BQ-123
Purity: ≥95%
Biological Activity
BQ-123 is a 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.Technical Data
(Modifications: Trp-1 = D-Trp, Asp-2 = D-Asp, Val-4 = D-Val, Cyclized)
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Background References
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Role of endothelin in cardiovascular disease.
Agapitov and Haynes
J.Renin Angiotensin Aldosterone Syst., 2002;3:1 -
Effects of selective ETB-receptor stimulation on arterial, venous and capillary functions in cat skeletal muscle.
Ekelund et al.
Br.J.Pharmacol., 1994;112:887 -
Effect of a novel bifunctional endothelin receptor antagonist, IRL 3630A, on guinea pig respiratory mechanics.
Makatani et al.
Eur.J.Pharmacol., 2000;406:139 -
Distinct subdomains of human endothelin receptors determine their selectivity to endothelinA-selective antagonist and endothelinB-selective agonists.
Sakamoto et al.
J.Biol.Chem., 1993;268:8547
Product Datasheets
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Citations for BQ-123
The citations listed below are publications that use Tocris products. Selected citations for BQ-123 include:
7 Citations: Showing 1 - 7
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Water deprivation induces neurovascular and cognitive dysfunction through vasopressin-induced oxidative stress.
Authors: Faraco Et al.
Am J Pathol 2014;34:852
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Adaptive regulation of endothelin receptor type-A and type-B in vascular smooth muscle cells during pregnancy in rats.
Authors: Ou Et al.
J Cell Physiol 2014;229:489
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Activation of the endothelin system mediates pathological angiogenesis during ischemic retinopathy.
Authors: Patel Et al.
J Neurosci 2014;184:3040
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Endothelin-1 contributes to endothelial dysfunction and enhanced vasoconstriction through augmented superoxide production in penile arteries from Ins-resistant obese rats: role of ET(A) and ET(B) receptors.
Authors: Sánchez Et al.
Br J Pharmacol 2014;171:5682
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Enhanced endothelin receptor type B-mediated vasodilation and underlying [Ca2+]i in mesenteric microvessels of pregnant rats.
Authors: Mazzuca Et al.
Br J Pharmacol 2013;169:1335
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Dominance of flow-mediated constriction over flow-mediated dilatation in the rat carotid artery.
Authors: Craig and Martin
Br J Pharmacol 2012;167:527
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Endothelin-1 activates ETA receptors to cause reflex scratching in BALB/c mice.
Authors: McQueen Et al.
Br J Pharmacol 2007;151:278
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We utilized this product at 1uM to inhibit endothelin-A receptors ex vivo in mouse aortas followed by conducting vasomotor function experiments. We utilized this ET-A inhibitor in combination with Tocris' BQ788 (endothelin-B receptor antagonist) which works equally as well. We have obtained high quality data using this BQ123 product!