AMG 837: a potent, orally bioavailable GPR40 agonist.

  title={AMG 837: a potent, orally bioavailable GPR40 agonist.},
  author={Jonathan B. Houze and Liusheng Zhu and Ying Sun and Michelle Akerman and Wei Qiu and Alex J. Zhang and Rajiv P. Sharma and Michael J Schmitt and Yingcai Wang and Jiwen Liu and Jinqian Liu and Julio Alfonso Cruz Medina and Jeff D. Reagan and Jian Luo and George Tonn and Jane Tong Wen Zhang and Jenny Ying-Lin Lu and Michael Isaac Chen and Edwin S{\'a}nchez L{\'o}pez and Kathy Nguyen and Li Yang and Liang Tang and Hui Tian and Steven J Shuttleworth and Daniel C-H Lin},
  journal={Bioorganic & medicinal chemistry letters},
  volume={22 2},
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… CONTINUE READING
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