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Overview
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Background
GW4064 is an agonist of FXR with EC50 values of 15nM and 90nM, respectively in an isolated receptor activity assay and in cells transfected with human FXR [1].GW4064 is identified as a highly effective, selective, nonsteroidal agonist of FXR. It shows beneficial effects on cholesterol and TG in various animal species. GW4064 is found to lower serum TG levels in both the KK-Ay and ob/ob mice potently. In KK-Ay mice, a 1-week administration of GW4064 also significantly lowers VLDL secretion. And in the SHP+/+ mice, GW4064 can also lower serum TGs. [2] Due to some limitations, such as limited solubility, potentially toxic stilbene pharmacophore and UV light instability, GW4064 is not a good candidate of drug. It is now usually used as a tool compound for investigating the physiological functions of FXR [3].
[1] Chiang PC, Thompson DC, Ghosh S, Heitmeier MR. A formulation-enabled preclinical efficacy assessment of a farnesoid X receptor agonist, GW4064, in hamsters and cynomolgus monkeys. J Pharm Sci. 2011 Nov;100(11):4722-33.
[2] Watanabe M, Houten SM, Wang L, Moschetta A, Mangelsdorf DJ, Heyman RA, Moore DD, Auwerx J. Bile acids lower triglyceride levels via a pathway involving FXR, SHP, and SREBP-1c. J Clin Invest. 2004 May;113(10):1408-18.
[3] Li W, Fu J, Cheng F, Zheng M, Zhang J, Liu G, Tang Y. Unbinding pathways of GW4064 from human farnesoid X receptor as revealed by molecular dynamics simulations. J Chem Inf Model. 2012 Nov 26;52(11):3043-52.
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