Azasetron HCl

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Chemical Structure| 123040-16-4 同义名 : 阿扎司琼盐酸盐 ;Y-25130 hydrochloride; Azasetron (hydrochloride); Y-25130; Y-25130 HCl; Azasetron HCl
CAS号 : 123040-16-4
货号 : A323775
分子式 : C17H21Cl2N3O3
纯度 : 99%
分子量 : 386.27
MDL号 : MFCD00209913
存储条件：

Pure form Sealed in dry,2-8°C

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

DMSO: 2 mg/mL(5.18 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

H2O: 20 mg/mL(51.78 mM)，配合低频超声助溶
生物活性
靶点

  • 5-HT3

    5-HT3, IC50:0.33 nM
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].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.59mL

0.52mL

0.26mL

12.94mL

2.59mL

1.29mL

25.89mL

5.18mL

2.59mL
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.