产品描述
JNJ4796 is an oral active fusion inhibitor of the influenza virus, by inhibiting hemagglutinin (HA)-mediated fusion to neutralizing the influenza A group 1 virus. JNJ4796 mimics the functionality of the broadly neutralizing antibodies (bnAbs).
体外活性
The mechanism of action of JNJ4796 is demonstrated to be based on inhibition of the pH-sensitive conformational change of HA, like bnAb CR6261. That triggers the fusion of the viral and endosomal membranes and the release of the viral genome into the host cell[1].
体内活性
JNJ4796(50 and 10 mg/kg; twice daily) treatment, initiated one day before the challenge and continuing for 7 days, results in 100% survival at day 21 in comparison to the less potent compound JNJ8897 for which less than 50% survival is achieved. JNJ4796 (p.o.) protects mice from lethal challenge of 25 times the median lethal dose (LD50) of H1N1 A/Puerto Rico/8/1934 virus. Oral doses of JNJ4796 cause dose-dependent efficacy after a sublethal viral challenge (LD90), with twice-daily administration of 15 and 5 mg/kg of JNJ4796 giving rise to 100% survival[1].
Cas No.
2241664-16-2
分子式
C28H27N9O3
分子量
537.57
别名
JNJ4796
储存和溶解度
(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years