BQ-123-

137P08

BQ-123

Cyclo(-D-Trp-D-Asp-Pro-D-Val-Leu)

纯度：>95%HPLC

储存条价：-20°C，避光，干燥。

另提供从粗品至98%纯度规格，具体请联系我们! 本产品仅用于科学研究，不得用于人体！

产品详情

Cat#:

137P08

序列(三字母)：

Cyclo(-D-Trp-D-Asp-Pro-D-Val-Leu)

序列(单字母)：

Cyclo(-wsPvL)

分子式:

C31H42N6O7

分子量:

610.71

CAS#:

136553-81-6

合成方法：

Synthetic

存储条件：

-20 °C，避光，干燥

应用：

Cardiovascular System & Diseases

产品描述：

BQ-123是一种高效、选择性内皮素 A (ETA) 受体拮抗剂，IC50 值为 7.3 nM，Ki 值为 25 nM。BQ-123 抑制内皮素-1 介导的人肺动脉平滑肌细胞增殖，降低高血压大鼠血压。

参考文献:

1. In vitro biological profile of a highly potent novel endothelin (ET) antagonist BQ-123 selective for the ETA receptor. Ihara M, et al. J Cardiovasc Pharmacol. 1992;20 Suppl 12:S11-S14.

2. Distinct subdomains of human endothelin receptors determine their selectivity to endothelinA-selective antagonist and endothelinB-selective agonists. Sakamoto A, et al. J Biol Chem. 1993 Apr 25;268(12):8547-53.

3. BQ123, an ETA receptor antagonist, inhibits endothelin-1-mediated proliferation of human pulmonary artery smooth muscle cells. Zamora MA, et al. Am J Respir Cell Mol Biol. 1993;9(4):429-433.

4. BQ-123, a selective endothelin subtype A-receptor antagonist, lowers blood pressure in different rat models of hypertension. Douglas SA, et al. J Hypertens. 1994;12(5):561-567.

5. The protective effects of endothelin-A receptor antagonist BQ-123 in pentylenetetrazole-induced seizure in rats. Erdogan H et al. Hum Exp Toxicol, 2014 Oct, 33(10):1008-16.

6. Isolation and structural determination of rat neuromedin U. N.Minamino et al., Biochem. Biophys. Res. Commun., 156, 355 (1988)

7. The endothelin receptor antagonist, BQ-123, inhibits angiotensin II-induced contractions in rabbit aorta. M.L.Webb et al., Biochem. Biophys. Res. Commun., 185, 887 (1992)

8. The selective endothelin ETA receptor antagonist BQ123 antagonizes endothelin-1-mediated mitogenesis. E.H.Ohlstein et al., Eur. J. Pharmacol.-Mol. Pharmacol. Sect., 225, 347 (1992)

9. Antihypertensive effect of a newly synthesized endothelin antagonist, BQ-123, in a genetic hypertensive model. M.Nishikibe et al., Life Sci., 52, 717 (1993)

10. The endothelin ETA receptor antagonist, BQ-123, normalizes the response of SHR aorta to Ca2+ channel activator. N.Morel and T.Godfraind, Eur. J. Pharmacol., 252, R3 (1994)

11. Mutational analysis of human endothelin receptors ETA and ETB identification of regions involved in the selectivity for endothelin 3 or cyclo-(D-Trp-D-Asp-Pro-D-Val-Leu). A.Becker et al., Eur. J. Biochem., 221, 951 (1994)

12. Conformational study of cyclo[D-Trp-D-Asp-Pro-D-Val-Leu], an endothelin-A receptor-selective antagonist. R.A.Atkinson and J.T.Pelton, FEBS Lett., 296, 1 (1992)

13. BQ-123, cyclo(-D-Trp-D-Asp-Pro-D-Val-Leu), is a non-competitive antagonist of the actions of endothelin-1 in SK-N-MC human neuroblastoma cells. C.R.Hiley et al., Biochem. Biophys. Res. Commun., 184, 504 (1992)

14. A novel ETA antagonist (BQ-123) inhibits endothelin-1-induced phosphoinositide breakdown and DNA synthesis in rat vascular smooth muscle cells. S.Eguchi et al., FEBS Lett., 302, 243 (1992)

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BQ-123

纯度：>95%HPLC

储存条价：-20°C，避光，干燥。

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