A novel intestinal-restricted FXR agonist.
作者信息
Wang Hong, Zhao Zhou, Zhou Jiyu, Guo Yitong, Wang Guangji, Hao Haiping, Xu Xiaowei
机构信息
State Key Laboratory of Natural Medicines, China Pharmaceutical University, Tongjiaxiang#24, Nanjing 210009, China; Key Lab of Drug Metabolism and Pharmacokinetics, China Pharmaceutical University, Tongjiaxiang#24, Nanjing 210009, China.
State Key Laboratory of Natural Medicines, China Pharmaceutical University, Tongjiaxiang#24, Nanjing 210009, China; School of Pharmacy, China Pharmaceutical University, Tongjiaxiang#24, Nanjing 210009, China.
出版信息
Bioorg Med Chem Lett. 2017 Aug 1;27(15):3386-3390. doi: 10.1016/j.bmcl.2017.06.003. Epub 2017 Jun 3.
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.
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