1. GPCR/G Protein Neuronal Signaling
  2. 5-HT Receptor
  3. Ondansetron

Ondansetron  (Synonyms: GR 38032; SN 307)

Cat. No.: HY-B0002B Purity: 99.40%
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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.

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

CAS No. : 99614-02-5

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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10 mM * 1 mL in DMSO In-stock
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Customer Review

Based on 10 publication(s) in Google Scholar

Top Publications Citing Use of Products

    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).

    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.
    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    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[1][2][3][4][5][6][7][8].

    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 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.
    Molecular Weight

    293.36

    Formula

    C18H19N3O

    CAS No.
    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
    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)

    Mass
    =
    Concentration
    ×
    Volume
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    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

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    Volume (final)

    V2

    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.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    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
    References

    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.

    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
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      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.

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    Product Name:
    Ondansetron
    Cat. No.:
    HY-B0002B
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