BAR501 is a selective agonist of the G protein-coupled bile acid-activated receptor (GP-BAR1; EC50 = 1 μM) that lacks activity at the farnesoid X receptor (FXR).
CAS：1632118-69-4
分子式：C26H46O3
分子量：406.6
纯度：98%
存储：Store at -20°C

Background:

BAR501 is a selective agonist of the G protein-coupled bile acid-activated receptor (GP-BAR1; EC50 = 1 μM) that lacks activity at the farnesoid X receptor (FXR). In vivo, BAR501 reduces hepatic perfusion pressure and counteracts norepinephrine-induced vasoconstriction in na?ve rats. It protects against development of endothelial dysfunction by increasing liver cystathione-γ-liase (CSE) expression and activity, while reducing endothelin 1 (ET-1) gene expression in a rat model of cirrhosis. In vitro, BAR501 increases Akt-dependent phosphorylation of CSE and endothelial nitric oxide synthase (eNOS) and inhibits ET-1 transcription in human liver sinusoidal cells. BAR501 also shifts macrophages from the inflammatory (M1) phenotype to the anti-inflammatory (M2) phenotype and reduces trinitrobenzenesulfonic acid-induced colitis in mice in a dose-dependent manner.