JNJ4796

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

JNJ4796 (JNJ 4796, JNJ-4796) 是一种口服活性流感病毒血凝素 (HA) 小分子融合抑制剂，EC50 为 33 nM（H1N1 中和）。

JNJ4796 (JNJ 4796, JNJ-4796) is an orally active small-molecule fusion inhibitor of influenza virus hemagglutinin (HA) with EC50 of 33 nM (H1N1 neutralization); mimics the binding and functionality of the broadly neutralizing antibody CR6261; targets the conserved HA stem region, acts as a fusion inhibitor by inhibiting conformational changes that lead to the postfusion HA structure, and neutralizes a broad spectrum of human pandemic, seasonal, and emerging group 1 influenza A viruses; specificly neutralizes influenza A group 1 viruses by inhibiting HA-mediated fusion in vitro, protects mice against lethal and sublethal influenza challenge after oral administration.

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.

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.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. Animal Model:Female BALB/cAnNCrl mice intranasally infected with 2 × 25 μL of 25 × LD50 or 1 × LD90 of H1N1 A/Puerto Rico/8/34 dissolved in sterile phosphate buffered saline (D-PBS) 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.

JNJ-4796 | JNJ 4796

Microbiology/Virology

Influenza Virus

Influenza Virus

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2241664-16-2

537.584

C28H27N9O3

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (186.02 mM)

CC(NC1=CC=C(OC(C2=CC(C(N3CCN([C@@H](C4=NN(C)N=N4)C5=CC=CC=C5)CC3)=O)=NC=C2)=N6)C6=C1)=O

(R)-N-(2-(2-(4-((2-methyl-2H-tetrazol-5-yl)(phenyl)methyl)piperazine-1-carbonyl)pyridin-4-yl)benzo[d]oxazol-5-yl)acetamide

(-20℃)

With Ice Pack

≥ 2 years