2017年11月30日星期四

BAR501 |cas 1632118-69-4

BAR501 |cas 1632118-69-4

DC Chemicals, Website: www.dcchemicals.com

Product Name: BAR501|Cas Number: 1632118-69-4| Catalog Number: DC10385|Other Nmaes: BAR 501; BAR-501

BAR501 is a potent and selective agonist of GPBAR1 with an EC50 of 1 μM.

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[1].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[1].

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