产品描述:
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).{38107} 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.