A potent free fatty acid receptor 1 agonist with a glucose-dependent antihyperglycemic effect

Xuekun Wang; Yurui Xu; Shujun Feng; Xinyu Huang; Xia Meng; Jiao Chen; Leilei Guo; Junliang Ge; Jikang Zhang; Jianmei Chen; Li Cheng; Kai Gu; Yu Zhang; Qing Jiang; Xinghai Ning

doi:10.1039/C9CC04040D

A potent free fatty acid receptor 1 agonist with a glucose-dependent antihyperglycemic effect†

Xuekun Wang,‡^ab Yurui Xu,‡^a Shujun Feng,^a Xinyu Huang,^a Xia Meng,^a Jiao Chen,^c Leilei Guo,^a Junliang Ge,^a Jikang Zhang,^a Jianmei Chen,^a Li Cheng,^a Kai Gu,^ad Yu Zhang,*^a Qing Jiang*^e and Xinghai Ning

*^a

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* Corresponding authors

^a Department of Biomedical Engineering, Nanjing National Laboratory of Microstructures, College of Engineering and Applied Sciences, Nanjing University, Nanjing 210093, P. R. China
E-mail: zhangyu2007sm@163.com, xning@nju.edu.cn

^b Department of Pharmaceutical Engineering, College of Pharmacy, Liaocheng University, Liaocheng 252059, P. R. China

^c Jiangsu Province Academy of Traditional Chinese Medicine, Nanjing 210028, P. R. China

^d Colleges of Medicine, State Key Laboratory of Natural Medicines, China Pharmaceutical University, 24 Tongjiaxiang, Nanjing 210009, P. R. China

^e The Center of Diagnosis and Treatment for Joint Disease, Drum Tower Hospital Affiliated with the Medical School of Nanjing University, Nanjing 210008, P. R. China
E-mail: qingj@nju.edu.cn

Abstract

We present a novel free fatty acid receptor 1 (FFA1) agonist, named PAFA, with a strong agonist potency (EC₅₀ = 6.04 nM) and good serum stability. PAFA significantly stimulates insulin secretion in INS-1 cells in a glucose-dependent manner and exhibits high antihyperglycemic effects in db/db mice without adverse effects.

Chemical Communications

A potent free fatty acid receptor 1 agonist with a glucose-dependent antihyperglycemic effect†

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A potent free fatty acid receptor 1 agonist with a glucose-dependent antihyperglycemic effect

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