Ondansetron hydrochloride dihydrate | GR 38032 hydrochloride dihydrate;SN 307 hydrochloride dihydrate;Ondansetron (hydrochloride hydrate) | 昂丹司琼盐酸盐二水合物 | 5-HT Receptor

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Ondansetron HCl dihydrate/盐酸昂丹司琼二水物 {[allProObj[0].p_purity_real_show]}

货号：A344767 同义名： 昂丹司琼盐酸盐二水合物 / GR 38032 hydrochloride dihydrate; SN 307 hydrochloride dihydrate

Ondansetron HCl ·2H2O是一种竞争性 5-HT3 受体拮抗剂。

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Ondansetron HCl dihydrate/盐酸昂丹司琼二水物化学结构
CAS号：103639-04-9

Ondansetron HCl dihydrate/盐酸昂丹司琼二水物 3D分子结构
CAS号：103639-04-9

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Ondansetron HCl dihydrate/盐酸昂丹司琼二水物纯度/质量文件产品仅供科研

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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								98%
Venlafaxine	✔								99%
Fluvoxamine maleate	✔								99%
Iloperidone	✔								99%
Ziprasidone HCl	✔								98+%
Atomoxetine HCI	+ 5-HT, Ki: 77 nM								98%
Dapoxetine HCl	✔								97%
Trazodone	✔								98+%
Clomipramine HCl	✔								98%
Mirtazapine	✔								99+%
Escitalopram oxalate	+++ 5-HT, Ki: 0.89 nM								97%
Duloxetine	✔								97%
Sertraline HCl	++ 5-HT, Ki: 13 nM								98%
Citalopram HBr	+++ serotonin reuptake, IC50: 1.8 nM								98%
Latrepirdine 2HCl	✔							GluR	99%
Fluoxetine HCl	✔								99.5%
Paroxetine HCl	✔							AChR	99%
BMY 7378		++ 5-HT1A, pIC50: 6.4 5-HT1D, pIC50: 5.9	+ 5-HT2, pIC50: 5.5						97%
Flibanserin		+++ 5-HT1A, Ki: 1 nM	+ 5-HT2A, Ki: 49 nM						95%
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 (human), Ki: 6.8 nM 5-HT2 (bovine), Ki: 6.6 nM						98%
Agomelatine			✔						98%
Clozapine			✔						98%
Amitriptyline			+ 5-HT2, Ki: 235 nM					SERT	99%
PRX-08066 maleate			+++ 5-HT2B, IC50: 3.4 nM						98+%
RS-127445			++++ 5-HT2B, pIC50: 10.4 5-HT2B, pKi: 9.5						99%+
Sarpogrelate HCl			++++ 5-HT2C, Kd: 1.1 nM 5-HT2A, Kd: 2.1 nM						98%
Tropisetron				✔					99%
Ramosetron HCl				++++ 5-HT3 receptor, Ki: 0.091 nM					98%
Ondansetron				✔					99%
Granisetron				✔					98%
Alosetron HCl				✔					98%
Ondansetron HCl dihydrate				✔					98%
VUF10166				++++ 5-HT3A, Ki: 0.04 nM 5-HT3AB, Ki: 22 nM					99%+
Azasetron HCl				++++ 5-HT3, IC50: 0.33 nM					99%
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		97%
Risperidone		++ 5-HT1D, Ki: 84.6 nM 5-HT1B, Ki: 14.9 nM	++++ 5-HT2A, Ki: 61.9 nM 5-HT2C, Ki: 12 nM		+ 5-HT5A, Ki: 206 nM		++ 5-HT7, Ki: 6.6 nM		98%
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-HT1D, pKi: 6 5-HT1B, pKi: 6.1	++ 5-HT2A, pKi: 6.6 5-HT2B, pKi: 6.2			+ 5-HT6, pKi: 5.9	+ 5-HT7, pKi: 6.3		95%
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。

Ondansetron HCl dihydrate/盐酸昂丹司琼二水物生物活性

靶点

5-HT3

5-HT3 receptor, IC50:810 nM
5-HT3

描述

Ondansetron Hydrochloride Dihydrate is the hydrated state of Ondansetron hydrochloride. Ondansetron is a selective 5-hydroxytryptamine3 (5-HT3) receptor antagonist as an antiemetic for cancer treatment-induced and anesthesia-related nausea and vomiting^[3]. 5-HT evoked transient inward currents (EC₅₀ = 3.4 mM; Hill coefficient = 1.8) that were blocked by the 5-HT3 receptor antagonist ondansetron (IC50 = 103 pM)^[4]. Indirect stimulation of nicotinic acetylcholine receptor by ondansetron can improve the auditory gating parameters of DBA/2 mice^[5]. Different doses of ondansetron were injected intraperitoneally (i.p.) at fixed times during the day to determine both the sublethal (TD50) and lethal (LD50) doses, which were, 3.7 +/- 0.6 mg/kg and 4.6 +/- 0.5 mg/kg, respectively^[6].

Ondansetron HCl dihydrate/盐酸昂丹司琼二水物细胞实验

Cell Line HEK-293 cells overexpressing mMate1 HEK-293 cells overexpressing mOct2 HEK-293 cells overexpressing hMATE2-K HEK-293 cells overexpressing hMATE1 HEK-293 cells overexpressing hOCT2	Concentration	Treated Time	Description	References
HEK-293 cells overexpressing mMate1	0-50 µM	10 minutes	Determine the inhibitory potency of ondansetron on mMate1, Ki value was 0.07 μM	Toxicol Appl Pharmacol. 2013 Nov 15;273(1):100-9
HEK-293 cells overexpressing mOct2	0-50 µM	10 minutes	Determine the inhibitory potency of ondansetron on mOct2, Ki value was 3.5 μM	Toxicol Appl Pharmacol. 2013 Nov 15;273(1):100-9
HEK-293 cells overexpressing hMATE2-K	0-50 µM	10 minutes	Determine the inhibitory potency of ondansetron on hMATE2-K, Ki value was 0.015 μM	Toxicol Appl Pharmacol. 2013 Nov 15;273(1):100-9
HEK-293 cells overexpressing hMATE1	0-50 µM	10 minutes	Determine the inhibitory potency of ondansetron on hMATE1, Ki value was 0.035 μM	Toxicol Appl Pharmacol. 2013 Nov 15;273(1):100-9
HEK-293 cells overexpressing hOCT2	0-50 µM	10 minutes	Determine the inhibitory potency of ondansetron on hOCT2, Ki value was 3.85 μM	Toxicol Appl Pharmacol. 2013 Nov 15;273(1):100-9

Ondansetron HCl dihydrate/盐酸昂丹司琼二水物动物实验

Species New Zealand white rabbits Mice	Animal Model Heart failure model Wild-type and Mate1−/− mice	Administration	Dosage	Frequency	Description	References
New Zealand white rabbits	Heart failure model	Perfusion	100 nM	Single administration	To investigate the effects of Ondansetron on action potential duration (APD) and QT interval in rabbit hearts with heart failure, showing that Ondansetron significantly prolonged APD and QT interval and increased ventricular fibrillation vulnerability.	Heart Rhythm. 2020 Feb;17(2):332-340
Mice	Wild-type and Mate1−/− mice	Intraperitoneal injection	6.4 mg/kg	Single dose	Evaluate the effect of ondansetron on cisplatin-induced nephrotoxicity, results showed ondansetron enhanced cisplatin nephrotoxicity via inhibition of Mate1	Toxicol Appl Pharmacol. 2013 Nov 15;273(1):100-9

Ondansetron HCl dihydrate/盐酸昂丹司琼二水物参考文献

[1]Wildeboer KM, Zheng L, et al. Ondansetron results in improved auditory gating in DBA/2 mice through a cholinergic mechanism. Brain Res. 2009 Dec 1;1300:41-50.

[2]Brown AM, Hope AG, et al. Ion permeation and conduction in a human recombinant 5-HT3 receptor subunit (h5-HT3A). J Physiol. 1998 Mar 15;507 ( Pt 3):653-65.

[3]Ye JH, Ponnudurai R, Schaefer R. Ondansetron: a selective 5-HT(3) receptor antagonist and its applications in CNS-related disorders. CNS Drug Rev. 2001 Summer;7(2):199-213. doi: 10.1111/j.1527-3458.2001.tb00195.x. PMID: 11474424; PMCID: PMC6741689.

[4]Brown AM, Hope AG, Lambert JJ, Peters JA. Ion permeation and conduction in a human recombinant 5-HT3 receptor subunit (h5-HT3A). J Physiol. 1998 Mar 15;507 ( Pt 3)(Pt 3):653-65. doi: 10.1111/j.1469-7793.1998.653bs.x. PMID: 9508827; PMCID: PMC2230823.

[5]Wildeboer KM, Zheng L, Choo KS, Stevens KE. Ondansetron results in improved auditory gating in DBA/2 mice through a cholinergic mechanism. Brain Res. 2009 Dec 1;1300:41-50. doi: 10.1016/j.brainres.2009.08.075. Epub 2009 Sep 1. PMID: 19728991; PMCID: PMC2784252.

[6]Khedhaier A, Ben Attia M, Gadacha W, Sani M, Bouzouita K, Chouchane L, Mechkouri M, Reinberg A, Boughattas NA. Circadian rhythms in toxic effects of the serotonin antagonist ondansetron in mice. Chronobiol Int. 2003 Nov;20(6):1103-16. doi: 10.1081/cbi-120025532. PMID: 14680146.

Ondansetron HCl dihydrate/盐酸昂丹司琼二水物实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.73mL

0.55mL

0.27mL

13.67mL

2.73mL

1.37mL

27.33mL

5.47mL

2.73mL

Ondansetron HCl dihydrate/盐酸昂丹司琼二水物技术信息

CAS号	103639-04-9
分子式	C₁₈H₂₄ClN₃O₃
分子量	365.85
SMILES Code	O=C1C(CN2C=CN=C2C)CCC(N3C)=C1C4=C3C=CC=C4.[H]Cl.[H]O[H].[H]O[H]
MDL No.	MFCD00374371

别名	昂丹司琼盐酸盐二水合物 ;GR 38032 hydrochloride dihydrate; SN 307 hydrochloride dihydrate; Ondansetron (hydrochloride hydrate)
运输	蓝冰
InChI Key	VRSLTNZJOUZKLX-UHFFFAOYSA-N
Pubchem ID	59774

存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Sealed in dry, store in freezer, under -20°C

溶解方案

细胞实验：

DMSO: 105 mg/mL(287 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: 15 mg/mL(41 mM)，配合低频超声助溶

动物实验：请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用；以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

方案一

方案二

CHO cells	Function assay	Inhibition of human ERG expressed in CHO cells by whole cell patch clamp technique, IC50=0.81283 μM	18448342
HEK cells	Function assay	Inhibition of human ERG expressed in HEK cells by patch clamp technique, IC50=0.4 μM	20889341
HEK293 cells	Function assay	Displacement of [3H]granisetron from human 5HT3A receptor expressed in HEK293 cells by filter binding assay, Ki=0.0028 μM	21486038
MDCK2 cells	Function assay	Inhibition of human MATE1-mediated [14]-metformin uptake expressed in polarized MDCK2 cells after 5 mins by liquid scintillation counting analysis, IC50=0.01 μM	23241029

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Ondansetron HCl dihydrate/盐酸昂丹司琼二水物生物活性

Ondansetron HCl dihydrate/盐酸昂丹司琼二水物细胞实验

Ondansetron HCl dihydrate/盐酸昂丹司琼二水物动物实验

Ondansetron HCl dihydrate/盐酸昂丹司琼二水物参考文献

Ondansetron HCl dihydrate/盐酸昂丹司琼二水物实验方案

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Ondansetron HCl dihydrate/盐酸昂丹司琼二水物 质控信息

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Ondansetron HCl dihydrate/盐酸昂丹司琼二水物 细胞实验

Ondansetron HCl dihydrate/盐酸昂丹司琼二水物 动物实验

Ondansetron HCl dihydrate/盐酸昂丹司琼二水物 参考文献

Ondansetron HCl dihydrate/盐酸昂丹司琼二水物 实验方案

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Ondansetron HCl dihydrate/盐酸昂丹司琼二水物质控信息

Ondansetron HCl dihydrate/盐酸昂丹司琼二水物生物活性

Ondansetron HCl dihydrate/盐酸昂丹司琼二水物细胞实验

Ondansetron HCl dihydrate/盐酸昂丹司琼二水物动物实验

Ondansetron HCl dihydrate/盐酸昂丹司琼二水物参考文献

Ondansetron HCl dihydrate/盐酸昂丹司琼二水物实验方案

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