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BAR501研究进展

发布日期：2017-10-27   浏览次数：0
核心提示：a href=https://www.medchemexpress.com/BAR501.htmlBAR501/a产品描述：BAR501 is a potent and selective agonist of bGPBAR1/b
<a href="https://www.medchemexpress.com/BAR501.html">BAR501</a>产品描述：BAR501 is a potent and selective agonist of <b>GPBAR1</b> with an <b>EC<sub>50</sub></b> of 1 μM.

IC50 & Target: EC50: 1 μM (GPBAR1)<sup>[1]</sup>

<i><b>In Vitro:</b></i> 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 EC<sub>50</sub> of 1 μM. Exposure of GLUTAg cells to BAR501 (10 μM) increases the expression of GLP-1 mRNA by 2.5 folds<sup>[1]</sup>.

<i><b>In Vivo:</b></i> 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 express<br><br>
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