JNJ4796 |CAS:2241664-16-2 Probechem Biochemicals

Chemical Structure : JNJ4796

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JNJ4796 (JNJ-4796;JNJ 4796)

货号: PC-36123Not For Human Use, Lab Use Only.

JNJ4796 (JNJ-4796) is a potent, orally bioavailable small molecule fusion inhibitor of influenza virus, selectively binds to Group-1 subtype of influenza A viruses HA.

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生物&药学活性

JNJ4796 (JNJ-4796) is a potent, orally bioavailable small molecule fusion inhibitor of influenza virus, selectively binds to Group-1 subtype of influenza A viruses HA.

JNJ4796 dose-dependently prevents pH-induced transition of HA to the post-fusion conformation and subsequent loss of the HA1 subunit after reduction of the inter-chain HA disulfide.

JNJ4796 stabilizes the pre-fusion conformation and blocks the HA conformational change at low pH and the subsequent susceptibility to trypsin.

JNJ4796 binds with a stoichiometry of three binding sites per trimer in a highly conserved hydrophobic groove at the HA1/HA2 interface in the HA stem.

JNJ4796 demonstrated high potency (EC50=12-66 nM) of virus neutralization against representative influenza viruses: Influenza A H1N1 (H1/Bris), H1N1 A/California/07/2009 (H1/Cal), H1N1 A/New Caledonia/20/1999 (H1/NCa), H1N1 A/Puerto Rico/8/1934 (H1/PR8), H1N1 A/Solomon Islands/3/2006 IVR-145 (H1/SI06), weaker effect against H5N1 A/Hong Kong/156/1997 (H5/H97, EC50=449 nM), H5N1 A/Vietnam/1194/2004 (H5/Viet, EC50=3240 nM), and no potency against H3N1 A/Brisbane/10/2007 (H3/Bris), H7 NY (7:1 reassortant virus with the HA of A/New York/107/2003 (H7N7).

物理化学性质&存储条件

分子量	537.584
分子式	C28H27N9O3
外观性状	Solid
CAS No.
储存条件	固体粉末 -20 °C 12 个月; 4°C 6 个月	配置液 -80 °C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	(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

参考文献

1. van Dongen MJP, et al. Science. 2019 Mar 8;363(6431). pii: eaar6221. doi: 10.1126/science.aar6221.

JNJ4796 (JNJ-4796;JNJ 4796)

生物&药学活性

物理化学性质&存储条件

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JNJ4796 (JNJ-4796;JNJ 4796)

生物&药学活性

物理化学性质&存储条件

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