BAR501CAS号： 1632118-69-4分子式： C26H46O3分子量： 406.64描述纯度储存/保存方法别名可溶性/溶解性靶点In vitro(体外研究)In vivo(体内研究)
| 产品描述 | |
| 描述 |
BAR501 is a potent and selective agonist of GPBAR1 with an EC50 of 1 μM.
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| 纯度 |
98%
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| 储存/保存方法 |
Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.
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| 基本信息 | |
| 别名 |
BAR-501；BAR 501
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| 可溶性/溶解性 |
Ethanol : 120 mg/mL (295.10 mM; Need ultrasonic)
DMSO : ≥ 50 mg/mL (122.96 mM) |
| 生物活性 | |
| 靶点 |
GPCR19
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| In vitro(体外研究) |
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.
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| In vivo(体内研究) |
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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分子结构图
