2. Ketotifen

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.

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Ketotifen Chemical Structure

Ketotifen Chemical Structure

CAS No. : 34580-13-7

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Ketotifen Related Antibodies

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Description

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[1][2][3][4].

IC50 & Target

Histamine 1, SARS-CoV-2, Influenza virus[1][3][4]
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.

Ketotifen Related Antibodies
In Vivo

Ketotifen (80 mg/kg; i.g.; daily for 3 days) reduces end organ damage and mortality in mice infected with influenza virus[4].
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.

Animal Model: Female C57BL/6 mice (4-6 weeks; intranasal infection with 1×103 TCID50 of PR8 in 30 μL of DMEM)[4]
Dosage: 80 mg/kg
Administration: i.g.; daily for 3 days
Result: Reduced end organ damage and mortality in infected mice.
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]
Dosage: 0.4 mg/kg
Administration: i.p.; daily for 10 days (from the 7th day of infection)
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.
Clinical Trial
Molecular Weight

309.43

Formula

C19H19NOS
CAS No.
SMILES

O=C(C1=C/2C=CS1)CC3=CC=CC=C3C2=C4CCN(C)CC/4
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Room temperature in continental US; may vary elsewhere.
Storage

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Purity & Documentation
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Ketotifen34580-13-7HC 20-511Inhibitorinhibitorinhibit

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