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 (; EC50 = 80 nM). Fexaramine does not display activity at the following nuclear receptors: hRXRα, hPPARαγδ, mPXR, hPXR, hLXRα, hTRβ, hRARβ, mCAR, mERRγ, or hVDR.
Fexaramine has been used to study its action on RANKL (receptor activator of nuclear factor-κB ligand)-induced osteoclastogenesis in mouse model.
ChEBI: Fexaramine is a member of biphenyls.
Fexaramine belongs to the nuclear hormone receptor family.
Potent, selective farnesoid X receptor agonist (EC 50 = 25 nM). Displays no activity at hRXR α , hPPAR α , hPPAR γ , hPPAR δ , mPXR, hPXR, hLXR α , hTR β , hRAR β , mCAR, mERR γ and hVDR receptors.
Fexaramine might regulate lipid and glucose metabolism and can serve as a therapeutic target in the treatment of fatty liver disease, type 2 diabetes and obesity. Fexaramine might mediate cholesterol homeostasis and promotes osteoblast differentiation and suppresses differentiation of osteoclast.
[1] MICHAEL DOWNES. A chemical, genetic, and structural analysis of the nuclear bile acid receptor FXR.[J]. Molecular Cell, 2003, 11 4: 1079-1092. DOI:
10.1016/s1097-2765(03)00104-7
