| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| 1g |
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| 5g |
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| Other Sizes |
| Targets |
5-HT3 Receptor
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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].
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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). |
| 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). |
| 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).
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| 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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| 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) |
|---|---|
| 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.
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