JNJ4796 是具有口服活性的流感病毒融合性抑制剂,通过抑制血球凝集素 (HA) 介导的融合来中和甲型流感病毒。JNJ4796 和广泛中和抗体 (bnAbs) 的功能类似。
Cas No. | 2241664-16-2 |
分子式 | C28H27N9O3 |
分子量 | 537.57 |
溶解度 | DMSO : 100 mg/mL (186.02 mM; Need ultrasonic) |
储存条件 | Store at -20°C |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
产品描述 | JNJ4796 is an oral active fusion inhibitor ofinfluenza virus, neutralizing influenza A group 1 viruses by inhibitinghemagglutinin (HA)-mediated fusion. JNJ4796 mimics the functionality of the broadly neutralizing antibodies (bnAbs)[1]. Like bnAb CR6261, the mechanism of action of JNJ4796 is demonstrated to be based on inhibition of the pH-sensitive conformational change of HA that triggers fusion of the viral and endosomal membranes and release of the viral genome into the host cell[1]. Oral administration of JNJ4796 protects mice from lethal challenge of 25 times the median lethal dose (LD50) of H1N1 A/Puerto Rico/8/1934 virus. Doses of 50 and 10 mg/kg of JNJ4796 twice daily, initiated one day before 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[1]. Oral doses of JNJ4796 results in 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]. Animal Model: | Female BALB/cAnNCrl mice intranasally infected with 2 × 25 μL of 25 × LD50or 1 × LD90of H1N1 A/Puerto Rico/8/34 dissolved in sterile phosphate buffered saline (D-PBS)[1] | Dosage: | 50 and 10 mg/kg. | Administration: | Oral twice daily for 7 days. | Result: | Resulted in 100% survival at day 21 in comparison to the less potent compound JNJ8897. |
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