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Purity: ≥98%
Ondansetron (GRC-50775; GR-38032; SN-307; GR38032; SN307; GR-C507/75; Zofran), an approved antiemetic drug, is a potent serotonin 5-HT3 receptor antagonist which is used to prevent nausea and vomiting caused by cancer chemotherapy, and radiation therapy. Ondansetron, a 5-HT3A receptor antagonist, reversibly inhibited the 5-HT (30 microM) signal by 70% at 0.3 nM and completely eliminated the response at 3 nM. The study found that auditory gating improved with 0.33 and 1 mg/kg, IP, but not with the lowest tested acute ondansetron dose of 0.1 mg/kg.
| Targets |
5-HT3
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|---|---|
| ln Vivo |
Ondansetron (GR 38032; SN 307) (2.4-6 mg/kg; intraperitoneal injection; six times in 15 days) has a TD50 value of 3.7±0.6 mg/kg and an LD50 of 4.6±0.5 mg/kg in mice [4]. Ondansetron (8 mg/kg; intraperitoneal injection; once) combined with olanzapine has a good effect in preventing CINV in patients with NSCLC, especially for advanced patients [7]. Ondansetron (2 mg/kg; intraperitoneal injection; six consecutive days) Animal model: NSCLC patients receiving chemotherapy [7] Dosage: 8 mg Administration method: intraperitoneal injection (ip) Results: showed TD50 and LD50 doses of 3.7± 0.6 mg) exhibits anti-inflammatory effects through 5-HT3 receptors [8]. They are 4.6±0.5 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 (ip) Results: Demonstrated MPO activity and tumor necrosis factor-α, interleukin-6 and leukocyte-interleukin 1β was significantly reduced.
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| Animal Protocol |
NSCLC Patients Treated With Chemotherapy
8 mg Intraperitoneal Injection (i.p.) |
| References |
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| Molecular Formula |
C18H19N3O
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|---|---|
| Molecular Weight |
293.36
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| Exact Mass |
293.15
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| Elemental Analysis |
C, 73.69; H, 6.53; N, 14.32; O, 5.45
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| CAS # |
99614-02-5
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| Related CAS # |
Ondansetron hydrochloride dihydrate; 103639-04-9; Ondansetron-d5; 1219798-86-3; Ondansetron hydrochloride; 99614-01-4; Ondansetron-d3; 1132757-82-4; Ondansetron-13C,d3; 2699607-85-5
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| Appearance |
Solid powder
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| SMILES |
CC1=NC=CN1CC2CCC3=C(C2=O)C4=CC=CC=C4N3C
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| InChi Key |
FELGMEQIXOGIFQ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C18H19N3O/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
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| Chemical Name |
9-methyl-3-[(2-methylimidazol-1-yl)methyl]-2,3-dihydro-1H-carbazol-4-one
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| Synonyms |
GR 38032; SN 307; GR 38032F; GRC50775; GR-38032; SN-307; GR38032; SN307; GR-C507/75; trade name: Zofran
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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 |
| 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) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1 mg/mL (3.41 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 10.0 mg/mL clear DMSO stock solution to 400 μL of PEG300 and mix evenly; then add 50 μL of Tween-80 to the above solution and mix evenly; then add 450 μL of 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: 1 mg/mL (3.41 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 10.0 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. View More
Solubility in Formulation 3: ≥ 1 mg/mL (3.41 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 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 |
*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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT04169828 | Active recruiting |
Drug: Methotrexate Drug: Ondansetron Drug: Folic/folinic acid |
Juvenile Idiopathic Arthritis | University of British Columbia | August 2, 2019 | Not Applicable |
| NCT04209595 | Active recruiting |
Drug: PLX038 Drug: Rucaparib Drug: Ondansetron |
Small Cell Lung Cancer Extra-Pulmonary Small Cell Carcinomas |
National Cancer Institute (NCI) |
April 8, 2020 | Phase 1 Phase 2 |
| NCT05378113 | Recruiting | Drug: Ondansetron Drug: Lidocaine |
Injection Site Irritation | Emory University | May 18, 2023 | Phase 2 |
| NCT03851835 | Recruiting | Drug: Ondansetron Oral Solution Drug: Oral Placebo |
Acute Gastroenteritis Viral Illness Vomiting Diarrhea |
University of Calgary | September 4, 2019 | Phase 3 |
| NCT03865290 | Recruiting | Drug: Ondansetron 8mg Drug: Placebo |
Indigestion Diabetes Mellitus |
Mayo Clinic | April 2, 2019 | Phase 2 |
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