JTP-0157602 | HIV-1 integrase inhibitor | Probechem Biochemicals

Chemical Structure : JTP-0157602

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JTP-0157602 (JTP0157602)

货号: PC-72632Not For Human Use, Lab Use Only.

JTP-0157602 (JTP0157602) is a novel non-catalytic site integrase inhibitor of HIV-1 integrase (IN), inhibits the interaction between LEDGF IBD and IN with IC50 of 4.2 nM.

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生物&药学活性

JTP-0157602 (JTP0157602) is a novel non-catalytic site integrase inhibitor of HIV-1 integrase (IN), inhibits the interaction between LEDGF IBD and IN with IC50 of 4.2 nM.
JTP-0157602 exhibits potent antiviral activity against HIV-1 with EC90 of 138 nM.
JTP-0157602 retained potent antiviral activity (EC50=1-6 nM) against a broad panel of recombinant viruses with INSTI-related resistant mutations, including multiple substitutions that emerged in clinical studies of INSTIs (IN strand transfer inhibitors (INSTIs).
JTP-0157602 inhibited HIV-1 replication mainly during the late-phase of the replication cycle.
JTP-0157602 binds to the LEDGF/p75 binding pocket of HIV-1 integrase (IN).

物理化学性质&存储条件

分子量	687.857
分子式	C39H50FN5O5
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	(2S)-2-(1-(4-(((1r,4S)-4-(8-oxa-3-azabicyclo[3.2.1]octan-3-yl)cyclohexyl)carbamoyl)pyrimidin-2-yl)-3-(4,4-dimethylcyclohex-1-en-1-yl)-5-fluoro-1H-indol-4-yl)-2-(tert-butoxy)acetic acid

参考文献

1. Yoshitsugu Ohata, et al. J Virol. 2022 Jan 19;JVI0184321.

JTP-0157602 (JTP0157602)

生物&药学活性

物理化学性质&存储条件

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JTP-0157602 (JTP0157602)

生物&药学活性

物理化学性质&存储条件

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