A novel intestinal-restricted FXR agonist

作者：Wang, Hong; Zhao, Zhou; Zhou, Jiyu; Guo, Yitong; Wang, Guangji; Hao, Haiping^*; Xu, Xiaowei^*

来源：Bioorganic & Medicinal Chemistry Letters, 2017, 27(15): 3386-3390.

DOI：10.1016/j.bmcl.2017.06.003

• Farnesoid X receptor
• Agonist
• Intestinal-restricted
• Fexaramine

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.

• 出版日期2017-8-1
• 单位中国药科大学; 天然药物活性组分与药效国家重点实验室