Ondansetron (Synonyms: GR 38032F, NSC 665799) |
Catalog No.GC16142
One-Click Copy Product Info
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Ondansetron, a carbazole derivative, is a competitive and selective antagonist of serotonin 5-HT3 receptors with an IC50 value of 103pM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 99614-02-5
Sample solution is provided at 25 µL, 10mM.
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Ondansetron, a carbazole derivative, is a competitive and selective antagonist of serotonin 5-HT3 receptors with an IC50 value of 103pM[1]. Ondansetron inhibits the mobilization of intracellular Ca2+, the production of thromboxane B2, and the release of ATP by weakening the IP3 signaling pathway and the MAPK (p38 and ERK2) pathway, which prevents platelet aggregation[2]. Ondansetron has been widely used as an antiemetic for cancer treatment-induced and anesthesia-related nausea and vomiting[3].
In vitro, Ondansetron incubation (1µM) for 4 hours significantly reduced the 1µg/ml lipopolysaccharide (LPS)-stimulated production of inflammatory factors (IL-6, IL-1β, TNF-α) and the chemokine receptor CXCR4 in rat neutrophils[4]. Treatment with 10µM Ondansetron for 3 minutes reduced the activity of the excitatory amino acid transporter 3 (EAAT3) expressed in Xenopus oocytes[5]. Treatment with 10µM Ondansetron for 24 hours increased the secretion of apolipoprotein E (apoE) in mouse astrocytes and elevated the levels of ABCA1 mRNA and protein[6].
In vivo, Ondansetron treatment via intraperitoneal injection at a dose of 1.5mg/kg/day for 6 days increased the survival time of mice infected with Enterovirus 71 and reduced the viral load in various tissues[7]. Daily intraperitoneal injection of Ondansetron (2mg/kg) for 6 days alleviated the trinitrobenzene sulfonic acid (TNBS)-induced colitis in rats and reduced the levels of inflammatory cytokines in the colon[8]. Intraperitoneal injection of Ondansetron (1mg/kg/day) for 5 days improved the cognitive function of epileptic rats, attenuated hippocampal impairment, stabilized the synaptic cytoskeleton structure of the hippocampus, and regulated plasticity[9].
References:
[1] Brown A M, Hope A G, Lambert J J, et al. Ion permeation and conduction in a human recombinant 5-HT3 receptor subunit (h5-HT3A)[J]. The Journal of Physiology, 1998, 507(Pt 3): 653.
[2] Liu F C, Liou J T, Liao H R, et al. The anti-aggregation effects of ondansetron on platelets involve IP3 signaling and MAP kinase pathway, but not 5-HT3-dependent pathway[J]. Thrombosis Research, 2012, 130(3): e84-e94.
[3] Ye J H, Ponnudurai R, Schaefer R. Ondansetron: a selective 5‐HT3 receptor antagonist and its applications in CNS‐related disorders[J]. CNS drug reviews, 2001, 7(2): 199-213.
[4] Tao L, Zhang Z, Li C, et al. The therapeutic targets and signaling mechanisms of ondansetron in the treatment of critical illness in the ICU[J]. Frontiers in Pharmacology, 2024, 15: 1443169.
[5] Hur W, Lee M K, Park H P, et al. Ondansetron attenuates the activity of excitatory amino acid transporter type 3 expressed in Xenopus oocytes[J]. European Journal of Pharmacology, 2014, 733: 7-12.
[6] Shinohara M, Shinohara M, Zhao J, et al. 5-HT3 antagonist ondansetron increases apoE secretion by modulating the LXR-ABCA1 pathway[J]. International journal of molecular sciences, 2019, 20(6): 1488.
[7] Li Z, Rui J, Li J, et al. Ondansetron exhibits potent antiviral activity against enterovirus 71 infection in vitro and in vivo[J]. Virus Research, 2026: 199771.
[8] Motavallian-Naeini A, Minaiyan M, Rabbani M, et al. Anti-inflammatory effect of ondansetron through 5-HT3 receptors on TNBS-induced colitis in rat[J]. EXCLI journal, 2012, 11: 30.
[9] Zhang Y, Sun Y, Gao J, et al. Ondansetron reduces seizures and improves cognitive impairment in a rat model of temporal lobe epilepsy[J]. IBRO Neuroscience Reports, 2025.
| Cell experiment [1]: | |
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Cell lines |
REH cells |
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Preparation Method |
REH cells were cultured in RPMI-1640 medium supplemented with 100μg/ml streptomycin, 100μg/ml penicillin, and 10% fetal bovine serum, at 37°C in an incubator with 5% CO2. REH cells in the logarithmic growth phase were cultured in 24-well culture plates at cell concentrations of 2×104 cells/ml (1ml/well) in RPMI-1640 Medium. After 24h, cells were treated with different concentrations of Ondansetron (0, 10, 20, 30, 40, and 50µM) for 72h and cell viability was measured. |
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Reaction Conditions |
0, 10, 20, 30, 40, and 50µM; 72h |
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Applications |
Ondansetron reduced cell viability in REH cells in a dose-dependent manner. |
| Animal experiment [2]: | |
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Animal models |
Male Wistar rats |
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Preparation Method |
Male Wistar rats (250±20g; 12-week-old) were housed in groups of 6, under controlled temperature (23±1°C), relative humidity (55±10%), and lighting conditions (12/12 hours light/dark) and fed standard pelleted chow and water ad libitum. Rats were randomly divided into the following groups of 6 rats in each: (I) TNBS-control group: 2 hours subsequent to induction of colitis, normal saline was administered intraperitoneally (i.p.); (II) normal group: rectal cannulation proceeded without induction of colitis, receiving normal saline (0.25ml/rat) in lieu of TNBS; (III) Dexamethasone group: 2 hours subsequent to induction of colitis, dexamethasone (1mg/kg) was administered i.p.; (IV) Ondansetron group: 2 hours subsequent to induction of colitis, Ondansetron (2mg/kg; i.p.) was given, and continued daily for six days. Rats were sacrificed by means of ether inhalation on day 6. The abdomen was opened and the colon was then examined. |
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Dosage form |
2mg/kg/day; 6 days; i.p. |
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Applications |
Ondansetron treatment reduced colonic damage, neutrophil infiltration and colonic levels of pro-inflammatory cytokines in the TNBS model of rat colitis. |
References: [1] Prada J, Shalapour S, Pfau M, et al. Antiproliferative effect of the serotonin receptor antagonist ondansetron in the acute lymphoblastic leukemia cell line REH[J]. Acta Oncologica, 2011, 50(4): 591-592. [2] Motavallian-Naeini A, Minaiyan M, Rabbani M, et al. Anti-inflammatory effect of ondansetron through 5-HT3 receptors on TNBS-induced colitis in rat[J]. EXCLI journal, 2012, 11: 30. | |
| Cas No. | 99614-02-5 | SDF | |
| Synonyms | GR 38032F, NSC 665799 | ||
| Chemical Name | 9-methyl-3-[(2-methylimidazol-1-yl)methyl]-2,3-dihydro-1H-carbazol-4-one | ||
| Canonical SMILES | CC1=NC=CN1CC2CCC3=C(C2=O)C4=CC=CC=C4N3C | ||
| Formula | C18H19N3O | M.Wt | 293.36 |
| Solubility | ≥ 7.3mg/mL in DMSO | Storage | Store at RT, protect from light |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.4088 mL | 17.0439 mL | 34.0878 mL |
| 5 mM | 681.8 μL | 3.4088 mL | 6.8176 mL |
| 10 mM | 340.9 μL | 1.7044 mL | 3.4088 mL |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Quality Control & SDS
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- Purity: >99.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 8 reference(s) in Google Scholar.)