Document Detail


AMG 837: A potent, orally bioavailable GPR40 agonist.
MedLine Citation:
PMID:  22217876     Owner:  NLM     Status:  Publisher    
Abstract/OtherAbstract:
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.
Authors:
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.
Affiliation:
Amgen Inc. 1120 Veterans Blvd., South San Francisco, CA 94080, USA.
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