| 名称 | BQ-788 |
| 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. |
| 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]. |
| 存储条件 | Keep away from moisture,
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度 | DMSO : 150 mg/mL (233.72 mM), Sonication is recommended.
10% DMSO+90% Saline : 10 mg/mL (15.58 mM), Suspension.
10% DMSO+90% Corn Oil : 5 mg/mL (7.79 mM), Sonication is recommended.
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| 关键字 | ETB | EndothelinReceptor | Endothelin Receptor | Endothelin B receptor | BQ-788 | BQ 788 |
| 相关产品 | Clazosentan | Aprocitentan | SB-209670 | Edonentan | Sulfisoxazole | Sparsentan | BMS 182874 | BMS 182874 hydrochloride | Nebentan potassium | Bosentan | Ambrisentan | Sitaxsentan sodium |
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