Fexaramine is a potent (EC50 = 25 nM) and selective agonist of the nuclear bile acid receptor FXR.1 It significantly enhanced osteoblastic differentiation and suppressed osteoclast differentiation from bone marrow macrophages.2 Fexaramine induces enteric FGF15 and reduces diet-induced weight gain, body-wide inflammation, and hepatic glucose production while enhancing thermogenesis and browning of white adipose tissue.3 It protected mice from ethanol-induced liver injury4 and decreased lipid accumulation via hepatic fatty acid oxidation5.
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