Pricing updated 2019-07-17. Prices are subject to change without notice.
Farnesoid X receptor (FXR) is a nuclear receptor that acts as a bile acid sensor, protecting cells and organs against bile acid toxicity.1 GW 4064 is a selective agonist of FXR (EC50 = 15 nM).2 It displays no activity at other nuclear receptors, including the retinoic acid receptor, at concentrations up to 1 μM.2 GW 4064 is used to elucidate the role of FXR in dyslipidemia, diabetes, obesity, and cancer.3,4,5,6,7
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1. Rader, D.J. Liver X receptor and farnesoid X receptor as therapeutic targets American Journal of Cardiology 100, 15N-19N (2007).
2. Maloney, P.R., Parks, D.J., Haffner, C.D., et al. Identification of a chemical tool for the orphan nuclear receptor FXR Journal of Medicinal Chemistry 43(16), 2971-2974 (2000).
Haeusler, R.A., Pratt-
4. Watanabe, M., Horai, Y., Houten, S.M., et al. Lowering bile acid pool size with a synthetic farnesoid X receptor (FXR) agonist induces obesity and diabetes through reduced energy expenditure The Journal of Biological Chemisty 286(30), 26913-26920 (2011).
5. Deuschle, U., Schüler, J., Schulz, A., et al. FXR controls the tumor suppressor NDRG2 and FXR agonists reduce liver tumor growth and metastasis in an orthotopic mouse xenograft model PLoS One 7(10), e43044 (2012).
Catalano, S., Malvindi, R., Giordano, C., et al. Farnesoid X receptor, through the binding with steroidogenic factor 1-
Cariou, B., van Harmelen, K., Duran-