JNJ4796
目录号: PL02577 纯度: ≥99%
CAS No. :2241664-16-2
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中文名称
JNJ4796
英文名称
JNJ4796
英文别名
JNJ4796;N-[2-(2-{4-[(R)-(2-methyl-2H-tetrazol-5-yl)(phenyl)methyl]piperazine-1-carbonyl}pyridin-4-yl)-1,3-benzoxazol-5-yl]acetamide;EZ7;Q62019796;(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;N-[2-[2-[4-[(R)-(2-Methyltetrazol-5-yl)-phenylmethyl]piperazine-1-carbonyl]pyridin-4-yl]-1,3-benzoxa
Cas No.
2241664-16-2
分子式
C28H27N9O3
分子量
537.57
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
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。
生物活性
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).
性状
Solid
IC50 & Target[1][2]
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).
Hemagglutinin.
体外研究(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. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
Oral administration of JNJ4796 protects mice from lethal challenge of 25 times the median lethal dose (LD 50 ) 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 (LD 90 ), with twice daily administration of 15 and 5 mg/kg of JNJ4796 giving rise to 100% survival. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[1]. van Dongen MJP, et al. A small-molecule fusion inhibitor of influenza virus is orally active in mice. Science. 2019 Mar 8;363(6431).
溶解度数据
In Vitro: DMSO : 100 mg/mL (186.02 mM; Need ultrasonic)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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