GW4064

Description: GW4064 is a novel, potent and selective agonist of farnesoid X receptor (FXR) with EC50 of 65 nM in CV1 cell line. It displays no activity at other nuclear receptors, including the retinoic acid receptor, at concentrations up to 1 uM. GW-4064 upregulates adipokine expression in preadipocytes and HepG2 cells. GW4064 could reduce induction of proinflammatory cytokines by LPS in vitro. GW4064 shows beneficial effects on cholesterol and TG (triglycerides) 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. GW4064 can also lower serum TGs in the SHP+/+ mice.

References: Bioorg Med Chem Lett. 2008 Aug 1; 18(15):4339-43; J Med Chem. 2000 Aug 10; 43(16):2971-4.