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Submit ReviewBQ-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.
分子量 | 611 |
公式 | C31H42N6O7 |
序列 |
WDPVL (Modifications: Trp-1 = D-Trp, Asp-2 = D-Asp, Val-4 = D-Val, Cyclized) |
储存 | Store at -20°C |
纯度 | ≥95% (HPLC) |
CAS Number | 136553-81-6 |
PubChem ID | 52943236 |
InChI Key | VYCMAAOURFJIHD-AOYLRGCGSA-N |
Smiles | CC(C)C[C@@H]1NC(=O)[C@H](NC(=O)[C@@H]2CCCN2C(=O)[C@H](CC(O)=O)NC(=O)[C@@H](CC2=CNC3=C2C=CC=C3)NC1=O)C(C)C |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性 | Soluble to 0.40 mg/ml in water |
参考文献是支持产品生物活性的出版物。
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.
关键词: BQ-123, BQ-123 supplier, Selective, ETA, antagonists, Receptors, Endothelin, 1188, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 BQ-123 的部分引用包括:
Ou et al (2014) Adaptive regulation of endothelin receptor type-A and type-B in vascular smooth muscle cells during pregnancy in rats. J Cell Physiol 229 489 PMID: 24105843
Mazzuca et al (2013) Enhanced endothelin receptor type B-mediated vasodilation and underlying [Ca2+]i in mesenteric microvessels of pregnant rats. Br J Pharmacol 169 1335 PMID: 23646960
Sánchez et al (2014) 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. Br J Pharmacol 171 5682 PMID: 25091502
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
Craig and Martin (2012) Dominance of flow-mediated constriction over flow-mediated dilatation in the rat carotid artery. Br J Pharmacol 167 527 PMID: 22537086
McQueen et al (2007) Endothelin-1 activates ETA receptors to cause reflex scratching in BALB/c mice. Br J Pharmacol 151 278 PMID: 17351652
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