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500mg |
ln Vitro |
Ketotifen (0-100 μM; 2 or 4 days) suppresses SARS-CoV-2 with an EC50 of 48.9 μM; the percentages of SARS-CoV-2 inhibition that increase to 79%, 83%, and 93% when coadministered with 25, 50, and 100 μM indomethacin, respectively[3]. Ketotifen (0-50 μM; 24 h) demonstrates comparatively moderate cytotoxicity in MDCK cells (EC50=291 μM), with inhibitory efficacy against PR8, pH1N1, and H3N2 (EC50 of 5.9 μM, 33.7 μM, and 48.5 μM, respectively) [4].
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ln Vivo |
Ketotifen (80 mg/kg; injectable; given daily for 3 days) lowers end-organ damage and mortality in mice infected with influenza virus [4]. Ketotifen (0.4 mg/kg; intraperitoneally; given daily for 10 days) lowers the prevalence and severity of encephalomyelitis (EAE) [5].
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Animal Protocol |
Animal/Disease Models: Female C57BL/6 mice (4-6 weeks; PR8 intranasally infected with 1×103 TCID50 in 30 μL DMEM) [4]
Doses: 80 mg/kg Route of Administration: ig; one time/day for 3 Day Experimental Results: diminished end-organ damage and mortality in infected mice. Animal/Disease Models: Female C57BL/6 mice (5-6 weeks old; immunized subcutaneously (sc) (sc) with 150 μg of MOG35-55 peptide containing 4 mg/mL of Mycobacterium tuberculosis) [5] Doses: 0.4 mg/kg Route of Administration: intraperitoneal (ip) injection; one time/day for 10 days (starting on day 7 of infection) Experimental Results: diminished prevalence and severity of EAE; diminished oxidative stress state and inflammasome activation in the central nervous system; diminished T cell activation in the central nervous system numbers, especially Th1; downregulates local mRNA expression of mast cell enzymes and maintains blood-CNS barrier permeability; triggers lymphocyte accumulation in draining lymph nodes. |
References |
[1]. Klooker TK, et al. The mast cell stabiliser ketotifen decreases visceral hypersensitivity and improves intestinal symptoms in patients with irritable bowel syndrome. Gut. 2010 Sep;59(9):1213-21.
[2]. Zhang H, et al. Advances in the discovery of exosome inhibitors in cancer. J Enzyme Inhib Med Chem. 2020;35(1):1322-1330. [3]. Kiani P, et al. In Vitro Assessment of the Antiviral Activity of Ketotifen, Indomethacin and Naproxen, Alone and in Combination, against SARS-CoV-2. Viruses. 2021 Mar 26;13(4):558. [4]. Enkirch T, et al. Identification and in vivo Efficacy Assessment of Approved Orally Bioavailable Human Host Protein-Targeting Drugs With Broad Anti-influenza A Activity. Front Immunol. 2019 Jun 5;10:1097. [5]. Pinke KH, et al. Calming Down Mast Cells with Ketotifen: A Potential Strategy for Multiple Sclerosis Therapy? Neurotherapeutics. 2020 Jan;17(1):218-234. |
Molecular Formula |
C19H19NOS
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Molecular Weight |
309.426
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CAS # |
34580-13-7
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Related CAS # |
Ketotifen fumarate;34580-14-8;Ketotifen-13C,d3;2748522-40-7
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
CN1CCC(=C2C3=CC=CC=C3CC(=O)C4=C2C=CS4)CC1
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 3.2317 mL | 16.1587 mL | 32.3175 mL | |
5 mM | 0.6463 mL | 3.2317 mL | 6.4635 mL | |
10 mM | 0.3232 mL | 1.6159 mL | 3.2317 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.