| Size | Price | Stock | Qty |
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| 100mg |
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| 250mg |
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| 500mg |
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| 1g |
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| 2g |
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| 5g |
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Purity: ≥98%
Ketotifen Fumarate (HC20511; Ketotifene, Zaditor, Zaditen, Ketotiphen), the fumaric acid salt of ketotifen, is a second-generation and noncompetitive H1-antihistamine and mast cell stabilizer used to treat allergic symptoms and to prevent asthma attacks. It comes in two forms and is most frequently sold as a salt that contains fumaric acid, ketotifen fumarate. It is used to treat allergic conjunctivitis, or itchy red eyes brought on by allergies, in its ophthalmic form. When taken orally, it helps prevent asthma attacks.
| Targets |
Histamine 1; SARS-CoV-2; Influenza virus
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| ln Vitro |
Ketotifen (0-100 μM; 2 or 4 days) inhibits SARS-CoV-2 with an EC50 of 48.9 μM; when co-administered with 25, 50, and 100 μM Indomethacin, respectively, increases the percentage inhibition of SARS-CoV-2 to 79%, 83%, and 93%[3].
Ketotifen (0-50 μM; 24 h) demonstrates comparatively low cytotoxicity in MDCK cells (EC50=291 μM) and has inhibitory activity against PR8, pH1N1, and H3N2 with EC50s of 5.9 μM, 33.7 μM, and 48.5 μM, respectively[4]. |
| ln Vivo |
Ketotifen (80 mg/kg; orally for 3 days) lowers mortality and end organ damage in mice with influenza virus infection[4].
Ketotifen fumarate (0.4 mg/kg; intraperitoneal; daily for 10 days) lowers the incidence and severity of encephalomyelitis (EAE)[5]. |
| Animal Protocol |
Female C57BL/6 mice (4-6 weeks; intranasal infection with 1×103 TCID50 of PR8 in 30 μL of DMEM)
80 mg/kg i.g.; daily for 3 days |
| References |
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| Molecular Formula |
C23H23NO5S
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|---|---|---|
| Molecular Weight |
425.5
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| Exact Mass |
425.13
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| Elemental Analysis |
C, 64.92; H, 5.45; N, 3.29; O, 18.80; S, 7.53
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| CAS # |
34580-14-8
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| Related CAS # |
Ketotifen-d3 fumarate; 1795138-23-6; Ketotifen; 34580-13-7
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| Appearance |
White to off-white solid powder
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| SMILES |
CN1CCC(=C2C3=C(C(=O)CC4=CC=CC=C42)SC=C3)CC1.C(=C/C(=O)O)\C(=O)O
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| InChi Key |
YNQQEYBLVYAWNX-WLHGVMLRSA-N
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| InChi Code |
InChI=1S/C19H19NOS.C4H4O4/c1-20-9-6-13(7-10-20)18-15-5-3-2-4-14(15)12-17(21)19-16(18)8-11-22-19;5-3(6)1-2-4(7)8/h2-5,8,11H,6-7,9-10,12H2,1H3;1-2H,(H,5,6)(H,7,8)/b;2-1+
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| Chemical Name |
(E)-but-2-enedioic acid;2-(1-methylpiperidin-4-ylidene)-6-thiatricyclo[8.4.0.03,7]tetradeca-1(14),3(7),4,10,12-pentaen-8-one
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| Synonyms |
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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: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
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| 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: ≥ 2.5 mg/mL (5.88 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 (5.88 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. View More
Solubility in Formulation 3: 37.5 mg/mL (88.13 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3502 mL | 11.7509 mL | 23.5018 mL | |
| 5 mM | 0.4700 mL | 2.3502 mL | 4.7004 mL | |
| 10 mM | 0.2350 mL | 1.1751 mL | 2.3502 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 |
| NCT03582176 | Active Recruiting |
Drug: Lactose Placebo Drug: Ketotifen Fumarate 2mg |
Elbow Fracture Elbow Injury Elbow Dislocation |
University of Calgary | April 26, 2019 | Phase 3 |
| NCT02484248 | Active Recruiting |
Drug: Ketotifen Drug: Placebo |
Functional Dyspepsia | Children's Mercy Hospital Kansas City |
August 2015 | Phase 3 |
| NCT05624138 | Recruiting | Drug: Placebo tablets Drug: Ketotifen Oral Tablet |
Neuropathy;Peripheral | Tanta University | November 9, 2022 | Phase 3 |
| NCT05007522 | Recruiting | Drug: Ketotifen/Indomethacin Drug: Placebo |
COVID-19 Respiratory Infection | Sen-Jam Pharmaceutical | May 3, 2022 | Phase 3 |
| NCT05511831 | Not yet recruiting | Drug: Ketotifen Fumarate Drug: standard treatment |
ST-segment Elevation Myocardial Infarction (STEMI) |
Peking University Third Hospital | September 1, 2022 | Phase 4 |
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Products are for research use only; We do not sell to patients
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