BQ-788 (sodium salt) [156161-89-6]
Referencia HY-15894-10mg
embalaje : 10mg
Marca : MedChemExpress
BQ-788 sodium salt is a potent and selective ETB receptor antagonist, inhibiting ET-1 binding to ETB receptors with an IC50 of 1.2 nM in human Girrardi heart cells.
Para uso exclusivo en investigación. No vendemos a pacientes.
BQ-788 sodium salt Estructura química
No. CAS : 156161-89-6
This product is a controlled substance and not for sale in your territory.
Based on 9 publication(s) in Google Scholar
Other Forms of BQ-788 sodium salt:
- BQ-788 In-stock
Descripciòn |
BQ-788 sodium salt is a potent and selective ETB receptor antagonist, inhibiting ET-1 binding to ETB receptors with an IC50 of 1.2 nM in human Girrardi heart cells[1]. |
||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|
IC50 & Target |
|
||||||||||||
In Vitro |
BQ-788 potently and competitively inhibits 125I-labeled ET-1 binding to ETB receptors in human Girrardi heart cells with an IC50 of 1.2 nM, but only poorly inhibits the binding to ETA receptors in human neuro-blastoma cell line SK-N-MC cells (IC50, 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[1]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. |
||||||||||||
In Vivo |
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[1]. 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[2]. 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[3]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. |
||||||||||||
Ensayo clínico |
|
||||||||||||
Peso molecular |
663.78 |
||||||||||||
Fòrmula |
C34H50N5NaO7 |
||||||||||||
No. CAS |
156161-89-6 |
||||||||||||
Appearance |
Solid |
||||||||||||
Color |
White to off-white |
||||||||||||
SMILES |
CCCC[C@H](C(O[Na])=O)NC([C@@H](CC1=CN(C(OC)=O)C2=CC=CC=C12)NC([C@H](CC(C)(C)C)NC(N3[C@H](C)CCC[C@@H]3C)=O)=O)=O |
||||||||||||
Envío | Room temperature in continental US; may vary elsewhere. |
||||||||||||
Almacenamiento |
-20°C, protect from light, stored under nitrogen *The compound is unstable in solutions, freshly prepared is recommended. |
||||||||||||
Solvente y solubilidad |
In Vitro:
DMSO : 30 mg/mL (45.20 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) H2O : 20 mg/mL (30.13 mM; Need ultrasonic) Preparing
Stock Solutions
View the Complete Stock Solution Preparation Table
* Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended. * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol) Concentration (start) × Volume (start) = Concentration (final) × Volume (final) This equation is commonly abbreviated as: C1V1 = C2V2 In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
Dosage mg/kgAnimal weight Dosing volume Number of animals Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration:
mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
|
||||||||||||
Pureza y Documentación | |||||||||||||
Referencias |
|
Complete Stock Solution Preparation Table
* Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.
Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
---|
H2O / DMSO | 1 mM | 1.5065 mL | 7.5326 mL | 15.0652 mL | 37.6631 mL |
5 mM | 0.3013 mL | 1.5065 mL | 3.0130 mL | 7.5326 mL | |
10 mM | 0.1507 mL | 0.7533 mL | 1.5065 mL | 3.7663 mL | |
15 mM | 0.1004 mL | 0.5022 mL | 1.0043 mL | 2.5109 mL | |
20 mM | 0.0753 mL | 0.3766 mL | 0.7533 mL | 1.8832 mL | |
25 mM | 0.0603 mL | 0.3013 mL | 0.6026 mL | 1.5065 mL | |
30 mM | 0.0502 mL | 0.2511 mL | 0.5022 mL | 1.2554 mL | |
DMSO | 40 mM | 0.0377 mL | 0.1883 mL | 0.3766 mL | 0.9416 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.