BAR501

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 naïve rats. It protects against development of endothelial dysfunction by increasing liver cystathione-gamma-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.Formal Name: (3alpha,5beta,6beta,7beta)-6-ethyl-cholane-3,7,24-triol. CAS Number: 1632118-69-4. Molecular Formula: C26H46O3. Formula Weight: 406.6. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 20 mg/mL, DMSO: 100µg/ml, Ethanol: 2 mg/mL, Ethanol:PBS (pH 7.2)(1:2): 500µg/ml. SMILES: C[C@H](CCCO)[C@@]1([H])CC[C@@]2([H])[C@]3([H])[C@@H](O)[C@@H](CC)[C@]4([H])C[C@H](O)CC[C@]4(C)[C@@]3([H])CC[C@@]21C. InChi Code: InChI=1S/C26H46O3/c1-5-18-22-15-17(28)10-12-26(22,4)21-11-13-25(3)19(16(2)7-6-14-27)8-9-20(25)23(21)24(18)29/h16-24,27-29H,5-15H2,1-4H3/t16-,17-,18+,19-,20+,21+,22+,23+,24+,25-,26-/m1/s1. InChi Key: DQBAHTQWQZRMFH-CRPAWOMZSA-N.