|AMG837GPR40 agonist,orally bioavailable|
Sample solution is provided at 25 µL, 10mM.
Publications citing ApexBio Products
|Cas No.||865231-46-5||SDF||Download SDF|
|Chemical Name||(S)-3-(4-((4'-(trifluoromethyl)-[1,1'-biphenyl]-3-yl)methoxy)phenyl)hex-4-ynoic acid|
|Solubility||Soluble in DMSO||Storage||Store at -20°C|
AMG 837 is a potent and orally bioavailable GPR40 agonist (EC50=14nM). 
GPR40 is a G protein-coupled receptor that is activated by free fatty acid. It is located on the cell surface of pancreatic beta-cells, gastrointestinal enteroendocrine cells and immune cells etc. GPR40 is reported to be related the stimulation effects of fatty acids on insulin and incretin secretion. 
AMG 837 treatment on GPR40 containing cell membrane increases [35S]-GTPγ binding (EC=1.5±0.1 nM). AMG 837 also stimulates Ca2+ influx (EC50 = 13.5±0.8 nM) in CHO cells transfected with GPR40 and aequorin. 
The insulin secretion is stimulated and the postprandial glucose level is lowered in 8-week old Sprague-Dawley rats orally treated with AMG 837. In Zucker fatty rats treated with AMG 837 daily for 21-days shows decreased glucose excursions and elevated glucose stimulated insulin secretion in glucose tolerance tests. 
1. Houze JB, Zhu L, Sun Y et al. AMG 837: a potent, orally bioavailable GPR40 agonist. Bioorg Med Chem Lett. 2012 Jan 15;22(2):1267-70.
2. Lin DC, Zhang J, Zhuang R 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.