PF-3450074 blocks HIV-1 at an early postentry stage by binding the viral capsid and interfering with its function.
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描述 | PF-3450074 is a specific inhibitor of HIV-1 capsid protein (CA) with broad-spectrum inhibition of HIV isolates and submolar potency (EC50=8-640 nM). PF-3450074 acts at the early stage of HIV-1 infection, inhibiting viral replication by directly competing for the binding of CPSF6 and NUP153, and blocking the decapsidation, assembly and reverse transcription steps in the viral life cycle[1][2] .PF-3450074 exhibits antiviral activity against HIV wild-type NL4-3 and HIV T107N mutants with EC50 values of 0.72 μM and 4.5 μM, respectively[1] .PF-3450074 showed good potency in primary human peripheral blood mononuclear cells (PBMCs) and inhibited 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. The median The median IC50 and CC50 values of the compound were 0.9 ± 0.5 μM and 90.5 ± 5.9 μM, respectively[1] .Acting at a concentration of 10 μM for 8 hours, PF-3450074 significantly reduced late products of reverse transcription in DNase I-treated Env-deficient HIV-1 (R9.Env-) HeLa-P4 cells[2]. |
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存储液制备 | ![]() |
1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
2.35mL 0.47mL 0.24mL |
11.75mL 2.35mL 1.18mL |
23.50mL 4.70mL 2.35mL |
CAS号 | 1352879-65-2 |
分子式 | C27H27N3O2 |
分子量 | 425.52 |
SMILES Code | O=C(CC1=C(NC2=C1C=CC=C2)C)N[C@H](C(N(C3=CC=CC=C3)C)=O)CC4=CC=CC=C4 |
MDL No. | MFCD28160729 |
别名 | PF-74 |
运输 | 蓝冰 |
InChI Key | ACDFWSNAQWFRRF-VWLOTQADSA-N |
Pubchem ID | 49800090 |
存储条件 |
In solvent -20°C:3-6个月-80°C:12个月 Pure form Sealed in dry, 2-8°C |