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BAR501

CAS No. : 1632118-69-4

MCE 国际站：BAR501

产品活性：BAR501是高效选择性的GPBAR1激动剂，EC₅₀值为1 μM。

研究领域：GPCR/G Protein

作用靶点：G protein-coupled Bile Acid Receptor 1

In Vitro: BAR501 is a selective GPBAR1 agonist devoid of FXR agonistic activity. It effectively transactivates GPBAR1 in HEK293 cells overexpressing a CRE along with GPBAR1, with an EC₅₀ of 1 μM. Exposure of GLUTAg cells to BAR501 (10 μM) increases the expression of GLP-1 mRNA by 2.5 folds.

In Vivo: Pretreating rats for 6 days with BAR501, 15 mg/kg, reduces basal portal pressure and blunts the vasoconstriction activity of norepinephrine. Pretreatment with BAR501 attenuates the hepatic vasomotor activity induced by shear stress and methoxamine. Administration of BAR501 exerts a direct vasodilatory activity in the CCl4 model. Treating mice with BAR501 at the dose of 15 mg/Kg reduces portal pressure and AST plasma levels. BAR501 attenuates endothelial dysfunction by regulating CSE expression/activity.

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