BAR501
产品说明书
 |
同义名 : | - |
| CAS号 : | 1632118-69-4 | |
| 货号 : | A762703 | |
| 分子式 : | C26H46O3 | |
| 纯度 : | 98+% | |
| 分子量 : | 406.64 | |
| MDL号 : | MFCD30738007 | |
| 存储条件： |
Pure form Sealed in dry, 2-8°C In solvent -20°C:3-6个月-80°C:12个月 |
|
| 溶解度 : | - | |
| 动物实验配方： |
| 生物活性 | |||
|---|---|---|---|
| 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]. | ||
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
|
1 mM 5 mM 10 mM |
2.46mL 0.49mL 0.25mL |
12.30mL 2.46mL 1.23mL |
24.59mL 4.92mL 2.46mL |
| 参考文献 |
|---|