AMG 837: a potent, orally bioavailable GPR40 agonist.
作者： Jonathan B Houze , Liusheng Zhu , Ying Sun , Michelle Akerman , Wei Qiu
DOI: 10.1016/J.BMCL.2011.10.118
关键词:
摘要: The discovery that certain long chain fatty acids potentiate glucose stimulated insulin secretion through the previously orphan receptor GPR40 sparked interest in agonists as potential antidiabetic agents. Optimization of a series β-substituted phenylpropanoic led to identification (S)-3-(4-((4'-(trifluoromethyl)biphenyl-3-yl)methoxy)phenyl)hex-4-ynoic acid (AMG 837) potent agonist with superior pharmacokinetic profile and robust glucose-dependent stimulation rodents.
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