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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
WARNING This product is not for human or veterinary use.
1. A chemical, genetic, and structural analysis of the nuclear bile acid receptor FXR. Mol. Cell 11(4), 1079-1092 (2003).