Formulation: A crystalline solid
Formal Name: (3α,5β,6β,7β)-6-ethyl-cholane-3,7,24-triol
Purity: ≥95%
Formula Markup: C26H46O3
Formula Weight: 406,6
Shelf life (days): 1460
CAS Number: 1632118-69-4
Notes: 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).{36072} In vivo, BAR501 reduces hepatic perfusion pressure and counteracts norepinephrine-induced vasoconstriction in naïve 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.{36071}
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