A novel intestinal-restricted FXR agonist. Issue 15 (1st August 2017)

• Record Type: Journal Article
• Authors: Wang, Hong; Zhao, Zhou; Zhou, Jiyu; Guo, Yitong; Wang, Guangji; Hao, Haiping; Xu, Xiaowei
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 27:Issue 15(2017)
• Page Start: 3386
• Page End: 3390
• Publication Date: 2017-08-01
• Subjects: Farnesoid X receptor -- Agonist -- Intestinal-restricted -- Fexaramine; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2017.06.003
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: Highlights: A new FXR agonist Fex-3 was developed. Fex-3 could selectively activate intestinal FXR and promote the expression of BSEP and SHP while suppressing CYP7A1. We demonstrated that Fex-3 targeted on FXR in ileum and has better selectivity than Fex. 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.