<Suppliers Price>

AMG 837

Names

[ CAS No. ]:
865231-46-5

[ Name ]:
AMG 837

[Synonym ]:
amg-837
AMG 837

Biological Activity

[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 agonistAMG 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. showedno 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 potentand selective in vitro.

[Related Catalog]:

Signaling Pathways >> GPCR/G Protein >> GPR40
Research Areas >> Metabolic Disease

[References]

[1]. Houze JB, et al. AMG 837: a potent, orally bioavailable GPR40 agonist. Bioorg Med Chem Lett. 2012 Jan 15;22(2):1267-70.

[2]. Lin DC, et al. AMG 837: a novel GPR40/FFA1 agonist that enhances insulin secretion and lowers glucose levels in rodents. PLoS One. 2011;6(11):e27270.


[Related Small Molecules]

TAK-875 | GW-1100 | GW9508 | DC 260126 | PBI-4050 sodium salt | GPR40 Activator 2 | TUG-770 | AMG 837 (calcium hydrate) | FAA1 agonist-1 | GPR40 Activator 1 | AM-1638 | GPR40 Agonist 2

Chemical & Physical Properties

[ Molecular Formula ]:
C26H21F3O3

[ Molecular Weight ]:
438.43800

[ Exact Mass ]:
438.14400

[ PSA ]:
46.53000

[ LogP ]:
6.53300


Related Compounds