Agarwal, Sameer published the artcileDiscovery of a Potent and Orally Efficacious TGR5 Receptor Agonist, SDS of cas: 23351-09-9, the publication is ACS Medicinal Chemistry Letters (2016), 7(1), 51-55, database is CAplus and MEDLINE.
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.
ACS Medicinal Chemistry Letters published new progress about 23351-09-9. 23351-09-9 belongs to alcohols-buliding-blocks, auxiliary class Pyrrole,Benzene,Alcohol, name is 4-(1H-Pyrrol-1-yl)phenol, and the molecular formula is C10H9NO, SDS of cas: 23351-09-9.
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