Ketotifen (HC 20-511) 是一种具有口服活性的第二代非竞争性组胺 1 (H1) 受体阻滞剂和肥大细胞稳定剂。Ketotifen 可在体外阻断 6-磷酸葡萄糖酸脱氢酶 (6-PGD)。Ketotifen 还对SARS-CoV-2和流感病毒 (Influenza virus) 具有抗病毒活性。Ketotifen 可用于自身免疫性脑脊髓炎 (EAE) 和预防哮喘发作的研究。
| 生物活性 | Ketotifen (HC 20-511) is an orally active second-generation noncompetitivehistamine 1 (H1)receptor blocker and mast cell stabilizer. Ketotifen can block 6-phosphogluconate dehydrogenase (PGD)in vitro. Ketotifen also has antiviral activity againstSARS-CoV-2andInfluenza 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] |
体外研究
(In Vitro) | Ketotifen (0-100 μM; 2 or 4 days) inhibits SARS-CoV-2 with an EC50of 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].
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体内研究
(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].
| Animal Model: | Female C57BL/6 mice (4-6 weeks; intranasal infection with 1×103TCID50of 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 MOG35-55peptide containing 4 mg/mL ofMycobacterium 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. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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