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10.1021/ml1000855 http://scihub22266oqcxt.onion/10.1021/ml1000855 C4007909!4007909!24900210     free     free     free Deprecated: Implicit conversion from float 233.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 233.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 233.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534       ACS+Med+Chem+Lett 2010 ; 1 (6): 290-4 Nephropedia Template TP {{tp|p=24900210|t=2010. Discovery of TAK-875: A Potent, Selective, and Orally Bioavailable GPR40 Agonist |pdf=|usr=}}{{24900210}} gab.com Text Discovery of TAK-875: A Potent, Selective, and Orally Bioavailable GPR40 Agonist JO: ACS Med Chem Lett http://www.kidney.de/pget.php?&tw=1&pmid=24900210 #FOAvip GPR40, one of the G protein-coupled receptors predominantly expressed in pancreatic ?-cells, mediates enhancement of glucose-stimulated insulin secretion by free fatty acids. A potent and selective GPR40 agonist is theorized to be a safe and effective antidiabetic drug with little or no risk of hypoglycemia. Cyclization of the phenylpropanoic acid moiety of lead compound 1 produced fused phenylalkanoic acids with favorable in vitro agonist activities and pharmacokinetic profiles. Further optimization led to the discovery of dihydrobenzofuran derivative 9a ([(3S)-6-({2?,6?-dimethyl-4?-[3-(methylsulfonyl)propoxy]biphenyl-3-yl}methoxy)-2, 3-dihydro-1-benzofuran-3-yl]acetic acid hemi-hydrate, TAK-875) as a potent, selective, and orally bioavailable GPR40 agonist, with a pharmacokinetic profile enabling long-acting drug efficacy. Compound 9a showed potent plasma glucose-lowering action and insulinotropic action during an oral glucose tolerance test in female Wistar fatty rats with impaired glucose tolerance. Compound 9a is currently in clinical trials for the treatment of type 2 diabetes mellitus. Twit Text FOAVip Discovery of TAK-875: A Potent, Selective, and Orally Bioavailable GPR40 Agonist ????ACS Med Chem Lett http://www.kidney.de/pget.php?&tw=1&pmid=24900210 #FOAvip Twit Text # Free Paper on # # # # # LINK http://www.kidney.de/pget.php?&tw=1&pmid=24900210 #FOAvip English Wikipedia <ref>{{Cite pmid|24900210}}</ref> Discovery of TAK-875: A Potent, Selective, and Orally Bioavailable GPR40 Agonist #MMPMID24900210 Negoro N; Sasaki S; Mikami S; Ito M; Suzuki M; Tsujihata Y; Ito R; Harada A; Takeuchi K; Suzuki N; Miyazaki J; Santou T; Odani T; Kanzaki N; Funami M; Tanaka T; Kogame A; Matsunaga S; Yasuma T; Momose Y ACS Med Chem Lett 2010[Sep]; 1 (6): 290-4 PMID24900210show ga GPR40, one of the G protein-coupled receptors predominantly expressed in pancreatic ?-cells, mediates enhancement of glucose-stimulated insulin secretion by free fatty acids. A potent and selective GPR40 agonist is theorized to be a safe and effective antidiabetic drug with little or no risk of hypoglycemia. Cyclization of the phenylpropanoic acid moiety of lead compound 1 produced fused phenylalkanoic acids with favorable in vitro agonist activities and pharmacokinetic profiles. Further optimization led to the discovery of dihydrobenzofuran derivative 9a ([(3S)-6-({2?,6?-dimethyl-4?-[3-(methylsulfonyl)propoxy]biphenyl-3-yl}methoxy)-2, 3-dihydro-1-benzofuran-3-yl]acetic acid hemi-hydrate, TAK-875) as a potent, selective, and orally bioavailable GPR40 agonist, with a pharmacokinetic profile enabling long-acting drug efficacy. Compound 9a showed potent plasma glucose-lowering action and insulinotropic action during an oral glucose tolerance test in female Wistar fatty rats with impaired glucose tolerance. Compound 9a is currently in clinical trials for the treatment of type 2 diabetes mellitus. äDiscovery of TAK-875: A Potent, Selective, and Orally Bioavailable GPR(epmc).pdf DeepDyve Pubget Overpricing