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编 号:F329827
分子式:C23H23NO5S
分子量:425.5
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10mM*1mL in DMSO
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询价
100mg
400
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生物活性:
Ketotifen (HC 20-511) fumarate is an orally active second-generation noncompetitive histamine 1 (H1) receptor blocker and mast cell stabilizer. Ketotifen fumarate can block 6-phosphogluconate dehydrogenase (PGD) in vitro. Ketotifen fumarate also has antiviral activity against SARS-CoV-2 and Influenza virus. Ketotifen fumarate can be used to the research of autoimmune encephalomyelitis (EAE) and asthma attack prevention.

体内研究:
Ketotifen (80 mg/kg; i.g.; daily for 3 days) reduces end organ damage and mortality in mice infected with influenza virus.Ketotifen fumarate (0.4 mg/kg; i.p.; daily for 10 days) reduces encephalomyelitis (EAE) prevalence and severity.Animal Model:Female C57BL/6 mice (4-6 weeks; intranasal infection with 1×103 TCID50 of PR8 in 30 μL of DMEM)
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)
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.

体外研究:
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.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).
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