Document Detail

AMG 837: A potent, orally bioavailable GPR40 agonist.
MedLine Citation:
PMID:  22217876     Owner:  NLM     Status:  Publisher    
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.
Jonathan B Houze; Liusheng Zhu; Ying Sun; Michelle Akerman; Wei Qiu; Alex J Zhang; Rajiv Sharma; Michael Schmitt; Yingcai Wang; Jiwen Liu; Jinqian Liu; Julio C Medina; Jeff D Reagan; Jian Luo; George Tonn; Jane Zhang; Jenny Ying-Lin Lu; Michael Chen; Edwin Lopez; Kathy Nguyen; Li Yang; Liang Tang; Hui Tian; Steven J Shuttleworth; Daniel C-H Lin
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Publication Detail:
Type:  JOURNAL ARTICLE     Date:  2011-11-6
Journal Detail:
Title:  Bioorganic & medicinal chemistry letters     Volume:  -     ISSN:  1464-3405     ISO Abbreviation:  -     Publication Date:  2011 Nov 
Date Detail:
Created Date:  2012-1-5     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  9107377     Medline TA:  Bioorg Med Chem Lett     Country:  -    
Other Details:
Languages:  ENG     Pagination:  -     Citation Subset:  -    
Copyright Information:
Copyright © 2011 Elsevier Ltd. All rights reserved.
Amgen Inc. 1120 Veterans Blvd., South San Francisco, CA 94080, USA.
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