1. Anti-infection
  2. Influenza Virus

JNJ4796 

目录号: HY-122907
产品使用指南

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。

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JNJ4796 Chemical Structure

JNJ4796 Chemical Structure

CAS No. : 2241664-16-2

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Description

JNJ4796 is an oral active fusion inhibitor of influenza virus, neutralizing influenza A group 1 viruses by inhibiting hemagglutinin (HA)-mediated fusion. JNJ4796 mimics the functionality of the broadly neutralizing antibodies (bnAbs)[1].

IC50 & Target

EC50: 12 nM (H1/Bris), 66 nM (H1/Cal), 38 nM (H1/NCa), 22 nM (H1/PR8), 13 nM (H1/SI06), 449 nM (H5/H97), 3.24 μM (H5/Viet)[1].
Hemagglutinin[1].

In Vitro

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].

In Vivo

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 × LD50 or 1 × LD90 of 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.
References
Molecular Weight

537.57

Formula

C₂₈H₂₇N₉O₃

CAS No.

2241664-16-2

SMILES

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

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping

Room temperature in continental US; may vary elsewhere

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× = ×
C1   V1   C2   V2

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产品名称:
JNJ4796
目录号:
HY-122907
需求量:

JNJ4796

Cat. No.: HY-122907