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Results for "amg837" in TargetMol Product Catalog
  • Inhibitor Products
    3
    TargetMol | Activity
(Rac)-AMG8379
T126551641574-26-6In house
(Rac)-AMG8379 ((Rac)-AMG8380) is a racemate of AMG8379 which is an orally active and selective sulfonamide NaV1.7 antagonist.
  • $195
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AMG8379
T10301L1642112-31-9
    Inquiry
    AMG 837
    T14216865231-46-5
    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.
    • $93
    35 days
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