Name: (S)-3-(4-Hydroxyphenyl)hex-4-ynoic acidOn October 31, 2012 ,《A potent class of GPR40 full agonists engages the enteroinsular axis to promote glucose control in rodents》 appeared in PLoS One. The author of the article were Luo, Jian; Swaminath, Gayathri; Brown, Sean P.; Zhang, Jane; Guo, Qi; Chen, Michael; Nguyen, Kathy; Tran, Thanhvien; Miao, Lynn; Dransfield, Paul J.; Vimolratana, Marc; Houze, Jonathan B.; Wong, Simon; Toteva, Maria; Shan, Bei; Li, Frank; Zhuang, Run; Lin, Daniel C.-H.. The article conveys some information:
Type 2 diabetes is characterized by impaired glucose homeostasis due to defects in insulin secretion, insulin resistance and the incretin response. GPR40 (FFAR1 or FFA1) is a G-protein-coupled receptor (GPCR), primarily expressed in insulin-producing pancreatic β-cells and incretin-producing enteroendocrine cells of the small intestine. Several GPR40 agonists, including AMG 837 and TAK-875, have been disclosed, but no GPR40 synthetic agonists have been reported that engage both the insulinogenic and incretinogenic axes. In this report we provide a mol. explanation and describe the discovery of a unique and potent class of GPR40 full agonists that engages the enteroinsular axis to promote dramatic improvement in glucose control in rodents. GPR40 full agonists AM-1638 and AM-6226 stimulate GLP-1 and GIP secretion from intestinal enteroendocrine cells and increase GSIS from pancreatic islets, leading to enhanced glucose control in the high fat fed, streptozotocin treated and NONcNZO10/LtJ mouse models of type 2 diabetes. The improvement in hyperglycemia by AM-1638 was reduced in the presence of the GLP-1 receptor antagonist Ex(9-39)NH2. After reading the article, we found that the author used (S)-3-(4-Hydroxyphenyl)hex-4-ynoic acid(cas: 865233-35-8Name: (S)-3-(4-Hydroxyphenyl)hex-4-ynoic acid)
(S)-3-(4-Hydroxyphenyl)hex-4-ynoic acid(cas: 865233-35-8) belongs to alkynes. The addition of nonpolar E−H bonds across C≡C is general for silanes, boranes, and related hydrides. The hydroboration of alkynes gives vinylic boranes which oxidize to the corresponding aldehyde or ketone. In the thiol-yne reaction the substrate is a thiol.Name: (S)-3-(4-Hydroxyphenyl)hex-4-ynoic acid
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