156161-89-6 - Names and Identifiers
156161-89-6 - Physico-chemical Properties
Molecular Formula | C34H50N5O7.Na
|
Molar Mass | 663.79 |
Solubility | DMSO: ≥ 43 mg/mL |
Appearance | solid |
Color | white |
Storage Condition | -20°C |
In vitro study | BQ-788 potently and competitively inhibits 125 I-labeled ET-1 binding to ETB receptors in human Girrardi heart cells with an IC 50 of 1.2 nM, but only poorly inhibits the binding to ETA receptors in human neuro-blastoma cell line SK-N-MC cells (IC 50 , 1300 nM). BQ-788 shows no agonistic activity up to 10 μM and competitively inhibits thevasoconstriction induced by an ETB-selective agonist (pA2, 8.4). BQ-788 also inhibits several bioactivities of ET-1, such as bronchoconstriction, cell proliferation, and clearance of perfused ET-1. |
In vivo study | BQ-788 (3 mg/kg/h, i.v.) completely inhibits a pharmacological dose of ET-1- or sarafotoxin6c (0.5 nmol/kg, i.v.)-induced ETB receptor-mediated depressor, but not pressor responses in conscious rats. Furthermore, BQ-788 markedly increases the plasma concentration of ET-1, which is 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.) increases blood pressure by about 20 mm Hg. It is reported that BQ-788 also inhibits ET-1-induced bronchoconstriction, tumor growth and lipopolysaccharide-induced organfailure. BQ 788 (3 mg/kg) results in an eightfold leftward shift in the ET-1 dose-response curve, suggesting a significant involvement of ETB dilator receptors. Mice are treated with 30 nmol BQ-788 by intraplantar, reduce mechanical hyperalgesia (47% and 42%), thermal hyperalgesia (68% and 76%), oedema (50% and 30%); myeloperoxidase activity (64% and 32%), and overt-pain like behaviours. 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. |
156161-89-6 - Risk and Safety
156161-89-6 - Preparation solution concentration reference
| 1mg | 5mg | 10mg |
---|
1 mM | 1.507 ml | 7.533 ml | 15.065 ml |
5 mM | 0.301 ml | 1.507 ml | 3.013 ml |
10 mM | 0.151 ml | 0.753 ml | 1.507 ml |
5 mM | 0.03 ml | 0.151 ml | 0.301 ml |
Last Update:2024-01-02 23:10:35
156161-89-6 - Introduction
BQ-788 (sodium salt) is a chemical substance whose main properties are as follows:
1. Physical properties: BQ-788 (sodium salt) is a white crystalline solid, soluble in water and some organic solvents at room temperature.
2. Chemical properties: BQ-788 (sodium salt) is a compound with anti endothelin receptor effect.
The main use of BQ-788 (sodium salt) is to study the biology of endothelin, especially its interaction with endothelin type B receptor (ETB receptor).
The production method of BQ-788 (sodium salt) is generally obtained by the method of synthetic chemistry. A particular preparation would involve multiple steps and reactions between the compounds.
Although BQ-788 (sodium salt) has a wide range of applications in scientific research, attention should be paid to its safe use. If used, please follow the laboratory safety procedures, wear appropriate protective equipment, avoid inhalation, contact with skin or food. Before use, please consult the relevant information to understand the safety operation guide and hazard assessment report to ensure safe operation and storage. When handling waste, it should be handled in accordance with relevant regulations to avoid environmental pollution and harm.
Last Update:2024-04-09 01:59:58