|BAR501游离态|CsnPharm

CAS No.: 1632118-69-4

BAR501 is an agonist of GPBAR1 with EC50 of 1 μM. It can effectively reduce hepatic perfusion pressure.

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400-920-2911

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400-920-2911

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描述GPBAR1 is a bile acids activated receptor expressed in entero-hepatic tissues which mediates non-genomic activities of secondary bile acids by increasing intracellular concentrations of cAMP, leading to downstream activation of cAMP-response element (CRE)-binding proteins (CREBs) in target cells. BAR501 is a selective GPBAR1 agonist with an EC₅₀ value of 1 μM. In GLUTAg cells, BAR501 (10 μM) increased the expression of GLP-1 (pro-glugagon-1 gene) mRNA by 2.5 folds associating with a robust increase of cAMP concentrations. In vivo, pretreating rats with 15 mg/kg BAR501 for 6 days reduced basal portal pressure and blunted the vasoconstriction activity of NE (nor-epinephrine). Additionally, pretreatment with BAR501 attenuated the hepatic vasomotor activity induced byshear stress and methoxamine. Moreover, in the CCL₄ model, treating mice with BAR501 at the dose of 15 mg/Kg reduced portal pressure and AST (aspartate aminotransferase) plasma levels^[2].
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技术信息

CAS号

1632118-69-4

储存条件

分子式

C26H46O3

运输

蓝冰

分子量

406.64

别名

溶解度

动物实验配方

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