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ID: ALA4052684

Journal: Bioorg Med Chem Lett

Title: A novel intestinal-restricted FXR agonist.

Authors: Wang H, Zhao Z, Zhou J, Guo Y, Wang G, Hao H, Xu X.

Abstract: In this study, a new intestinal-restricted FXR agonist named fexaramine-3 (Fex-3) was developed and investigated both in vitro and in vivo. Fex-3 could selectively activate intestinal FXR and promote the expression of BSEP and SHP while suppressing CYP7A1 which is involved in bile acids syntheses better than the reported intestinal-restricted FXR agonist fexaramine (Fex). We demonstrated that Fex-3 targeted on FXR in ileum and has better selectivity than Fex. And the study of utilizing Fex-3 to reduce obesity was undergoing.

CiteXplore: 28629595

DOI: 10.1016/j.bmcl.2017.06.003