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BAR502 is a dual agonist of the G protein-coupled bile acid-activated receptor and farnesoid x receptor (GP-BAR1 and FXR; EC50s = 0.2 and 1 μM, respectively).1 It increases the expression of the FXR-regulated bile salt export pump (BSEP), organic solute transporter α (OSTα), and small heterodimer partner (SHP) in primary hepatocytes isolated from FXR wild-type mice. BAR502 also increases cAMP-luciferase reporter gene expression, a marker of GP-BAR1 activity, in HEK293T cells.
WARNING This product is not for human or veterinary use.
1. Design, synthesis, and biological evaluation of potent dual agonists of nuclear and membrane bile acid receptors. J. Med. Chem. 57(3), 937-954 (2014).