Powder: -20°C for 3 years | In solvent: -80°C for 1 year
BAR501是高效选择性的 GPBAR1激动剂(EC50:1 μM)。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 496 | 现货 | ||
5 mg | ¥ 1,080 | 现货 | ||
10 mg | ¥ 1,830 | 现货 | ||
25 mg | ¥ 3,580 | 现货 | ||
50 mg | ¥ 5,170 | 现货 | ||
100 mg | ¥ 7,320 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 997 | 现货 |
产品描述 | BAR501 is an effective and specific GPBAR1 agonist (EC50: 1 μM). |
靶点活性 | GPBAR1:1 μM(EC50) |
体外活性 | In HEK293 cells overexpressing a CRE along with GPBAR1, BAR501 effectively transactivates GPBAR1 (EC50: 1 μM). In GLUTAg cells, BAR501 (10 μM) increases the mRNA expression of GLP-1 by 2.5 folds. |
体内活性 | Pretreating rats for 6 days with BAR501 (15 mg/kg), the basal portal pressure reduces and the vasoconstriction activity of norepinephrine blunts. BAR501 attenuates the hepatic vasomotor activity induced by methoxamine and shear stress. In the CCl4 model, BAR501 exerts a direct vasodilatory activity. BAR501 (15 mg/kg) can reduce AST plasma levels and portal pressure. BAR501 attenuates endothelial dysfunction by regulating CSE expression/activity. |
细胞实验 | For GPBAR1 mediated transactivation, HEK-293T cells are plated at 10000 cells/well in a 24 well-plate and transfected with 200 ng of pGL4.29, a reporter vector containing a cAMP response element (CRE) that drives the transcription of the luciferase reporter gene luc2P, with 100 ng of pCMVSPORT6-human GPBAR1, and with 100 ng of pGL4.70. At 24 h post-transfection, HepG2 and HEK293T cells are incubated with 10 μM BAR501 for 18 h and luciferase activities are assayed and normalized against the Renilla activities[1]. |
动物实验 | Animal: C57BL6 miceAdministration: i.p., 500 μL/kg of CCl4 in an equal volume of paraffin oil twice a week for 9 weeks. CCL4 mice are randomized to receive BAR501 (15 mg/Kg daily by gavage) or vehicle (distilled water). Serum bilirubin, albumin, aspartate aminotransferase, alanine aminotransferase and alkaline phosphatase are measured by routine biochemical clinical chemistry[1]. |
别名 | BAR 501 |
分子量 | 406.64 |
分子式 | C26H46O3 |
CAS No. | 1632118-69-4 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 50 mg/mL (122.96 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.4592 mL | 12.2959 mL | 24.5918 mL | 61.4794 mL |
5 mM | 0.4918 mL | 2.4592 mL | 4.9184 mL | 12.2959 mL | |
10 mM | 0.2459 mL | 1.2296 mL | 2.4592 mL | 6.1479 mL | |
20 mM | 0.123 mL | 0.6148 mL | 1.2296 mL | 3.074 mL | |
50 mM | 0.0492 mL | 0.2459 mL | 0.4918 mL | 1.2296 mL | |
100 mM | 0.0246 mL | 0.123 mL | 0.2459 mL | 0.6148 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
BAR501 1632118-69-4 GPCR/G Protein GPCR19 Inhibitor GPBAR1 BAR-501 TGR5 BAR 501 G-protein coupled receptor 19 G protein-coupled Bile Acid Receptor 1 inhibit inhibitor