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BQ-788 sodium salt

产品编号 T10595L CAS 156161-89-6

BQ-788 sodium salt is a potent and selective antagonist of ETB receptor(ETB receptors with an IC50 of 1.2 nM in human Girrardi heart cells).

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BQ-788 sodium salt, CAS 156161-89-6

规格	价格/CNY	货期
2 mg	￥ 1,820	5日内发货
25 mg	￥ 7,930	10-14周
50 mg	￥ 10,300	10-14周
100 mg	￥ 15,900	10-14周

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BQ-788 sodium salt 的其他形式现货产品:

BQ-788

其他形式的 BQ-788 sodium salt:

BQ-788
现货

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生物活性

化学信息

存储 & 溶解度

参考文献

产品描述	BQ-788 sodium salt is a potent and selective antagonist of ETB receptor(ETB receptors with an IC50 of 1.2 nM in human Girrardi heart cells).
靶点活性	ETB:1.2 nM
体外活性	BQ-788 potently and competitively inhibits 125I-labeled ET-1 binding to ETB receptors in human Girrardi heart cells (hGH) with an IC50 of 1.2 nM. However, it only poorly inhibits the binding to ETA receptors in human neuro-blastoma cell line SK-N-MC cells (IC50, 1300 nM). BQ-788 also inhibits several bioactivities of ET-1, such as bronchoconstriction, cell proliferation, and clearance of perfused ET-1[1]. BQ-788 shows no agonistic activity up to 10 μM and competitively inhibits thevasoconstriction induced by an ETB-selective agonist (pA2, 8.4).
体内活性	BQ-788 (3 mg/kg/h, i.v.) completely inhibits a pharmacological dose of ET-1- or sarafotoxin6c (0.5 nmol/kg, i.v.)-induced ETB receptor-mediated depressor, but not pressor responses in conscious rats. In Dahl salt-sensitive hypertensive (DS) rats, BQ-788 (3 mg/kg/h, i.v.) increases blood pressure by about 20 mm Hg. It is reported that BQ-788 also inhibits ET-1-induced bronchoconstriction, tumor growth and lipopolysaccharide-induced organfailure[1]. BQ 788 (3 mg/kg) results in an eightfold leftward shift in the ET-1 dose-response curve, suggesting a significant involvement of ETB dilator receptors[2]. BQ-788 markedly increases the plasma concentration of ET-1, which is considered an index of potential ETB receptor blockade in vivo. Mice are treated with 30 nmol BQ-788 by intraplantar, reduce mechanical hyperalgesia (47% and 42%), thermal hyperalgesia (68% and 76%), oedema (50% and 30%); myeloperoxidase activity (64% and 32%), and overt-pain like behaviours. Additionally, intraplantar treatment with clazosentan or BQ-788 decreases spinal (45% and 41%) and peripheral (47% and 47%) superoxide anion production as well as spinal (47% and 47%) and peripheral (33% and 54%) lipid peroxidation, respectively[3].

分子量	664.8
分子式	C34H51N5NaO7
CAS No.	156161-89-6

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 43 mg/mL (64.78 mM)

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.5042 mL	7.5211 mL	15.0421 mL	37.6053 mL
	5 mM	0.3008 mL	1.5042 mL	3.0084 mL	7.5211 mL
	10 mM	0.1504 mL	0.7521 mL	1.5042 mL	3.7605 mL
	20 mM	0.0752 mL	0.3761 mL	0.7521 mL	1.8803 mL
	50 mM	0.0301 mL	0.1504 mL	0.3008 mL	0.7521 mL

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参考文献

1. Okada M, et al. BQ-788, a selective endothelin ET(B) receptor antagonist. Cardiovasc Drug Rev. 2002 Winter;20(1):53-66. 2. Sargent CA, et al. Effect of endothelin antagonists with or without BQ 788 on ET-1 responses in pithed rats. J Cardiovasc Pharmacol. 1995;26 Suppl 3:S216-8. 3. Fattori V, et al. Differential regulation of oxidative stress and cytokine production by endothelin ETA and ETB receptors in superoxide anion-induced inflammation and pain in mice. J Drug Target. 2016 Oct 5:1-27

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

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第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

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