Selective 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)
|Storage||Desiccate at -20°C|
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.
|Solubility||Soluble to 0.40 mg/ml in water|
Preparing Stock Solutions
The following data is based on the product molecular weight 611. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||1.64 mL||8.18 mL||16.37 mL|
|5 mM||0.33 mL||1.64 mL||3.27 mL|
|10 mM||0.16 mL||0.82 mL||1.64 mL|
|50 mM||0.03 mL||0.16 mL||0.33 mL|
The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.
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
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
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
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.
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Keywords: Selective ETA antagonists Receptors Endothelin Endothelin ETA Receptors
3 Citations for BQ-123
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.
Literature in this Area
Peripheral sensitization is the reduction in the threshold of excitability of sensory neurons that results in an augmented response to a given external stimulus. This poster outlines the excitatory and inhibitory signaling pathways involved in modulation of peripheral sensitization. The role of ion channels, GPCRs, neurotrophins, and cytokines in sensory neurons are also described.