BAR501 is an agonist of GPBAR1 with EC50 of 1 μM. It can effectively reduce hepatic perfusion pressure.
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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]. |
计算器 | ||||
存储液制备 | ![]() |
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 |
CAS号 | 1632118-69-4 |
分子式 | C26H46O3 |
分子量 | 406.64 |
SMILES Code | O[C@@H]1CC[C@]2(C)[C@@]3([H])CC[C@]4(C)[C@@H]([C@@H](CCCO)C)CC[C@@]4([H])[C@]3([H])[C@@H](O)[C@@H](CC)[C@]2([H])C1 |
MDL No. | MFCD30738007 |
别名 | |
运输 | 蓝冰 |
存储条件 |
In solvent -20°C:3-6个月-80°C:12个月 Pure form Sealed in dry, 2-8°C |
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