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Postion:Product Catalog >Biologics>Biochemical Reagents>Antagonist>BQ-788
BQ-788
  • BQ-788

BQ-788 NEW

Price $139 $198 $347
Package 1mg 2mg 5mg
Supply Ability: 10g
Update Time: 2026-05-11

Product Details

Product Name: BQ-788 CAS No.: 173326-37-9
Purity: 98.81% Supply Ability: 10g
Release date: 2026/05/11

Product Introduction

Bioactivity

NameBQ-788
DescriptionBQ-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.
In vitroBQ-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 vivoIn 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].
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.
Solubility InformationDMSO : 150 mg/mL (233.72 mM), Sonication is recommended.
10% DMSO+90% Corn Oil : 5 mg/mL (7.79 mM), Sonication is recommended.
KeywordsETB | EndothelinReceptor | Endothelin Receptor | Endothelin B receptor | BQ-788 | BQ 788
Inhibitors RelatedMacitentan | BMS 182874 | Bosentan | BMS 182874 hydrochloride | Sitaxsentan sodium | Edonentan | SB-209670 | Ambrisentan | Sparsentan | Aprocitentan | Nebentan potassium | Clazosentan
Related Compound LibrariesBioactive Compound Library | Pain-Related Compound Library | Membrane Protein-targeted Compound Library | ReFRAME Related Library | Drug Repurposing Compound Library | Inhibitor Library | Anti-Cardiovascular Disease Compound Library | Clinical Compound Library | Bioactive Compounds Library Max | GPCR Compound Library

Company Profile Introduction

Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers. TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.

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TargetMol Chemicals Inc.

6YR United StatesUnited States
  • Since: 2011-01-07
  • Address: 36 Washington Street, Wellesley Hill, MA
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