| AMG 837: A potent, orally bioavailable GPR40 agonist. | |
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MedLine Citation:
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PMID: 22217876 Owner: NLM Status: Publisher |
Abstract/OtherAbstract:
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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. |
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Authors:
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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:
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Type: JOURNAL ARTICLE Date: 2011-11-6 |
Journal Detail:
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Title: Bioorganic & medicinal chemistry letters Volume: - ISSN: 1464-3405 ISO Abbreviation: - Publication Date: 2011 Nov |
Date Detail:
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Created Date: 2012-1-5 Completed Date: - Revised Date: - |
Medline Journal Info:
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Nlm Unique ID: 9107377 Medline TA: Bioorg Med Chem Lett Country: - |
Other Details:
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Languages: ENG Pagination: - Citation Subset: - |
Copyright Information:
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Copyright © 2011 Elsevier Ltd. All rights reserved. |
Affiliation:
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Amgen Inc. 1120 Veterans Blvd., South San Francisco, CA 94080, USA. |
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From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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