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BQ-788 sodium salt

现货
Catalog No.
B3278
ET B受体拮抗剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 4,700.00
现货
1mg
¥ 1,580.00
现货
5mg
¥ 3,500.00
现货
10mg
¥ 5,000.00
现货

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Background

BQ-788 is a potent and selective antagonist of endothelin (ET) B-receptor with IC50 value of 1.2nM [1].

In the in vitro assay, BQ-788 prevents ET-1 from binding to ETB receptors in human Girardi heart cells with IC50 value of 1.2nM. The inhibition to ETA receptors is much weaker with IC50 value of 1300nM. BQ-788 also inhibits ET binding to ETB receptors with IC50 values of 0.9nM and 1.2nM in porcine cerebellar membranes and hGH cells, respectively. The inhibition effects are quite poor in pCASM cells and SK-N-MC cells with IC50 values of 280nM and 1300nM, respectively. BQ-788 is specific to ET receptors. It cannot significantly inhibit other peptide hormone receptors at concentration of 10μM. It is found that BQ-788 interacts with ETB receptors competitively in hGH cells. Moreover, the in vivo assay demonstrates that ETB receptors are responsible for ET-1-elicited bronchoconstriction in guinea pigs [1].

References:
[1] Ishikawa K, Ihara M, Noguchi K, et al. Biochemical and pharmacological profile of a potent and selective endothelin B-receptor antagonist, BQ-788. Proceedings of the National Academy of Sciences, 1994, 91(11): 4892-4896.

文献引用

1. Huang X, Chen C, et al. "Transdermal BQ-788/EA@ZnO quantum dots as targeting and smart tyrosinase inhibitors in melanocytes." Mater Sci Eng C Mater Biol Appl. 2019 Sep;102:45-52. PMID:31147016

Chemical Properties

Physical AppearanceA solid
StorageDesiccate at RT
M.Wt663.78
Cas No.156161-89-6
FormulaC34H50N5NaO7
Solubility≥33.2mg/mL in DMSO
Chemical Namesodium;(2R)-2-[[(2R)-2-amino-3-(1-methoxycarbonylindol-3-yl)propanoyl]-[(2S)-2-[[(2R,6S)-2,6-dimethylpiperidine-1-carbonyl]amino]-4,4-dimethylpentanoyl]amino]hexanoate
SDFDownload SDF
Canonical SMILESCCCCC(C(=O)[O-])N(C(=O)C(CC1=CN(C2=CC=CC=C21)C(=O)OC)N)C(=O)C(CC(C)(C)C)NC(=O)N3C(CCCC3C)C.[Na+]
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

细胞实验 [1]:

细胞系

hGH和pCASM细胞

制备方法

在DMSO中的溶解度大于33.2 mg/mL。若配制更高浓度的溶液,一般步骤如下:请将试管置于37 °C加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20 °C可放置数月。

反应条件

100 μM

实验结果

BQ-788 (100 μM) 不增加hGH和pCASM细胞中的[Ca2+]i。然而,在上述2种细胞系中,BQ-788显著抑制ET-1诱导的[Ca2+]i增加。

动物实验 [1]:

动物模型

大鼠

给药剂量

1 mg/kg;静脉注射

实验结果

在注射ET-1 5分钟前,静脉注射1 mg/kg BQ-788完全抑制降压作用,相应地引起快速而明显的增压作用。

注意事项

请于室内测试所有化合物的溶解度。虽然化合物的实际溶解度可能与其理论值略有不同,但仍处于实验系统误差的允许范围内。

References:

[1]. Ishikawa K, Ihara M, Noguchi K, et al. Biochemical and pharmacological profile of a potent and selective endothelin B-receptor antagonist, BQ-788. Proceedings of the National Academy of Sciences, 1994, 91(11): 4892-4896.

质量控制

化学结构

BQ-788 sodium salt

相关生物数据

BQ-788 sodium salt