BAR-501

BAR-501 is a small molecule, UDCA derivative that acts as a highly selective agonist of the G protein-coupled bile acid receptor 1 (GPBAR1, also known as TGR5), with no detectable agonist activity at the farnesoid X receptor (FXR). The drug has demonstrated efficacy in preclinical models of primary sclerosing cholangitis (PSC), atherosclerosis, nonalcoholic fatty liver disease (NAFLD), and portal hypertension, where it shows anti-inflammatory, anti-fibrotic, and endothelial-protective effects. Mechanistically, BAR-501 targets GPBAR1 to modulate immune responses, reduce inflammation, shift macrophage phenotypes, enhance insulin sensitivity, and alter bile acid composition. Developed for conditions with significant hepatic and vascular inflammation, it has shown ability to downregulate pro-inflammatory gene expression, improve gut-liver axis integrity, and reduce fibrosis and cardiovascular disease risk. BAR-501 is typically studied in oral formulations in animal models, and is warranting evaluation in human PSC and related liver/inflammatory diseases[1][2][4][5][7].

Other names

BAR 501BAR501BAR-501Cholane-3,7,24-triol, 6-ethyl-, (3α,5β,6β,7β)-(3α,5β,6β,7β)-6-Ethylcholane-3,7,24-triol