Cat. No. 1188
Biological ActivitySelective ETA endothelin receptor antagonist (Ki values are 1.4 and 1500 nM at ETA and ETB receptors respectively). Reduces ischemia-induced ventricular arrhythmias in a rat model.
(Modifications: Trp-1 = D-Trp, Val-4 = D-Val, Cyclized)
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Certificate of Analysis / Product Datasheet / Safety Datasheet
References are publications that support the products' biological activity.
Agapitov and Haynes (2002) Role of endothelin in cardiovascular disease. J.Renin Angiotensin Aldosterone Syst. 3 1. PMID: 11984741.
Makatani et al (2000) Effect of a novel bifunctional endothelin receptor antagonist, IRL 3630A, on guinea pig respiratory mechanics. Eur.J.Pharmacol. 406 139. PMID: 11011045.
Ekelund et al (1994) Effects of selective ETB-receptor stimulation on arterial, venous and capillary functions in cat skeletal muscle. Br.J.Pharmacol. 112 887. PMID: 7921617.
Sakamoto et al (1993) Distinct subdomains of human endothelin receptors determine their selectivity to endothelinA-selective antagonist and endothelinB-selective agonists. J.Biol.Chem. 268 8547. PMID: 8473300.
If you know of a relevant reference for BQ-123 please let us know.
Citations are publications that use Tocris products. Selected citations for BQ-123 include:
Faraco et al (2014) Water deprivation induces neurovascular and cognitive dysfunction through vasopressin-induced oxidative stress. Am J Pathol 34 852. PMID: 24517977.
Patel et al (2014) Activation of the endothelin system mediates pathological angiogenesis during ischemic retinopathy. J Neurosci 184 3040. PMID: 25203536.
McQueen et al (2007) Endothelin-1 activates ETA receptors to cause reflex scratching in BALB/c mice. Br J Pharmacol 151 278. PMID: 17351652.
Do you know of a great paper that uses BQ-123 from Tocris? If so please let us know.
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Keywords: BQ-123, supplier, Selective, ETA, antagonists, Receptors, Endothelin, Tocris Bioscience, ETA Receptor Antagonist products
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High affinity dual ETA and ETB receptor antagonist;orally bioavailable
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