Azasetron hydrochloride | Y-25130 hydrochloride;Azasetron (hydrochloride);Y-25130;Y-25130 HCl;Azasetron HCl | 阿扎司琼盐酸盐 | 5-HT Receptor

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盐酸阿扎司琼 /Azasetron hydrochloride 98%

货号：A323775 同义名： 阿扎司琼盐酸盐 / Y-25130 hydrochloride;Azasetron (hydrochloride)

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

Azasetron hydrochloride 化学结构
CAS号：123040-16-4

Azasetron hydrochloride 3D分子结构
CAS号：123040-16-4

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Azasetron hydrochloride 纯度/质量文件产品仅供科研

货号：A323775 标准纯度： 98% 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

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5-羟色胺受体亚型比较

产品名称	5-HT ↓ ↑	5-HT1 ↓ ↑	5-HT2 ↓ ↑	5-HT3 ↓ ↑	5-HT5 ↓ ↑	5-HT6 ↓ ↑	5-HT7 ↓ ↑	其他靶点	纯度
Desvenlafaxine	++ 5-HT, Ki: 40.2 nM								98%
Lamotrigine	+ 5-HT (rat brain synaptosomes), IC50: 474 μM 5-HT (human platelets), IC50: 240 μM								99%+
Venlafaxine	✔								99%+
Fluvoxamine maleate	✔								99%
Iloperidone	✔								99%+
Ziprasidone HCl	✔								98+%
Atomoxetine HCI	+ 5-HT, Ki: 77 nM								98%
Dapoxetine HCl	✔								99%+
Trazodone	✔								98+%
Clomipramine HCl	✔								99%+
Mirtazapine	✔								99+%
Escitalopram oxalate	+++ 5-HT, Ki: 0.89 nM								99%+
Duloxetine	✔								98+%
Sertraline HCl	++ 5-HT, Ki: 13 nM								99%+
Citalopram HBr	+++ serotonin reuptake, IC50: 1.8 nM								99%+
Latrepirdine 2HCl	✔							GluR	99%+
Fluoxetine hydrochloride	✔								98%
Paroxetine hydrochloride	✔							AChR	99%+
BMY 7378		++ 5-HT1D, pIC50: 5.9 5-HT1A, pIC50: 6.4	+ 5-HT2, pIC50: 5.5						97%
Flibanserin		+++ 5-HT1A, Ki: 1 nM	+ 5-HT2A, Ki: 49 nM						98%
LY310762		+ 5-HT1D, Ki: 249 nM							99%+
Cyclobenzaprine HCI			✔						99%
Blonanserin			+++ 5-HT2, Ki: 3.98 nM						99%+
Cyproheptadine HCl			++++ 5-HT2, IC50: 0.6 nM						99+%
Olanzapine			✔						99+%
Pimavanserin hemitartrate			+++ 5-HT2A, pIC50: 8.7						99%
Ketanserin			+++ 5-HT2C (Human), Ki: 2.5 nM 5-HT2C (Rat), Ki: 50 nM						99%+
Loxapine succinate			++ 5-HT2 (bovine), Ki: 6.6 nM 5-HT2 (human), Ki: 6.8 nM						99%
Agomelatine			✔						99%+
Clozapine			✔						99%+
Amitriptyline			+ 5-HT2, Ki: 235 nM					SERT	98%
PRX-08066 maleate			+++ 5-HT2B, IC50: 3.4 nM						98+%
RS-127445			++++ 5-HT2B, pKi: 9.5 5-HT2B, pIC50: 10.4						99%+
Sarpogrelate HCl			++++ 5-HT2A, Kd: 2.1 nM 5-HT2C, Kd: 1.1 nM						98%
Tropisetron				✔					99%
Palonosetron				✔					98+%
Ramosetron HCl				++++ 5-HT3 receptor, Ki: 0.091 nM					99%+
Ondansetron				✔					99%
Granisetron				✔					98%
Alosetron HCl				✔					98%
Ondansetron hydrochloride dihydrate				✔					99%+
VUF10166				++++ 5-HT3AB, Ki: 22 nM 5-HT3A, Ki: 0.04 nM					99%+
Azasetron hydrochloride				++++ 5-HT3, IC50: 0.33 nM					98%
Asenapine maleate		+++ 5-HT1B, pKi: 8.4 5-HT1A, pKi: 8.6	++++ 5-HT2A, pKi: 9.75 5-HT2C, pKi: 10.46		+++ 5-HT5A, pKi: 8.84	++++ 5-HT6, pKi: 9.6	++++ 5-HT7, pKi: 9.94		99%+
Risperidone		++ 5-HT1B, Ki: 14.9 nM 5-HT1D, Ki: 84.6 nM	++++ 5-HT2A, Ki: 61.9 nM 5-HT2C, Ki: 12 nM		+ 5-HT5A, Ki: 206 nM		++ 5-HT7, Ki: 6.6 nM		99%+
SB 271046 HCl						+++ 5-HT6, pKi: 8.92			99%+
Intepirdine						++++ 5-HT6, pKi: 9.63			99%+
SB-269970 HCl							++ 5-HT7, pKi: 8.3		98+%
BRL 15572		++ 5-HT1B, pKi: 6.1 5-HT1D, pKi: 6	++ 5-HT2A, pKi: 6.6 5-HT2B, pKi: 6.2			+ 5-HT6, pKi: 5.9	+ 5-HT7, pKi: 6.3		98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Azasetron hydrochloride 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].

Azasetron hydrochloride 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.

Azasetron hydrochloride 实验方案

计算器

存储液制备

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

Azasetron hydrochloride 技术信息

CAS号	123040-16-4
分子式	C₁₇H₂₁Cl₂N₃O₃
分子量	386.273

别名	阿扎司琼盐酸盐 ;Y-25130 hydrochloride;Azasetron (hydrochloride);Y-25130;Y-25130 HCl;Azasetron HCl
运输	蓝冰

存储条件

粉末 Sealed in dry,Room Temperature

液体 -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

动物实验配方

盐酸阿扎司琼 /Azasetron hydrochloride 98%

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盐酸阿扎司琼 /Azasetron hydrochloride 98%

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摩尔计算器

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总药量计算器

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