Product Details
| Product Name:
BQ-788 sodium salt |
CAS No.:
156161-89-6 |
| Supply Ability:
10g |
Release date:
2025/07/20 |
Product Introduction
Bioactivity
| Name | BQ-788 sodium salt |
| Description | BQ-788 sodium salt is a potent and selective antagonist of ETB receptor [ETB receptors] with an IC50 of 1.2 nM in human Girrardi heart cells. |
| In vitro | BQ-788 potently and competitively inhibits 125I-labeled ET-1 binding to ETB receptors in human Girrardi heart cells (hGH) with an IC50 of 1.2 nM, while poorly inhibiting ETA receptor binding in human neuro-blastoma cell line SK-N-MC cells (IC50, 1300 nM). It inhibits ET-1 bioactivities, including bronchoconstriction, cell proliferation, and clearance of perfused ET-1[1], and shows no agonistic activity up to 10 μM. Additionally, BQ-788 competitively inhibits vasoconstriction induced by an ETB-selective agonist (pA2, 8.4). |
| In vivo | Administered intravenously at a dosage of 3 mg/kg/h, BQ-788 effectively blocks the ETB receptor-mediated depressor responses induced by pharmacological levels of ET-1 or sarafotoxin6c (0.5 nmol/kg) in conscious rats, without affecting pressor responses. In Dahl salt-sensitive hypertensive rats, this dosage of BQ-788 results in a significant increase in blood pressure, approximately 20 mm Hg. Moreover, BQ-788 is noted to inhibit ET-1-induced bronchoconstriction, tumor proliferation, and lipopolysaccharide-triggered organ failure. It notably shifts the ET-1 dose-response curve eightfold to the left, highlighting a substantial role of ETB dilator receptors. Additionally, BQ-788 significantly raises plasma ET-1 levels, indicating its potential as an ETB receptor blocker in vivo. In mice, intraplantar administration of 30 nmol BQ-788 reduces mechanical and thermal hyperalgesia, oedema, and myeloperoxidase activity by significant margins, alongside diminishing overt pain-like behaviors. Likewise, intraplantar interventions with either clazosentan or BQ-788 lower superoxide anion production and lipid peroxidation in both spinal and peripheral contexts. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 43 mg/mL (64.68 mM), Sonication is recommended.
|
| Keywords | ETB | BQ788 sodium salt | BQ-788 sodium | BQ 788 sodium salt |
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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Recommended supplier
| Product name |
Price |
|
Suppliers |
Update time |
|
|
$139.00/1mg |
VIP5Y
|
TargetMol Chemicals Inc.
|
2025-07-23 |
|
|
$80.00/1kg |
VIP3Y
|
Zibo Hangyu Biotechnology Development Co., Ltd
|
2023-10-30 |
United States