Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 1,230 | 现货 | ||
2 mg | ¥ 1,730 | 现货 | ||
5 mg | ¥ 2,680 | 现货 | ||
10 mg | ¥ 3,850 | 现货 | ||
25 mg | ¥ 5,970 | 现货 | ||
50 mg | ¥ 8,230 | 现货 | ||
100 mg | ¥ 10,900 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 2,970 | 现货 |
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 | ETA:1300 nM (Human SK-N-MC cells), ETB:1.2 nM |
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 |
分子量 | 641.8 |
分子式 | C34H51N5O7 |
CAS No. | 173326-37-9 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 150 mg/mL (233.72 mM), Sonication is recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 1.5581 mL | 7.7906 mL | 15.5812 mL | 38.9529 mL |
5 mM | 0.3116 mL | 1.5581 mL | 3.1162 mL | 7.7906 mL | |
10 mM | 0.1558 mL | 0.7791 mL | 1.5581 mL | 3.8953 mL | |
20 mM | 0.0779 mL | 0.3895 mL | 0.7791 mL | 1.9476 mL | |
50 mM | 0.0312 mL | 0.1558 mL | 0.3116 mL | 0.7791 mL | |
100 mM | 0.0156 mL | 0.0779 mL | 0.1558 mL | 0.3895 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。
BQ-788 173326-37-9 GPCR/G Protein Endothelin Receptor BQ 788 BQ788 Inhibitor inhibitor inhibit