Cat. No.: HY-B0002B

Ondansetron

(Synonyms: GR 38032; SN 307)

11 Cited Publications

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Based on 11 publication(s) in Google Scholar

Ondansetron (GR 38032; SN 307) is a highly selective 5-HT₃ receptor antagonist with an IC₅₀ value of 103 pM. Ondansetron exerts its antiemetic effect by antagonizing 5-HT receptors located in localized neurons in the peripheral and central nervous systems. Ondansetron can inhibit nausea and vomiting induced by chemotherapy and radiotherapy.

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Pureté: 99.40%
CAS No.: 99614-02-5
Formule: C₁₈H₁₉N₃O
Masse moléculaire:293.36

Stockage:

4°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Ondansetron Chemical Structure

CAS No.: 99614-02-5

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (11)
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target

5-HT₃ Receptor

Voir tous les produits spécifiques à Isoform 5-HT Receptor :

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	IC₅₀	>300 μM Compound: ondansetron	Inhibition of human OCT1-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay Inhibition of human OCT1-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay	[PMID: 23241029]
HEK293	IC₅₀	0.03 μM Compound: ondansetron	Inhibition of human MATE1-mediated [14]-metformin uptake expressed in HEK293 cells after 1.5 mins by scintillation counting analysis Inhibition of human MATE1-mediated [14]-metformin uptake expressed in HEK293 cells after 1.5 mins by scintillation counting analysis	[PMID: 23241029]
HEK293	IC₅₀	0.16 μM Compound: ondansetron	Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay	[PMID: 23241029]
HEK293	IC₅₀	0.16 μM Compound: ondansetron	Inhibition of human MATE2K-mediated ASP+ uptake expressed in HEK293 cells up to 500 uM after 1.5 mins by fluorescence assay Inhibition of human MATE2K-mediated ASP+ uptake expressed in HEK293 cells up to 500 uM after 1.5 mins by fluorescence assay	[PMID: 23241029]
HEK293	IC₅₀	0.3 μM Compound: ondansetron	Inhibition of human MATE2K-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay Inhibition of human MATE2K-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay	[PMID: 23241029]
HEK293	IC₅₀	0.4 μM Compound: Ondansetron	Inhibition of human ERG expressed in HEK cells by patch clamp technique Inhibition of human ERG expressed in HEK cells by patch clamp technique	[PMID: 20889341]
HEK293	IC₅₀	1.7 μM Compound: ondansetron	Inhibition of human OCT2-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay Inhibition of human OCT2-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay	[PMID: 23241029]
HEK293	IC₅₀	17.4 μM Compound: ondansetron	Inhibition of human OCT3-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay Inhibition of human OCT3-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay	[PMID: 23241029]
HEK293	IC₅₀	20.4 μM Compound: Ondansetrone	Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells by confocal microscopy Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells by confocal microscopy	[PMID: 18788725]
MDCK-II	IC₅₀	<0.01 μM Compound: ondansetron	Inhibition of human MATE1-mediated [14]-metformin uptake expressed in polarized MDCK2 cells after 5 mins by liquid scintillation counting analysis Inhibition of human MATE1-mediated [14]-metformin uptake expressed in polarized MDCK2 cells after 5 mins by liquid scintillation counting analysis	[PMID: 23241029]
Oocyte	IC₅₀	0.09 nM Compound: 3	Antagonist activity at human 5HT3A receptor expressed in xenopus oocytes assessed as inhibition of 5HT-induced effect by electrophysiological method Antagonist activity at human 5HT3A receptor expressed in xenopus oocytes assessed as inhibition of 5HT-induced effect by electrophysiological method	[PMID: 21486038]
Oocyte	IC₅₀	0.16 nM Compound: 3	Antagonist activity at rat 5HT3A receptor expressed in xenopus oocytes assessed as inhibition of 5HT-induced effect by electrophysiological method Antagonist activity at rat 5HT3A receptor expressed in xenopus oocytes assessed as inhibition of 5HT-induced effect by electrophysiological method	[PMID: 21486038]
Oocyte	IC₅₀	27 μM Compound: Ondansetron	Antagonism of ACh-evoked responses at human Nicotinic acetylcholine receptor alpha3-beta4 expressed in xenopus oocytes Antagonism of ACh-evoked responses at human Nicotinic acetylcholine receptor alpha3-beta4 expressed in xenopus oocytes	[PMID: 15050614]
Oocyte	IC₅₀	66 μM Compound: Ondansetron	Antagonism of ACh response at Nicotinic acetylcholine receptor alpha4-beta2 expressed in xenopus oocytes Antagonism of ACh response at Nicotinic acetylcholine receptor alpha4-beta2 expressed in xenopus oocytes	[PMID: 15050614]

In Vitro

Ondansetron (1-1000 μM) dose-dependently reduces the response of EAAT3 to 30 μM L-glutamate with an IC₅₀ of 8.57 μM^[9].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Ondansetron (2.4-6 mg/kg; i.p.; six times over 15 days) has a TD₅₀ value of 3.7 mg/kg and an LD₅₀ of 4.6 mg/kg^[4] in mice.
Ondansetron (2 mg/kg; i.p.; six consecutive days) exhibits anti-inflammatory effects in rats through the 5-HT₃ receptor^[8].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

NSCLC Patients Treated With Chemotherapy^[7]
Dosage:

8 mg
Administration:

Intraperitoneal Injection (i.p.)
Result:

Showed TD₅₀ and LD₅₀ doses with 3.7±0.6 mg/kg and 4.6±0.5 mg/kg, respectively.

Animal Model:

Male Swiss Mice with Colitis^[8]
Dosage:

2 mg/kg
Administration:

Intraperitoneal Injection (i.p.)
Result:

Showed dramatic reduction in MPO activity and tumor necrosis factor-alpha, interleukin-6 and interleukin-1 beta.

Chemical Information

CAS No. 99614-02-5
Appearance Solid
Masse moléculaire 293.36
Formule C₁₈H₁₉N₃O
Color White to off-white
SMILES

O=C1C(CN2C=CN=C2C)CCC(N3C)=C1C4=C3C=CC=C4
Synonyms

GR 38032; SN 307
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

4°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Publications (11)

All In Vivo Efficacy StudyIHC

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Journal Impact Factor

Adv Sci (Weinh)

The Locus Coeruleus-Periaqueductal Gray GABAergic Projection Regulates Comorbid Pain and Depression. [Abstract]

2025 Jul;12(26):e2503739. PMID: 40192524
J Ethnopharmacol

Phytomedicine Fructus Aurantii-derived two absorbed compounds unlock antidepressant and prokinetic multi-functions via modulating 5-HT3/GHSR. [Abstract]

2024 Apr 6:323:117703. PMID: 38185260

Ondansetron purchased from MedChemExpress. Usage Cited in: J Ethnopharmacol. 2024 Apr 6:323:117703. [Abstract]

Ondansetron (1 mg/kg; IP) had no impact on immobility time compared with the model group in rats.

Ondansetron purchased from MedChemExpress. Usage Cited in: J Ethnopharmacol. 2024 Apr 6:323:117703. [Abstract]

Ondansetron (1 mg/kg; IP) alone did not affect GE (gastric emptying) and IT (intestinal transit), overturning the gastrointestinal efficacy of hesperidin (MH).

Ondansetron purchased from MedChemExpress. Usage Cited in: J Ethnopharmacol. 2024 Apr 6:323:117703. [Abstract]

Ondansetron (1 mg/kg; IP) reversed the rise in 5-HT3 compared to the hesperidin (MH) group (68.42 ± 4.05 vs 78.85 ± 3.28 ng/mL).
Int J Pharm

Formulation and development of pH-independent/dependent sustained release matrix tablets of ondansetron HCl by a continuous twin-screw melt granulation process. [Abstract]

2015 Dec 30;496(1):33-41. PMID: 25863118
Front Pharmacol

The therapeutic targets and signaling mechanisms of ondansetron in the treatment of critical illness in the ICU. [Abstract]

2024 Aug 21:15:1443169. PMID: 39234104
Eur J Pharm Sci

Investigating the relevance of CYP2J2 inhibition for drugs known to cause intermediate to high risk torsades de pointes. [Abstract]

2023 Aug 1:187:106475. PMID: 37225005
Biomedicines

Ferroptosis in Septic Cardiomyopathy Is Alleviated by Ondansetron: The Critical Role of the HTR3A-ATF3 Axis in Mitochondrial and Oxidative Homeostasis. [Abstract]

2026 May 3;14(5):1040. PMID: 42193366
Prog Neuropsychopharmacol Biol Psychiatry

Baicalein exerts anxiolytic and antinociceptive effects in a mouse model of posttraumatic stress disorder: Involvement of the serotonergic system and spinal delta-opioid receptors. [Abstract]

2023 Mar 2:122:110689. PMID: 36462602
J Radiat Res Appl Sci

2023 Dec, 16(4), 100682.

Ondansetron purchased from MedChemExpress. Usage Cited in: J Radiat Res Appl Sci. 2023 Dec, 16(4), 100682.

Ondansetron (ODN; 2 mg/kg; subcutaneously; 0-120 min) produced significant analgesia in both the Tail flick (TF) and hot plate (HP) tests compared with saline in rats.

Ondansetron purchased from MedChemExpress. Usage Cited in: J Radiat Res Appl Sci. 2023 Dec, 16(4), 100682.

Ondansetron (ODN; 2 mg/kg; subcutaneously) decreased 5-HT3A immunoreactivity in rats dorsal root ganglia.
Biochem Biophys Res Commun

Dual-cardiotoxicity evaluation of torsadogenic risk drugs using human iPSC-derived cardiomyocytes. [Abstract]

2025 Oct 30:786:152756. PMID: 41043280
SSRN

2023 Srep 5.
Patent

US20170319486A1.

Solvant et solubilité

In Vitro:

DMSO : 10 mg/mL (34.09 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

3.4088 mL

17.0439 mL

34.0878 mL

5 mM

0.6818 mL

3.4088 mL

6.8176 mL

10 mM

0.3409 mL

1.7044 mL

3.4088 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Calculateur de molarité

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 1 mg/mL (3.41 mM); Clear solution

This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: 1 mg/mL (3.41 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 1 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 1 mg/mL (3.41 mM); Clear solution

This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

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Instruction de manipulation (2659 KB)

Références

[1]. Brown AM, 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. [Content Brief]

[2]. Barann M, et al. Recombinant human 5-HT3A receptors in outside-out patches of HEK 293 cells: basic properties and barbiturate effects. Naunyn Schmiedebergs Arch Pharmacol. 2000 Sep;362(3):255-65. [Content Brief]

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

[4]. Khedhaier A, et al. Circadian rhythms in toxic effects of the serotonin antagonist ondansetron in mice. Chronobiol Int. 2003 Nov;20(6):1103-16. [Content Brief]

[5]. Umathe SN, et al. The 5-HT3 receptor antagonist, ondansetron, blocks the development and expression of ethanol-induced locomotor sensitization in mice. Behav Pharmacol. 2009 Feb;20(1):78-83. [Content Brief]

[6]. Doggrell SA, et al. Cardiac safety concerns for ondansetron, an antiemetic commonly used for nausea linked to cancer treatment and following anaesthesia. Expert Opin Drug Saf. 2013 May;12(3):421-31. [Content Brief]

[7]. Xin Wang, et al. Effectiveness of Olanzapine Combined with Ondansetron in Prevention of Chemotherapy-Induced Nausea and Vomiting of Non-small Cell Lung Cancer. Cell Biochem Biophys. 2015 Jun;72(2):471-3. [Content Brief]

[8]. Azadeh Motavallian-Naeini, et al. Anti-inflammatory effect of ondansetron through 5-HT3 receptors on TNBS-induced colitis in rat. EXCLI J2012 Feb 22:11:30-44. eCollection 2012. [Content Brief]

[9]. 허원석. Effects of ondansetron on the activity of glutamate transporter type 3 and the modulation mechanism[D]. 서울대학교 대학원, 2014.

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	3.4088 mL	17.0439 mL	34.0878 mL	85.2195 mL
	5 mM	0.6818 mL	3.4088 mL	6.8176 mL	17.0439 mL
	10 mM	0.3409 mL	1.7044 mL	3.4088 mL	8.5220 mL
	15 mM	0.2273 mL	1.1363 mL	2.2725 mL	5.6813 mL
	20 mM	0.1704 mL	0.8522 mL	1.7044 mL	4.2610 mL
	25 mM	0.1364 mL	0.6818 mL	1.3635 mL	3.4088 mL
	30 mM	0.1136 mL	0.5681 mL	1.1363 mL	2.8407 mL

Keywords

Ondansetron

11 Cited Publications

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Ondansetron

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Publications Citing Use of MedChemExpress (MCE) Ondansetron

Voir tous les produits spécifiques à Isoform 5-HT Receptor

Activité biologique

Chemical Information

Publications (11)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Ondansetron Related Classifications

HY-B0002B Related Classifications