1202575-57-2Relevant academic research and scientific papers
Optimization of 3-aryl-3-ethoxypropanoic acids and discovery of the potent GPR40 agonist DS-1558
Takano, Rieko,Yoshida, Masao,Inoue, Masahiro,Honda, Takeshi,Nakashima, Ryutaro,Matsumoto, Koji,Yano, Tatsuya,Ogata, Tsuneaki,Watanabe, Nobuaki,Hirouchi, Masakazu,Kimura, Takako,Toda, Narihiro
, p. 5546 - 5565 (2015/11/11)
GPR40 agonists stimulate insulin secretion only under the presence of high glucose concentration. Based on this mechanism, GPR40 agonists are believed to be promising novel insulin secretagogues with low risk of hypoglycemia. The optimizations of 3-aryl-3-ethoxypropanoic acids were performed to improve in vitro activity. We discovered compound 29r (DS-1558), (3S)-3-ethoxy-3-(4-{[(1R)-4-(trifluoromethyl)-2,3-dihydro-1H-inden-1-yl]oxy}phenyl)propanoic acid, which was confirmed to have an enhancing effect on glucose-dependent insulin secretion after intravenous glucose injection in SD rats.
Discovery of DS-1558: A potent and orally bioavailable GPR40 agonist
Takano, Rieko,Yoshida, Masao,Inoue, Masahiro,Honda, Takeshi,Nakashima, Ryutaro,Matsumoto, Koji,Yano, Tatsuya,Ogata, Tsuneaki,Watanabe, Nobuaki,Hirouchi, Masakazu,Yoneyama, Tomoko,Ito, Shuichiro,Toda, Narihiro
supporting information, p. 266 - 270 (2015/03/30)
GPR40 is a G protein-coupled receptor that is predominantly expressed in pancreatic β-cells. GPR40 agonists stimulate insulin secretion in the presence of high glucose concentration. On the basis of this mechanism, GPR40 agonists are possible novel insuli
CARBOXYLIC ACID COMPOUND
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Page/Page column 52, (2011/04/14)
To find a therapeutic agent and/or a preventive agent for diabetes mellitus or the like having excellent activity and safety. A compound represented by the following general formula (I), or a pharmacologically acceptable salt thereof. In the formula, X re
