Fexaramine

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 (Cay-10006611, EC50 = 80 nM). Fexaramine does not display activity at the following nuclear receptors: hRXRalpha, hPPARalphagammadelta, mPXR, hPXR, hLXRalpha, hTRbeta, hRARbeta, mCAR, mERRgamma, or hVDR.Formal Name: 3-[3-[(cyclohexylcarbonyl)[[4'-(dimethylamino)[1,1'-biphenyl]-4-yl]methyl]amino]phenyl]-2-propenoic acid, methyl ester. CAS Number: 574013-66-4. Molecular Formula: C32H36N2O3. Formula Weight: 496.6. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 10 mg/ml. lambdamax: 286 nm. SMILES: CN(C)C(C=C1)=CC=C1C2=CC=C(CN(C3=CC=CC(/C=C/C(OC)=O)=C3)C(C4CCCCC4)=O)C=C2. InChi Code: InChI=1S/C32H36N2O3/c1-33(2)29-19-17-27(18-20-29)26-15-12-25(13-16-26)23-34(32(36)28-9-5-4-6-10-28)30-11-7-8-24(22-30)14-21-31(35)37-3/h7-8,11-22,28H,4-6,9-10,23H2,1-3H3/b21-14+. InChi Key: VLQTUNDJHLEFEQ-KGENOOAVSA-N.