Pricing updated 2019-07-17. Prices are subject to change without notice.
The farnesoid X receptor (FXR) is a nuclear receptor that acts as a bile acid sensor, protecting cells and organs against bile acid toxicity and coordinating cholesterol metabolism, lipid homeostasis, and absorption of dietary fats and vitamins. Fexaramine is an FXR agonist (EC50 = 25 nM) that demonstrates 100-fold increased affinity to FXR compared to endogenous bile acids and 3-fold increased potency compared to the high affinity FXR agonist GW 4064 (Item No. 10006611; EC50 = 80 nM).1 Fexaramine does not display activity at the following nuclear receptors: hRXRα, hPPARαγδ, mPXR, hPXR, hLXRα, hTRβ, hRARβ, mCAR, mERRγ, or hVDR.1
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1. Downes, M., Verdecia, M.A., Roecker, A.J., et al. A chemical, genetic, and structural analysis of the nuclear bile acid receptor FXR Molecular Cell 11(4), 1079-1092 (2003).