|6-氯-4-甲基-3-氧代-N-(奎宁环-3-基)-3,4-二氢-2H-苯并[b][1,4]恶嗪-8-甲酰胺盐酸盐|CsnPharm

CAS No.: 123040-16-4

盐酸阿扎司琼 Catalog No. CSN12514

Synonyms: Y-25130 hydrochloride;Y-25130 HCl;Azasetron (hydrochloride)

Azasetron HCl is a potent, selective and competitive 5-HT3 receptor antagonist with pKi value of 9.27.

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400-920-2911

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 5-HT Receptor 3

IC50:0.33nM
描述Azasetron Hydrochloride, a potent and selective 5-HT3 receptor antagonist, inhibits the chemotherapy-induced nausea and vomiting in animals and humans. The affinity of azasetron for the 5-HT3 receptor examined in the cerebral cortex of rats indicated that the agent binds to the receptor competitively with [3H]granisetron with a Ki value of 0.54 nM. Research has shown that azasetron was confirmed to show a high affinity to the 5-HT3 receptor at the very site of its antiemetic action^[3]. Azasetron has already been shown to be highly effective in the prophylaxis of nausea and vomiting induced by anticancer drugs^[4].
参考文献

[1] Haga K, Inaba K, et al. The effects of orally administered Y-25130, a selective serotonin3-receptor antagonist, on chemotherapeutic agent-induced emesis. Jpn J Pharmacol. 1993 Nov;63(3):377-83.
[2] Sato N, Sakamori M, et al. Antagonistic activity of Y-25130 on 5-HT3 receptors. Jpn J Pharmacol. 1992 Aug;59(4):443-8.
[3] Katayama K, Asano K, Haga K, Fukuda T. High affinity binding of azasetron hydrochloride to 5-hydroxytryptamine3 receptors in the small intestine of rats. Jpn J Pharmacol. 1997 Apr;73(4):357-60. doi: 10.1254/jjp.73.357. PMID: 9165374.
[4] Lin G, Ma J, Zhu J, Yang X, Hu L, Wang X. Determination of azasetron hydrochloride in rabbit plasma by liquid chromatography tandem mass spectrometry and its application. Biomed Chromatogr. 2011 Oct;25(10):1107-11. doi: 10.1002/bmc.1578. Epub 2010 Dec 29. PMID: 21204117.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.5888 mL
- 12.9442 mL
- 25.8884 mL
- 5 mM
- 0.5178 mL
- 2.5888 mL
- 5.1777 mL
- 10 mM
- 0.2589 mL
- 1.2944 mL
- 2.5888 mL

技术信息

CAS号

123040-16-4

储存条件

粉末: Sealed in dry,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C17H21Cl2N3O3

运输

蓝冰

分子量

386.27

别名

Y-25130 hydrochloride;Y-25130 HCl;Azasetron (hydrochloride);Y-25130;盐酸阿扎司琼

溶解度

DMSO	Insoluble
Ethanol	Insoluble

动物实验配方

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