BQ-788

SKU: orb1710217

Description

BQ-788 is a selective and potent antagonist of the endothelin B (ETB) receptor. It blocks ET-1 binding and its vasoconstrictive effects, as shown in coronary perfusion studies. This compound is widely used in cardiovascular research to investigate endothelin signaling in vitro and in animal models of hypertension.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 173326-37-9
• MW: 641.8
• Purity: 98.81%
• Formula: C₃₄H₅₁N₅O₇
• SMILES: CCCC[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
• Target: Endothelin Receptor
• Solubility: DMSO:150 mg/mL (233.72 mM);10% DMSO+90% Corn Oil:5 mg/mL (7.79 mM)

Bioactivity

• Target IC50:
  ETB:1.2 nM|ETA:1300 nM (Human SK-N-MC cells)
• 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. 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. 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.
• 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.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

EndothelinReceptor, Endothelin B receptor, Endothelin Receptor, ETB, BQ 788, BQ788, BQ-788

Compound Identifiers

PubChem CID

5311032