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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.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $139 | In Stock | |
2 mg | $198 | In Stock | |
5 mg | $347 | In Stock | |
10 mg | $496 | In Stock | |
25 mg | $793 | In Stock | |
50 mg | $1,070 | In Stock | |
100 mg | $1,450 | In Stock | |
500 mg | $2,880 | In Stock | |
1 mL x 10 mM (in DMSO) | $379 | In Stock |
Description | 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. |
Targets&IC50 | ETA:1300 nM (Human SK-N-MC cells), ETB:1.2 nM |
In vitro | BQ-788 potently and competitively inhibits the binding of (125I-labeled ET-1) to ETB receptors in human Girardi heart cells (hGH) with an IC50 of 1.2 nM, but poorly inhibits the binding to ETA receptors in human neuroblastoma cells (SK-N-MC) with an IC50 of 1300 nM. Up to 10 μM, BQ-788 shows no agonistic activity and competitively inhibits vasoconstriction induced by an ETB-selective agonist (pA2, 8.4). Additionally, BQ-788 inhibits several bioactivities of ET-1, including bronchoconstriction, cell proliferation, and clearance of perfused ET-1[1]. |
In vivo | 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]. |
Alias | BQ788 |
Molecular Weight | 641.8 |
Formula | C34H51N5O7 |
Cas No. | 173326-37-9 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 150 mg/mL (233.72 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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