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BAR501

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产品编号 T4083Cas号 1632118-69-4
别名 BAR 501

BAR501是高效选择性的 GPBAR1激动剂(EC50:1 μM)。

BAR501

BAR501

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纯度: 99.34%
产品编号 T4083 别名 BAR 501Cas号 1632118-69-4

BAR501是高效选择性的 GPBAR1激动剂(EC50:1 μM)。

规格价格库存数量
1 mg¥ 496现货
5 mg¥ 1,080现货
10 mg¥ 1,830现货
25 mg¥ 3,580现货
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纯度:99.34%
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产品介绍

生物活性
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
化学信息
分子量406.64
分子式C26H46O3
CAS No.1632118-69-4
SmilesCC[C@@H]1[C@H](O)[C@H]2[C@@H]3CC[C@H]([C@H](C)CCCO)[C@@]3(C)CC[C@@H]2[C@@]2(C)CC[C@@H](O)C[C@@H]12
密度1.047 g/cm3 (Predicted)
储存&溶解度
存储Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
溶解度信息
DMSO: 50 mg/mL (122.96 mM)
溶液配制表
1mg5mg10mg50mg
1 mM2.4592 mL12.2959 mL24.5918 mL122.9589 mL
5 mM0.4918 mL2.4592 mL4.9184 mL24.5918 mL
10 mM0.2459 mL1.2296 mL2.4592 mL12.2959 mL
20 mM0.1230 mL0.6148 mL1.2296 mL6.1479 mL
50 mM0.0492 mL0.2459 mL0.4918 mL2.4592 mL
100 mM0.0246 mL0.1230 mL0.2459 mL1.2296 mL

计算器

  • 摩尔浓度 计算器
  • 稀释 计算器
  • 配液 计算器
  • 分子量 计算器

体内实验配液计算器

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:
TargetMol | Animal experiments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 μLTargetMol | Animal experiments 一共给药动物 10 只 ,您使用的配方为 5% TargetMol | reagent 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 μLDMSOTargetMol | reagent ( 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:50μLDMSOTargetMol | reagent 母液,添加 300 μLPEG300TargetMol | reagent 混匀澄清,再加 50μLTween 80, 混匀澄清,再加 600μLddH2OTargetMol | reagent 混匀澄清

以上为“体内实验配液计算器”的使用方法举例,并不是具体某个化合物的推荐配制方式,请根据您的实验动物和给药方式选择适当的溶解方案。

1 请输入动物实验的基本信息
mg/kg
g
μL
2 请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
%
%Tween 80
%ddH2O

剂量转换

对于不同动物的给药剂量换算,您也可以参考 更多

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