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BQ-788

BQ-788
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.
Catalog No. T10595Cas No. 173326-37-9
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Purity:98.67%
ee:100%
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BQ-788

Purity: 98.67%
Catalog No. T10595Alias BQ788Cas No. 173326-37-9

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.
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Pack SizePriceAvailabilityQuantity
1 mg$139In Stock
2 mg$198In Stock
5 mg$347In Stock
10 mg$496In Stock
25 mg$793In Stock
50 mg$1,070In Stock
100 mg$1,450In Stock
500 mg$2,880In Stock
1 mL x 10 mM (in DMSO)$379In Stock
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Product Introduction

Bioactivity
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
ETB:1.2 nM, ETA:1300 nM (Human SK-N-MC cells)
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].
AliasBQ788
Chemical Properties
Molecular Weight641.8
FormulaC34H51N5O7
Cas No.173326-37-9
Storage & Solubility Information
StoragePowder: -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
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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