A selective GP-BAR1 agonist
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BAR501

Item No. 22460

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(3α,5β,6β,7β)-6-ethyl-cholane-3,7,24-triol
CAS Number
1632118-69-4
Molecular Formula
C26H46O3
Formula Weight
406.6
Purity
≥95%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 20 mg/mLDMSO: 100µg/mlEthanol: 2 mg/mLEthanol: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
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    Cayman Chemical
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    Product Description

    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).1 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.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Renga, B., Cipriani, C., Carino, A., et al. Reversal of endothelial dysfunction by GPBAR1 agonism in portal hypertension involves a AKT/FOXOA1 dependent regulation of H2S generation and Endothelin-1. PLoS One 5;10(11), (2015).

    2. Biagioli, M., Carino, A., Cipriani, S., et al. The bile acid receptor GPBAR1 regulates the M1/M2 phenotype of intestinal macrophages and activation of GPBAR1 rescues mice from murine colitis. J. Immunol. 199(2), 718-733 (2017).