1. GPCR/G Protein
  2. Endothelin Receptor
  3. BQ-788 sodium salt

BQ-788 sodium salt 

Cat. No.: HY-15894 Purity: 98.03%
Handling Instructions

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.

For research use only. We do not sell to patients.

BQ-788 sodium salt Chemical Structure

BQ-788 sodium salt Chemical Structure

CAS No. : 156161-89-6

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 613 In-stock
Estimated Time of Arrival: December 31
1 mg USD 180 In-stock
Estimated Time of Arrival: December 31
5 mg USD 420 In-stock
Estimated Time of Arrival: December 31
10 mg USD 600 In-stock
Estimated Time of Arrival: December 31
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100 mg   Get quote  

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Customer Review

Based on 6 publication(s) in Google Scholar

Other Forms of BQ-788 sodium salt:

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Description

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

IC50: 1.2 nM (ETB)

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].

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial
Molecular Weight

663.78

Formula

C₃₄H₅₀N₅NaO₇

CAS No.

156161-89-6

SMILES

CCCC[[email protected]](C(O[Na])=O)NC([[email protected]@H](CC1=CN(C(OC)=O)C2=CC=CC=C12)NC([[email protected]](CC(C)(C)C)NC(N3[[email protected]](C)CCC[[email protected]@H]3C)=O)=O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Solvent & Solubility
In Vitro: 

DMSO : ≥ 43 mg/mL (64.78 mM)

H2O : 2.5 mg/mL (3.77 mM; Need ultrasonic)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.5065 mL 7.5326 mL 15.0652 mL
5 mM 0.3013 mL 1.5065 mL 3.0130 mL
10 mM 0.1507 mL 0.7533 mL 1.5065 mL
*Please refer to the solubility information to select the appropriate solvent.
References
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Keywords:

BQ-788BQ788BQ 788Endothelin ReceptorInhibitorinhibitorinhibit

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Product Name:
BQ-788 sodium salt
Cat. No.:
HY-15894
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