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BQ-788

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产品编号 T10595Cas号 173326-37-9
别名 BQ788

BQ-788 是一种具有选择性和有效性的 ETB 受体拮抗剂,具有潜在的高血压活性,抑制 ET-1 与 ETB 受体结合,抑制外源性 ET-1 诱导的冠状动脉灌注压升高。

BQ-788

BQ-788

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纯度: 98.67%
产品编号 T10595 别名 BQ788Cas号 173326-37-9

BQ-788 是一种具有选择性和有效性的 ETB 受体拮抗剂,具有潜在的高血压活性,抑制 ET-1 与 ETB 受体结合,抑制外源性 ET-1 诱导的冠状动脉灌注压升高。

规格价格库存数量
1 mg
¥ 1,230
现货
2 mg
¥ 1,730
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5 mg
¥ 2,680
现货
10 mg
¥ 3,850
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25 mg
¥ 5,970
现货
50 mg
¥ 8,230
现货
100 mg
¥ 10,900
现货
1 mL x 10 mM (in DMSO)
¥ 2,970
现货
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纯度:98.67%
ee:100%
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产品介绍

生物活性
产品描述
BQ-788 is a selective and potent ETB receptor antagonist with potential hypertensive activity.BQ-788 inhibits ET-1 binding to ETB receptors and inhibits exogenous ET-1-induced elevation of coronary artery perfusion pressure.
靶点活性
ETB:1.2 nM, ETA:1300 nM (Human SK-N-MC cells)
体外活性
BQ-788 potently and competitively inhibits the binding of 125I-labeled ET-1 to ETB receptors in human Girrardi heart cells (hGH) with an IC50 of 1.2 nM. However, it poorly inhibits the binding to ETA receptors in the human neuroblastoma cell line SK-N-MC cells (IC50, 1300 nM). BQ-788, up to 10 μM, shows no agonistic activity and competitively inhibits the vasoconstriction induced by an ETB-selective agonist (pA2, 8.4). Additionally, BQ-788 inhibits several bioactivities of ET-1, such as bronchoconstriction, cell proliferation, and clearance of perfused ET-1[1].
体内活性
In conscious rats, BQ-788 (3 mg/kg/h, i.v.) completely inhibits ETB receptor-mediated depressor responses induced by a pharmacological dose of ET-1 or sarafotoxin6c (0.5 nmol/kg, i.v.), but not pressor responses. Additionally, BQ-788 markedly increases the plasma concentration of ET-1, considered an index of potential ETB receptor blockade in vivo. In Dahl salt-sensitive hypertensive (DS) rats, BQ-788 (3 mg/kg/h, i.v.) raises blood pressure by about 20 mm Hg. It is reported that BQ-788 also inhibits ET-1-induced bronchoconstriction, tumor growth, and lipopolysaccharide-induced organ failure[1]. BQ 788 (3 mg/kg) results in an eightfold leftward shift in the ET-1 dose-response curve, suggesting significant involvement of ETB dilator receptors[2]. In mice treated with 30 nmol BQ-788 by intraplantar administration, there is a reduction in mechanical hyperalgesia (47% and 42%), thermal hyperalgesia (68% and 76%), oedema (50% and 30%), myeloperoxidase activity (64% and 32%), and overt-pain like behaviors. Additionally, intraplantar treatment with clazosentan or BQ-788 decreases spinal (45% and 41%) and peripheral (47% and 47%) superoxide anion production as well as spinal (47% and 47%) and peripheral (33% and 54%) lipid peroxidation, respectively[3].
别名BQ788
化学信息
分子量641.8
分子式C34H51N5O7
CAS No.173326-37-9
SmilesCCCC[C@@H](NC(=O)[C@@H](Cc1cn(C(=O)OC)c2ccccc12)NC(=O)[C@H](CC(C)(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(O)=O
密度1.23 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: 150 mg/mL (233.72 mM), Sonication is recommended.
溶液配制表
DMSO
1mg5mg10mg50mg
1 mM1.5581 mL7.7906 mL15.5812 mL77.9059 mL
5 mM0.3116 mL1.5581 mL3.1162 mL15.5812 mL
10 mM0.1558 mL0.7791 mL1.5581 mL7.7906 mL
20 mM0.0779 mL0.3895 mL0.7791 mL3.8953 mL
50 mM0.0312 mL0.1558 mL0.3116 mL1.5581 mL
100 mM0.0156 mL0.0779 mL0.1558 mL0.7791 mL

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  • 稀释 计算器
  • 配液 计算器
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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

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