BQ-123
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货号：A370186
同义名：
Cyclo(D-Trp-D-Asp-Pro-D-Val-Leu)
BQ-123 is a specific antagonist of endothelin A receptor (ETA) and the IC50 is 7.3 nM.
BQ-123 化学结构
BQ-123 3D分子结构
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BQ-123 纯度/质量文件 产品仅供科研
货号：A370186
标准纯度：
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BQ-123 质控信息
BQ-123 生物活性
靶点
描述
BQ-123, a strong and specific endothelin A (ETA) receptor blocker, boasts an IC50 of 7.3 nM and a Ki of 25 nM. It hinders endothelin-1-induced growth of human pulmonary artery smooth muscle cells and reduces blood pressure in various rat hypertension models[1] [2] [3]
体内研究
Continuous intravenous infusions of BQ-123 (0.16-164 nmol/kg per min, for 6 hours) lead to dose-dependent decreases in mean arterial pressure in spontaneously hypertensive rats (SHR), with the greatest reduction achieved at 16 nmol/kg per min[4]
BQ-123 (3 mg/kg; i.v.; given 15 minutes before pentylenetetrazole (PTZ)) significantly hampers the initiation and propagation of seizures in groups treated with PTZ (50 mg/kg; i.p.) + BQ-123[5]
作用机制
BQ123 is a competitive antagonist selective for the ETA - receptor.[1]
BQ-123 动物研究
Dose
Mice: 0.2 mg/kg - 5 mg/kg[3] [4]
Administration
i.v.
BQ-123 参考文献
[1] Ihara M, et al. In vitro biological profile of a highly potent novel endothelin (ET) antagonist BQ-123 selective for the ETA receptor. J Cardiovasc Pharmacol. 1992;20 Suppl 12:S11-S14.
[2] Sakamoto A, et al. Distinct subdomains of human endothelin receptors determine their selectivity to endothelinA-selective antagonist and endothelinB-selective agonists. J Biol Chem. 1993 Apr 25;268(12):8547-53.
[3] Zamora MA, et al. BQ123, an ETA receptor antagonist, inhibits endothelin-1-mediated proliferation of human pulmonary artery smooth muscle cells. Am J Respir Cell Mol Biol. 1993;9(4):429-433.
[4] Douglas SA, et al. BQ-123, a selective endothelin subtype A-receptor antagonist, lowers blood pressure in different rat models of hypertension. J Hypertens. 1994;12(5):561-567.
[5] Erdogan H et al. The protective effects of endothelin-A receptor antagonist BQ-123 in pentylenetetrazole-induced seizure in rats. Hum Exp Toxicol, 2014 Oct, 33(10):1008-16.
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BQ-123 实验方案
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摩尔计算器
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存储液制备
1mg
5mg
10mg
1 mM
5 mM
10 mM
1.64mL
0.33mL
0.16mL
8.19mL
1.64mL
0.82mL
16.37mL
3.27mL
1.64mL
BQ-123 技术信息
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