AMG 837

• Catalog Number: orb1707666
• Category: Small Molecules
• Description: AMG 837
• CAS Number: 865231-46-5
• Purity: 98%
• MW: 438.44
• SMILES: C(OC1=CC=C([C@H](CC(O)=O)C#CC)C=C1)C=2C=C(C=CC2)C3=CC=C(C(F)(F)F)C=C3
• Formula: C₂₆H₂₁F₃O₃
• Biological Activity: AMG 837 is a partial GPR40 agonist with an EC50 value of 13 nM, showcasing 85% of the maximal activity displayed by DHA in standard assay conditions, indicating its high potency and selectivity in vitro. This compound excels as a GPR40 agonist with a notable pharmacokinetic profile, effectively stimulating insulin secretion in a glucose-dependent manner in rodents and demonstrating potent insulin secretion stimulation in MIN6 cells, with efficacy comparable to that observed in aequorin Ca2+-flux assays. Moreover, AMG 837 exhibits a two-fold increase in potency compared to its racemic counterpart on GPR40, with demonstrated activity across rat and mouse GPR40 versions (EC50 = 23 and 13 nM, respectively). It lacks significant activity against PPARα, δ, and γ in cell-based assays, and an analysis against an external panel of 64 receptors revealed negligible activity, except for a weak inhibition (IC50 = 3 μM) on the a2-adrenergic receptor.
• Note: For research use only
• Expiration Date: 12 months from date of receipt.