产品
编 号:F132490
分子式:C27H27N3O2
分子量:425.52
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10mM*1mL in DMSO
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5mg
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10mg
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25mg
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50mg
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100mg
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生物活性:
PF-3450074 (PF-74) is a specifical inhibitor of?HIV-1 capsid protein (CA) and displays a broad-spectrum inhibition of HIV isolates with submicromolar potency (EC50=8-640 nM). PF-3450074 (PF-74) acts at an early stage of HIV-1 infection, inhibits viral replication by directly competing with the binding of CPSF6 and NUP153, and blocks the uncoating, assembly, and the reverse transcription steps of the viral life cycle. CPSF6: nuclear host factors cleavage and polyadenylation specific factor 6; NUP153: nucleoporin 153.

体外研究:
PF-3450074 (PF-74) exhibits anti-viral activities against HIV wild type NL4-3 andHIV T107N mutant with EC50 values of 0.72 μM and 4.5μM, respectively.PF-3450074 (PF-74) displays a good potency in primary human peripheral blood mononuclear cells (PBMCs), inhibits HIV-193RW025, HIV-1JR-CSF and HIV-193MW965 with IC50 values of 1.5 ± 0.9 μM; 0.6 ± 0.20 μM; and 0.6 ± 0.10 μM, respectively. This compound shows Median IC50?and CC50?values of 0.9 ± 0.5 μM and 90.5 ± 5.9 μM, respectively.The KD?for the interaction between?PF-74?and the CA hexamer, derived in the same manner as for NUP153, is determined to be 176 ± 78 nM.PF-3450074 (PF-74) (10 μM; 8 hours) results in a marked reduction in late products of reverse transcription in HeLa-P4 cells with DNase I-treated stocks of Env-defective HIV-1 (R9.Env-).
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