMG 837

AMG 837 

Cat. No.: HY-13967
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AMG 837 is a potent GPR40 agonist(EC50=13 nM) with a superior pharmacokinetic profile and robust glucose-dependent stimulation of insulin secretion in rodents.

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AMG 837 Chemical Structure

AMG 837 Chemical Structure

CAS No. : 865231-46-5

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Description

AMG 837 is a potent GPR40 agonist(EC50=13 nM) with a superior pharmacokinetic profile and robust glucose-dependent stimulation of insulin secretion in rodents. IC50 value: 13 nM (EC50) [1] Target: GPR40 agonist AMG 837 displayed the expected two-fold increase in potency on GPR4 (EC50 = 13 [±7] nM) compared to the racemic compound and its activity crossed over to the rat and mouse forms of GPR40 (EC50 = 23 and 13 nM, respectively). AMG 837 was found to be a partial agonist on GPR40 with maximal activity 85% of that shown by DHA under our standard assay conditions. AMG 837 is a highly potent stimulator of insulin secretion in MIN6 cells with an EC50 comparable to that seen in the aequorin Ca2+-flux assay. showed no significant activity in cell-based assays against PPARα, δ, and γ. An external panel of 64 receptors also revealed no significant activity with the exception of weak inhibition (IC50 = 3 uM) on the a2-adrenergic receptor. Overall, AMG 837 was both highly potent and selective in vitro.

Molecular Weight

438.44

Formula

C₂₆H₂₁F₃O₃

CAS No.

865231-46-5

SMILES

OC(C[[email protected]](C#CC)C1=CC=C(C=C1)OCC2=CC=CC(C3=CC=C(C(F)(F)F)C=C3)=C2)=O

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Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

AMG 837AMG837AMG-837GPR40Free fatty acid receptor 1FFAR1FFA1G-protein-coupled receptor 40Inhibitorinhibitorinhibit

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AMG 837
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HY-13967
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