| Size | Price | Stock | Qty |
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| 250mg |
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| 500mg |
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| Other Sizes |
| Targets |
5-HT3 Receptor
Ondansetron hydrochloride dihydrate targets the serotonin 5-HT3 receptor. It is a selective and competitive antagonist of the 5-HT3 receptor. 5-HT3 receptors are ligand-gated ion channels that mediate the emetic response. By blocking 5-HT3 receptors, ondansetron inhibits the effects of serotonin released from enterochromaffin cells in the gastrointestinal tract, thereby preventing nausea and vomiting. |
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| ln Vitro |
In vitro, Ondansetron hydrochloride dihydrate acts as a selective 5-HT3 receptor antagonist. Its activity is typically assessed by measuring its ability to inhibit 5-HT-induced ion flux or calcium influx in cells expressing 5-HT3 receptors. The compound has been used as a 5-HT3 antagonist to attenuate rostroventromedial medulla (RVM)/cholecystokinin (CCK)-induced mechanical hypersensitivity and to block the effects of trichostatin A (TSA) on 5-HT3 protein. Standard in vitro assays include receptor binding studies using radiolabeled ligands such as [3H]-GR65630 and functional assays measuring ion flux.
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| ln Vivo |
In the radiation-induced pica model, ondansetron hydrochloride dehydrate (2 mg/kg; ip; single) prevents radiation sickness when combined with dexamethasone (2 mg/kg) and CP-99,994 (15 mg/kg)[1].
In vivo, Ondansetron hydrochloride dihydrate is used clinically to prevent nausea and vomiting caused by cancer chemotherapy, radiation therapy, and surgery. It is orally bioavailable and blood-brain barrier permeable. The compound is well tolerated with few side effects; headache, constipation, and dizziness are the most commonly reported side effects. It has also been used in research to study the role of 5-HT3 receptors in various physiological and pathological processes. |
| Enzyme Assay |
For non-cell-based receptor binding assays, Ondansetron hydrochloride dihydrate can be evaluated using membrane preparations from cells expressing human 5-HT3 receptors. Radioligand binding displacement experiments are performed using a suitable radiolabeled ligand such as [3H]-GR65630 or [3H]-LY278584. Membrane homogenates are incubated with increasing concentrations of the test compound and a fixed concentration of the radioligand at room temperature for 60-90 minutes. Bound radioligand is separated from free by rapid filtration through glass fiber filters. Non-specific binding is determined in the presence of excess unlabeled ondansetron or MDL-72222. Ki values are calculated from displacement curves using nonlinear regression analysis.
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| Cell Assay |
For in vitro cellular assays, cells expressing human 5-HT3 receptors (e.g., HEK293 cells) are cultured in appropriate media. For functional assays, calcium influx is measured using fluorescent calcium indicators such as Fluo-4 AM. Cells are loaded with the dye and pre-incubated with various concentrations of Ondansetron hydrochloride dihydrate. Receptor activation is stimulated by the addition of a 5-HT3 receptor agonist such as 5-HT or m-CPBG. Fluorescence intensity is measured using a fluorescence plate reader. The reduction in calcium signal compared to control wells indicates antagonist activity. IC50 values are calculated from dose-response curves.
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| Animal Protocol |
Animal/Disease Models: Male mice of ICR strain (8weeks old; 30-36 g; radiation-induced pica model (kaolin ingestion behavior “pica” may be analogous to nausea and vomiting in mice))[1].
Doses: 2 mg/kg Route of Administration: intraperitoneal (ip) injection; single. Experimental Results: Slightly decreased the radiation-induced kaolin consumption by dexamethasone to 48% of the control. demonstrated good activity of blocking radiation sickness by combining with Dexamethasone (2 mg/kg) and CP-99,994 (15 mg /kg). For in vivo animal studies, Ondansetron hydrochloride dihydrate can be administered to rodents via oral gavage or intraperitoneal injection. In models of emesis, the compound's ability to prevent vomiting or retching is assessed. In models of chemotherapy-induced nausea, behavioral and physiological parameters are evaluated. In pain models, the compound's effects on hypersensitivity are assessed. Dosing regimens vary depending on the specific model and desired exposure levels. Blood and tissue samples may be collected for pharmacokinetic analysis. |
| ADME/Pharmacokinetics |
Metabolism / Metabolites
Liver half-life: 5.7 hours Ondansetron hydrochloride dihydrate has a molecular weight of 365.86 and a molecular formula of C18H19N3O·HCl·2H2O. It is orally bioavailable and blood-brain barrier permeable. The compound should be stored at room temperature. It is for research use only and is not intended for human consumption outside of approved clinical indications. |
| Toxicity/Toxicokinetics |
Effects During Pregnancy and Lactation
◉ Overview of Use During Lactation Ondansetron is commonly used to relieve nausea during and after cesarean section, usually at an intravenous dose of 4 to 8 mg. Use of ondansetron during and after cesarean section does not appear to affect the initiation of breastfeeding. No adverse reactions have been reported in infants of women who received ondansetron postpartum, nor in pharmacokinetic studies. Studies on the use of ondansetron in postpartum lactating women are insufficient, but the drug is approved for use in infants up to 1 month old. Computer models show that drug concentrations in breast milk are far below this dose. No special precautions are required. ◉ Effects on Breastfed Infants A pharmacokinetic study of 78 women who received intravenous ondansetron postpartum showed no adverse reactions in their breastfed infants. ◉ Effects on Lactation and Breast Milk A randomized, double-blind study compared the effects of placebo versus intravenous 4 mg ondansetron after cesarean section in preventing postoperative nausea and vomiting. There was no difference in the time to first breastfeeding between the two groups. A retrospective study compared three medication regimens in women who underwent cesarean section: dexmedetomidine before anesthesia and during delivery (n = 115), saline before anesthesia and during delivery, and dexmedetomidine postpartum (n = 109), and saline before anesthesia and during delivery (n = 168). All women received 4 mg ondansetron as needed, prior to suture removal. The mean total ondansetron intake ranged from 6 mg to 9 mg across all groups. The time to first lactation was similar across all groups (25 to 28 minutes). The toxicity profile of Ondansetron hydrochloride dihydrate is well established from clinical use. It is a well-tolerated drug with few side effects. Headache, constipation, and dizziness are the most commonly reported side effects. The compound is for research use only and is not intended for human consumption outside of approved clinical indications. Standard toxicological evaluation would include acute and repeated-dose toxicity studies, as well as assessment of effects on the gastrointestinal and central nervous systems. |
| References | |
| Additional Infomation |
Ondansetron hydrochloride belongs to the carbazole class of drugs. Ondansetron hydrochloride is the hydrochloride salt of the racemic mixture of ondansetron. Ondansetron is a carbazole derivative and a selective competitive 5-HT3 receptor antagonist with antiemetic activity. Although its mechanism of action is not fully elucidated, ondansetron appears to competitively block the action of 5-HT3 receptors in the peripheral gastrointestinal tract and in the postmedula medulla oblongata (the region containing the chemoreceptor trigger zone (CTZ) of the central nervous system), thereby inhibiting nausea and vomiting induced by chemotherapy and radiotherapy. A competitive 5-HT3 receptor antagonist. It is effective in treating nausea and vomiting induced by cytotoxic chemotherapy drugs (including cisplatin) and has been reported to have anti-anxiety and antipsychotic effects. See also: Ondansetron hydrochloride (note moved to).
Ondansetron hydrochloride dihydrate (CAS 103639-04-9) is an orally bioavailable, selective and competitive 5-HT3 receptor antagonist that is blood-brain barrier permeable. It is used mainly to prevent nausea and vomiting caused by cancer chemotherapy, radiation therapy, and surgery. It is the first of a class of selective serotonin 5-HT3 receptor antagonists. It is available for research purposes only. |
| Molecular Formula |
C18H24CLN3O3
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|---|---|
| Molecular Weight |
365.85
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| Exact Mass |
365.15
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| CAS # |
103639-04-9
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| Related CAS # |
Ondansetron;99614-02-5;Ondansetron hydrochloride;99614-01-4
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| PubChem CID |
59774
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| Appearance |
White to off-white solid powder
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| Density |
1.1±0.1 g/cm3
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| Boiling Point |
267.0±9.0 °C at 760 mmHg
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| Melting Point |
231-232ºC
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| Flash Point |
144.9±5.1 °C
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| Vapour Pressure |
0.0±0.5 mmHg at 25°C
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| Index of Refraction |
1.523
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| LogP |
-0.37
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
25
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| Complexity |
440
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC1=NC=CN1CC2CCC3=C(C2=O)C4=CC=CC=C4N3C.O.O.Cl
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| InChi Key |
VRSLTNZJOUZKLX-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C18H19N3O.ClH.2H2O/c1-12-19-9-10-21(12)11-13-7-8-16-17(18(13)22)14-5-3-4-6-15(14)20(16)2;;;/h3-6,9-10,13H,7-8,11H2,1-2H3;1H;2*1H2
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| Chemical Name |
9-methyl-3-[(2-methylimidazol-1-yl)methyl]-2,3-dihydro-1H-carbazol-4-one;dihydrate;hydrochloride
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: (1). Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. (2). This product is not stable in solution, please use freshly prepared working solution for optimal results. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: 100 mg/mL (273.34 mM)
H2O: 16.67 mg/mL (45.57 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.83 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.83 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7334 mL | 13.6668 mL | 27.3336 mL | |
| 5 mM | 0.5467 mL | 2.7334 mL | 5.4667 mL | |
| 10 mM | 0.2733 mL | 1.3667 mL | 2.7334 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Link: https://clinicaltrials.gov/ct2/show/NCT02473042
Conditions:Post-Operative Nausea and Vomiting|Breast CancerLink: https://clinicaltrials.gov/ct2/show/NCT04240626
Conditions:Obesity, Morbid|Surgery|Bariatric Surgery CandidateLink: https://clinicaltrials.gov/ct2/show/NCT04766996
Conditions:Anesthesia|Opioid Use
Title:Study to Evaluate Rate of Nausea in Healthy Premenopausal Female Subjects Treated With Single Dose of Bremelanotide Alone or With Zofran
Status:Completed
updateDate:2022-04-04
Ctid:NCT03973047
Link: https://clinicaltrials.gov/ct2/show/NCT03973047
Conditions:NauseaLink: https://clinicaltrials.gov/ct2/show/NCT04872270
Conditions:Caffeine|Pain, JointLink: https://clinicaltrials.gov/ct2/show/NCT01217190
Conditions:Nausea and Vomiting, Postoperative|Nausea With Vomiting Chemotherapy-InducedLink: https://clinicaltrials.gov/ct2/show/NCT02246439
Conditions:Gastroenteritis|GastritisLink: https://clinicaltrials.gov/ct2/show/NCT03254459
Conditions:Pain, PostoperativeLink: https://clinicaltrials.gov/ct2/show/NCT02110719
Conditions:Narcotic Use|Pain|Constipation|NauseaLink: https://clinicaltrials.gov/ct2/show/NCT01953978
Conditions:PainLink: https://clinicaltrials.gov/ct2/show/NCT01933542
Conditions:Chlorzoxazone|Postoperative PainLink: https://clinicaltrials.gov/ct2/show/NCT01819857
Conditions:Cardiac RepolarizationLink: https://clinicaltrials.gov/ct2/show/NCT01719042
Conditions:Mycobacterium Avium Complex|Adverse EffectsLink: https://clinicaltrials.gov/ct2/show/NCT00659074
Conditions:HealthyLink: https://clinicaltrials.gov/ct2/show/NCT00654277
Conditions:HealthyLink: https://clinicaltrials.gov/ct2/show/NCT00653458
Conditions:HealthyLink: https://www.clinicaltrialsregister.eu/ctr-search/search?query=2011-005216-28
Condition:Post-operative nausea and vomiting (PONV)Link: https://www.clinicaltrialsregister.eu/ctr-search/search?query=2010-022872-30
Condition:Study to evaluate the efficacy and safety of two different doses of palonosetron compared to ondansetron in the prevention of CINV in pediatric patients undergoing single and repeated cycles of MEC or HECLink: https://www.clinicaltrialsregister.eu/ctr-search/search?query=2010-022971-79
Condition:Postoperative nausea and vomiting (PONV)Link: https://www.clinicaltrialsregister.eu/ctr-search/search?query=2008-004789-20
Condition:Prevention of post-operative nausea and vomiting.Link: https://www.clinicaltrialsregister.eu/ctr-search/search?query=2007-005311-25
Condition:Tähystysleikkauksen jälkeinen kipuLink: https://www.clinicaltrialsregister.eu/ctr-search/search?query=2006-000526-31
Condition:Peripheral neuropathyLink: https://www.clinicaltrialsregister.eu/ctr-search/search?query=2006-003512-22
Condition:Chemotherapy-induced Nausea and VomittingLink: https://www.clinicaltrialsregister.eu/ctr-search/search?query=2006-002033-21
Condition:Chemotherapy induced nausea and vomiting (CINV) due to Highly Emetogenic Chemotherapy (HEC)Link: https://www.clinicaltrialsregister.eu/ctr-search/search?query=2006-000781-37
Condition:Chemotherapy induced nausea and vomiting (CINV) due to Moderately Emetogenic Chemotherapy (MEC)Link: https://www.clinicaltrialsregister.eu/ctr-search/search?query=2006-001761-42
Condition:Postoperative Nausea and VomitingLink: https://www.clinicaltrialsregister.eu/ctr-search/search?query=2005-005856-42
Condition:Postoperative Nausea and Vomiting (PONV)Link: https://www.clinicaltrialsregister.eu/ctr-search/search?query=2005-005855-16
Condition:Postoperative Nausea and Vomiting (PONV)Link: https://www.clinicaltrialsregister.eu/ctr-search/search?query=2004-000370-31
Condition:Post Operative Nausea and Vomiting (PONV)Post Discharge Nausea and Vomiting (PDNV)Link: https://www.clinicaltrialsregister.eu/ctr-search/search?query=2004-001021-22
Condition:Post Operative Nausea and Vomiting (PONV)Post Discharge Nausea and Vomiting (PDNV)Link: https://www.clinicaltrialsregister.eu/ctr-search/search?query=2004-000369-37
Condition:Post Operative Nausea and Vomiting (PONV)Post Discharge Nausea and Vomiting (PDNV)Link: https://www.clinicaltrialsregister.eu/ctr-search/search?query=2004-001020-20
Condition:Chemotherapy Induced Nausea and Vomiting (CINV) 0 Moderately Emetogenic Chemotherapy (MEC)Link: https://www.clinicaltrialsregister.eu/ctr-search/search?query=2004-000371-34
Condition:Chemotherapy-Induced Nausea and Vomiting (CINV) - Highly Emetogenic Chemotherapy (HEC)Link: https://www.clinicaltrialsregister.eu/ctr-search/search?query=2011-004372-11
Condition:Enfants de 6 mois à 15 ans inclus, consultant aux urgences pour gastroentérite aiguë et ayant eu au moins 3 vomissements non bilieux, non sanglants dans les 12 heures qui précèdent la consultation.Products are for research use only; We do not sell to patients
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