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Bioorg Med Chem Lett. 2012 Jan 15;22(2):1267-70. doi: 10.1016/j.bmcl.2011.10.118. Epub 2011 Nov 6.

AMG 837: a potent, orally bioavailable GPR40 agonist.

Author information

1
Amgen Inc. 1120 Veterans Blvd., South San Francisco, CA 94080, USA. jhouze@amgen.com

Abstract

The discovery that certain long chain fatty acids potentiate glucose stimulated insulin secretion through the previously orphan receptor GPR40 sparked interest in GPR40 agonists as potential antidiabetic agents. Optimization of a series of β-substituted phenylpropanoic acids led to the identification of (S)-3-(4-((4'-(trifluoromethyl)biphenyl-3-yl)methoxy)phenyl)hex-4-ynoic acid (AMG 837) as a potent GPR40 agonist with a superior pharmacokinetic profile and robust glucose-dependent stimulation of insulin secretion in rodents.

PMID:
22217876
DOI:
10.1016/j.bmcl.2011.10.118
[Indexed for MEDLINE]

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