Ketotifen
Based on 4 publication(s) in Google Scholar
Ketotifen (HC 20-511) is an orally active second-generation noncompetitive histamine 1 (H1) receptor blocker and mast cell stabilizer. Ketotifen can block 6-phosphogluconate dehydrogenase (PGD) in vitro. Ketotifen also has antiviral activity against SARS-CoV-2 and Influenza virus. Ketotifen can be used to the research of autoimmune encephalomyelitis (EAE) and asthma attack prevention.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 99.94%
- No. CAS: 34580-13-7
- Fòrmula: C19H19NOS
- Peso molecular:309.43
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
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HY-B0320A
Cromolyn disodiumMast Cell Stabilizer -
HY-14648
DexamethasoneGR Agonist -
HY-B0539
DesloratadineH1-Receptor Antagonist -
HY-B0286
ChlorpheniramineAnti-histamine -
HY-17043
LoratadineInfluenza Virus Inhibitor -
HY-B0462
Azelastine hydrochlorideHistamine 1 Antagonist -
HY-17043R
Loratadine (Standard)Influenza Virus Inhibitor -
HY-B0157R
Ketotifen (Standard)Histamine 1 Receptor Blocker
Publications Citing Use of MedChemExpress (MCE) Ketotifen
MoreVer todos los productos específicos de isoformas Histamine Receptor
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Actividad biológica
Descripciòn
IC50 & Target
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H1 Receptor |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO-K1 | IC50 |
1 nM
Compound: Ketotifen
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Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO-K1 cells after 60 mins by scintillation counting
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO-K1 cells after 60 mins by scintillation counting
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[PMID: 21470866] |
| RBL-2H3 | IC50 |
35.2 μM
Compound: 6
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Inhibition of DNP-BSA-induced degranulation in rat RBL2H3 cells assessed as reduction in beta-hexosaminidase release after 20 mins by spectrophotometry
Inhibition of DNP-BSA-induced degranulation in rat RBL2H3 cells assessed as reduction in beta-hexosaminidase release after 20 mins by spectrophotometry
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[PMID: 22543029] |
| RBL-2H3 | IC50 |
27.9 μM
Compound: Ketotifen
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Antiallergic activity in rat RBL-2H3 cell model assessed as inhibition rate of IgE-mediated degranulation in by measuring beta-aminosidase
Antiallergic activity in rat RBL-2H3 cell model assessed as inhibition rate of IgE-mediated degranulation in by measuring beta-aminosidase
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[PMID: 38640354] |
| Sf21 | IC50 |
738.4 μM
Compound: Ketotifen
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Inhibition of human BSEP expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake
Inhibition of human BSEP expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake
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[PMID: 21965623] |
| Sf21 | IC50 |
>1000 μM
Compound: Ketotifen
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Inhibition of Sprague-Dawley rat Bsep expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake
Inhibition of Sprague-Dawley rat Bsep expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake
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[PMID: 21965623] |
In Vitro
Ketotifen (0-100 μM; 2 or 4 days) inhibits SARS-CoV-2 with an EC50 of 48.9 μM; and increases the percentage inhibition of SARS-CoV-2 to 79%, 83% and 93% when co-administers with 25, 50 and 100 μM Indomethacin, respectively[3].
Ketotifen (0-50 μM; 24 h) has inhibitory activity against PR8, pH1N1 and H3N2 with EC50s of 5.9 μM, 33.7 μM and 48.5 μM, respectively; and exhibits relatively low cytotoxicity in MDCK cells (EC50=291 μM)[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
Ketotifen (0.4 mg/kg; i.p.; daily for 10 days) reduces encephalomyelitis (EAE) prevalence and severity[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female C57BL/6 mice (4-6 weeks; intranasal infection with 1×103 TCID50 of PR8 in 30 μL of DMEM)[4]
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Dosage:80 mg/kg
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Administration:i.g.; daily for 3 days
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Result:Reduced end organ damage and mortality in infected mice.
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Animal Model:Female C57BL/6 mice (5-6 weeks old; subcutaneously immunized with 150 μg of MOG35-55 peptide containing 4 mg/mL of Mycobacterium tuberculosis)[5]
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Dosage:0.4 mg/kg
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Administration:i.p.; daily for 10 days (from the 7th day of infection)
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Result:Reduced EAE prevalence and severity; reduced oxidative stress status and inflammasome activation at the CNS; reduced the amount of T cells, especially Th1, in the CNS; downregulated local mRNA expression for mast cell enzymes and preserves blood-CNS barrier permeability; triggered lymphocyte accumulation in draining lymph nodes.
Ensayo clínico
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 34580-13-7
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Appearance Solid
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Peso molecular 309.43
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Fòrmula C19H19NOS
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Color Off-white to yellow
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SMILES
O=C(C1=C/2C=CS1)CC3=CC=CC=C3C2=C4CCN(C)CC/4
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Synonyms
HC 20-511
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (4)
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Journal Impact Factor
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Most Recent
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Eur J Med Chem
2024 Dec 5:279:116842. PMID: 39260319 -
Cell Oncol (Dordr)
Repurposing ketotifen as a therapeutic strategy for neuroendocrine prostate cancer by targeting the IL-6/STAT3 pathway. [Abstract]2023 Oct;46(5):1445-1456. PMID: 37120492 -
Microbiol Spectr
In vitro interaction of naphthoquine with ivermectin, atovaquone, curcumin, and ketotifen in the asexual blood stage of Plasmodium falciparum 3D7. [Abstract]2024 Jul 2;12(7):e0063024. PMID: 38780257
Solvente y solubilidad
In Vitro:
DMSO : 10 mg/mL (32.32 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 1 mg/mL (3.23 mM); Clear solution
This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 1 mg/mL (3.23 mM); Clear solution
This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocolo
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Research Protocol for Infectious Diseases
Infectious-disease experiments test how pathogens interact with host barriers, innate immune receptors, inflammatory signaling, pathogen replication, and tissue injury; pattern-recognition receptors such as TLRs, RIG-I-like receptors, NOD-like receptors, and inflammasomes detect microbial molecules and activate NF-κB, interferon, and cytokine responses. The central hypothesis is that infection severity reflects the balance between pathogen burden and host response: protective inflammation restricts pathogen growth, whereas excessive or mislocalized inflammation contributes to tissue damage and disease phenotype. Unresolved questions include which host pathways are protective versus pathogenic, why some infection models fail to translate to human disease, and which combined readouts best predict clinically relevant infection outcomes.
Pureza y Documentación
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Ficha de datos (295 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[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. [Content Brief]
[2]. Zhang H, et al. Advances in the discovery of exosome inhibitors in cancer. J Enzyme Inhib Med Chem. 2020;35(1):1322-1330. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.2317 mL | 16.1587 mL | 32.3175 mL | 80.7937 mL |
| 5 mM | 0.6463 mL | 3.2317 mL | 6.4635 mL | 16.1587 mL | |
| 10 mM | 0.3232 mL | 1.6159 mL | 3.2317 mL | 8.0794 mL | |
| 15 mM | 0.2154 mL | 1.0772 mL | 2.1545 mL | 5.3862 mL | |
| 20 mM | 0.1616 mL | 0.8079 mL | 1.6159 mL | 4.0397 mL | |
| 25 mM | 0.1293 mL | 0.6463 mL | 1.2927 mL | 3.2317 mL | |
| 30 mM | 0.1077 mL | 0.5386 mL | 1.0772 mL | 2.6931 mL |
Ketotifen Related Classifications
HY-B0157 Related Classifications
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