3R,5S,6S,7S,8S,9S,10S,13R,14S,17R)-6-ethyl-17-((R)-5-hydroxypentan-2-yl)-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthrene-3,7-diol BAR-501
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BAR-501, a UDCA derivative, is a selective GPBAR1 agonist devoid of any FXR agonistic activity. BAR-501 effectively transactivates GPBAR1 in HEK293 cells overexpressing a CRE along with GPBAR1, with a EC50 of 1 μM. Besides, it protects against development of portal hypertension in rodent models of liver injury and endothelial dysfunction.
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