Journal
ACS MEDICINAL CHEMISTRY LETTERS
Volume 7, Issue 1, Pages 51-55Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acsmedchemlett.5b00323
Keywords
TGR5; TGR5 agonist; GPR 131; GPBAR1; GLP1 secretion; diabetes
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TGR5 is a G protein -coupled receptor (GPCR), activation of which promotes secretion of glucagon-like peptide -1 (GLP-1) and modulates insulin secretion. The 2-thio-imidazole derivative 6g was identified as a novel, potent, and selective TGR5 agonist (hTGR5 EC50 = 57 pM, mTGR5 = 62 pM) with a favorable pharmacokinetic profile. The compound 6g was found to have potent glucose lowering effects in vivo during an oral glucose tolerance test in DIO C57 mice with ED50 of 7.9 mg/kg and ED90 of 29.2 mg/ kg.
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