Fexaramine | FXR agonist

Fexaramine chemical structure

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Fexaramine (574013-66-4) 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.

References/Citations:

  1. Downes et al. (2003), A chemical, genetic, and structural analysis of the nuclear bile receptor FXR; Mol. Cell, 11 1079
  2. Cho et al. (2013), Positive regulation of osteogenesis by bile acid through FXR; J. Bone Miner. Res., 28 2109
  3. Fang et al. (2015), Intestinal FXR agonism promotes adipose tissue browning and reduces obesity and insulin resistance; Nat. Med., 21 159
  4. Hartmann et al. (2018), Modulation of the intestinal bile acid/farnesoid X receptor/fibroblast growth factor 15 axis improves alcoholic liver disease in mice; Hepatology, 67 2150
  5. Liu et al. (2018), Farnesoid X receptor agonist decreases lipid accumulation by promoting hepatic fatty acid oxidation in db/db mice; Int. J. Mol. Med., 42 1723
574013-66-4, fexaramine, Fexaramine supplier, FXR agonist, intestinal FXR agonist

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Fexaramine (574013-66-4) 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.

References/Citations:

  1. Downes et al. (2003), A chemical, genetic, and structural analysis of the nuclear bile receptor FXR; Mol. Cell, 11 1079
  2. Cho et al. (2013), Positive regulation of osteogenesis by bile acid through FXR; J. Bone Miner. Res., 28 2109
  3. Fang et al. (2015), Intestinal FXR agonism promotes adipose tissue browning and reduces obesity and insulin resistance; Nat. Med., 21 159
  4. Hartmann et al. (2018), Modulation of the intestinal bile acid/farnesoid X receptor/fibroblast growth factor 15 axis improves alcoholic liver disease in mice; Hepatology, 67 2150
  5. Liu et al. (2018), Farnesoid X receptor agonist decreases lipid accumulation by promoting hepatic fatty acid oxidation in db/db mice; Int. J. Mol. Med., 42 1723