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BQ-788 sodium salt

Catalog No. T10595L CAS 156161-89-6

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).

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BQ-788 sodium salt, CAS 156161-89-6

Pack Size	Availability	Price/USD
2 mg	5 days	$ 285.00
25 mg	10-14 weeks	$ 977.00
50 mg	10-14 weeks	$ 1,270.00
100 mg	10-14 weeks	$ 1,930.00

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Biological Description

Chemical Properties

Storage & Solubility Information

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).
Targets&IC50	ETB:1.2 nM
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. However, it only poorly inhibits the binding to ETA receptors in human neuro-blastoma cell line SK-N-MC cells (IC50, 1300 nM). BQ-788 also inhibits several bioactivities of ET-1, such as bronchoconstriction, cell proliferation, and clearance of perfused ET-1[1]. BQ-788 shows no agonistic activity up to 10 μM and competitively inhibits thevasoconstriction 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.

Molecular Weight	664.8
Formula	C34H51N5NaO7
CAS No.	156161-89-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 43 mg/mL (64.78 mM)

References and Literature

1. Okada M, et al. BQ-788, a selective endothelin ET(B) receptor antagonist. Cardiovasc Drug Rev. 2002 Winter;20(1):53-66. 2. Sargent CA, et al. Effect of endothelin antagonists with or without BQ 788 on ET-1 responses in pithed rats. J Cardiovasc Pharmacol. 1995;26 Suppl 3:S216-8. 3. Fattori V, et al. Differential regulation of oxidative stress and cytokine production by endothelin ETA and ETB receptors in superoxide anion-induced inflammation and pain in mice. J Drug Target. 2016 Oct 5:1-27

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