BQ-123

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Chemical Structure| 136553-81-6 同义名 : Cyclo(D-Trp-D-Asp-Pro-D-Val-Leu)
CAS号 : 136553-81-6
货号 : A370186
分子式 : C31H42N6O7
纯度 : 98%
分子量 : 610.7
MDL号 : MFCD00133204
存储条件：

Pure form Sealed in dry, store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(81.87 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
生物活性
靶点

  • ET-A

    Endothelin A receptor, IC50:7.3 nM
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].
作用机制 BQ123 is a competitive antagonist selective for the ETA- receptor.[1]
实验方案
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
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.