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Synonyms: 6α-ethyl-23(S)-methyl-cholic acid | INT-777 | INT777
Compound class: Synthetic organic
Comment: S-EMCA (INT-777) is a potent and selective agonist of the G-protein-coupled bile acid receptor TGR5 (gene symbol GPBAR1) which is formally known as the GPBA receptor . The GPBA receptor was historically identified as a metabolic regulator with roles in energy homeostasis, bile acid homeostasis, and glucose metabolism. More recently additional functions for the GPBA receptor such as regulation of the inflammatory response, cancer and liver regeneration have been described .
Ligand Activity Visualisation Charts
These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts.✖
1. Guo C, Chen WD, Wang YD. (2016)
TGR5, Not Only a Metabolic Regulator.
Front Physiol, 7: 646. [PMID:28082913]
2. Li B, Yang N, Li C, Li C, Gao K, Xie X, Dong X, Yang J, Yang Q, Tong Z et al.. (2018)
INT-777, a bile acid receptor agonist, extenuates pancreatic acinar cells necrosis in a mouse model of acute pancreatitis.
Biochem Biophys Res Commun, 503 (1): 38-44. [PMID:29859191]
3. Pellicciari R, Gioiello A, Macchiarulo A, Thomas C, Rosatelli E, Natalini B, Sardella R, Pruzanski M, Roda A, Pastorini E et al.. (2009)
Discovery of 6alpha-ethyl-23(S)-methylcholic acid (S-EMCA, INT-777) as a potent and selective agonist for the TGR5 receptor, a novel target for diabesity.
J Med Chem, 52 (24): 7958-61. [PMID:20014870]