A selective GP-BAR1 agonist (EC50 = 1 μM); reduces hepatic perfusion pressure and counteracts norepinephrine-induced vasoconstriction in naïve rats; protects against development of endothelial dysfunction by increasing CSE expression and activity and reducing ET-1 gene expression in rat model of cirrhosis; increases Akt-dependent phosphorylation of CSE and eNOS and inhibits ET-1 transcription in vitro; reduces trinitrobenzenesulfonic acid-induced colitis in mice in a dose-dependent manner

BAR501 – 1 mg

Brand:
Cayman
CAS:
1632118-69-4
Storage:
-20
UN-No:
Non-Hazardous - /

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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Description

A selective GP-BAR1 agonist (EC50 = 1 μM); reduces hepatic perfusion pressure and counteracts norepinephrine-induced vasoconstriction in naïve rats; protects against development of endothelial dysfunction by increasing CSE expression and activity and reducing ET-1 gene expression in rat model of cirrhosis; increases Akt-dependent phosphorylation of CSE and eNOS and inhibits ET-1 transcription in vitro; reduces trinitrobenzenesulfonic acid-induced colitis in mice in a dose-dependent manner

Formal name: (3α,5β,6β,7β)-6-ethyl-cholane-3,7,24-triol

Synonyms: 

Molecular weight: 406.6

CAS: 1632118-69-4

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Agonists||Research Area|Cardiovascular System|Vasculature|Vasodilation||Research Area|Endocrinology & Metabolism|Bile Acids & Microbiome||Research Area|Immunology & Inflammation|Gastric Disease|Crohn’s Disease||Research Area|Immunology & Inflammation|Innate Immunity

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