FXR agonist 18 is an orally active FXR agonist, with an EC 50 of 10 nM against human FXR and an EC 50 of 1360 nM against human TGR5 . FXR agonist 18 inhibits inflammatory responses by reducing nitrite production, downregulating the expression of pro-inflammatory genes ( Tnf , Adgre1 , Cyp8b1 , upregulating the expression of FXR , Hmox1 , Nqo1 , Nrf2 , and enhancing antioxidant responses. FXR agonist 18 ameliorates liver fibrosis in mice, exhibits protective effects in mice with cholestatic liver injury, and shows anti-MASH efficacy. FXR agonist 18 can be used in studies of metabolic dysfunction-associated steatohepatitis.
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