Ondansetron (Synonyms: GR 38032; SN 307)

Name: Ondansetron
Brand: MedChemExpress
SKU: HY-B0002B
Rating: 5.0 (8 reviews)

Cat. No.: HY-B0002B Purity: 99.37%: FAQs
Data Sheet SDS COA Handling Instructions

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Ondansetron (GR 38032; SN 307) is a highly selective 5-HT₃ receptor antagonist, with IC₅₀ value of 103 pM. Ondansetron exerts antiemetic effects by antagonizing 5-HT receptor located on local neurons in the peripheral and central nervous system. Ondansetron suppresses nausea and vomiting caused by chemotherapy and radiation therapy. Ondansetron has orally bioactivity.

For research use only. We do not sell to patients.

Ondansetron Chemical Structure

CAS No. : 99614-02-5

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 66	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 66	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 38	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 60	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 72	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 84	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Based on 8 publication(s) in Google Scholar

Other Forms of Ondansetron:

Ondansetron hydrochloride dihydrate In-stock
Ondansetron-d₅ Get quote
Ondansetron-d₃ Get quote
Ondansetron-¹³C,d₃ Get quote
Ondansetron hydrochloride Get quote
Ondansetron (Standard) Get quote

8 Publications Citing Use of MCE Ondansetron

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View All 5-HT Receptor Isoform Specific Products:

View All Isoforms

5-HT₁ Receptor 5-HT₂ Receptor 5-HT₃ Receptor 5-HT₄ Receptor 5-HT₅ Receptor 5-HT₆ Receptor 5-HT₇ Receptor 5-HT Receptor

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

5-HT₃ 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 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	0.16 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	0.3 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]

In Vivo

Ondansetron (GR 38032; SN 307) (2.4-6 mg/kg; i.p.; six times in 15 D) has TD₅₀ with the value of 3.7±0.6 mg/kg, and LD₅₀ of 4.6±0.5 mg/kg in mice^[4].
Ondansetron (8 mg; i.p.; 1 time) with Olanzapine (HY-14541) has better effectiveness in preventing CINV in NSCLC patients, particularly for the delayed type^[7].
Ondansetron (2 mg/kg; i.p.; six consecutive days) exhibits anti-inflammatory effect through 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.

Clinical Trial

Molecular Weight

293.36

Formula

C₁₈H₁₉N₃O

CAS No.

99614-02-5

Appearance

Solid

Color

White to off-white

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light

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

Solvent & Solubility

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

View the Complete Stock Solution Preparation Table

* 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.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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

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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

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

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.37%

Select Batch:

Data Sheet (281 KB) SDS (725 KB)

COA (252 KB) LCMS (93 KB)

Handling Instructions (2659 KB)

References

[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]

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

Ondansetron Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Ondansetron99614-02-5GR 38032 SN 307GR38032GR-38032SN307SN 307SN-3075-HT ReceptorSerotonin Receptor5-hydroxytryptamine Receptor5-HT Receptor AntagonistAntiemeticInhibitorinhibitorinhibit

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Ondansetron (Synonyms: GR 38032; SN 307)

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8 Publications Citing Use of MCE Ondansetron

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References

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Complete Stock Solution Preparation Table

Ondansetron Related Classifications

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