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CAS No. : 34580-14-8
MCE 国际站:Ketotifen fumarate
产品活性:Ketotifen (HC 20-511) fumarate 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 fumarate 可在体外阻断 6-磷酸葡萄糖酸脱氢酶 (6-PGD)。Ketotifen fumarate 还对 SARS-CoV-2 和流感病毒 (Influenza virus) 具有抗病毒活性。Ketotifen fumarate 可用于自身免疫性脑脊髓炎 (EAE) 和预防哮喘发作的研究。
研究领域:GPCR/G Protein | Neuronal Signaling | Immunology/Inflammation | Metabolic Enzyme/Protease | Anti-infection
作用靶点:Histamine Receptor | Endogenous Metabolite | SARS-CoV | Influenza Virus
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.
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).
In Vivo: 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.
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