PF-3450074

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

PF-3450074 (PF74) 是一种小分子 HIV 衣壳蛋白，在体外使病毒衣壳不稳定；在 HIV-1 感染的早期阶段起作用并抑制靶细胞中的逆转录。

PF-3450074 (PF74) is a small molecule HIV capsid protein, destabilized the viral capsid in vitro; acts at an early stage of HIV-1 infection and inhibits reverse transcription in target cells, induced the rapid dissolution of the HIV-1 capsid; PF74 antiviral activity is promoted by binding of the host protein cyclophilin A to the HIV-1 capsid, and PF74 and cyclosporine exhibited mutual antagonism.

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-). RT-PCR Cell Line:HeLa-P4 cells Concentration:10 μMIncubation Time:8 hours Result:Inhibited HIV-1 reverse transcription in target cells.

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PF3450074 | PF-74 | PF74

Microbiology/Virology

HIV

HIV

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1352879-65-2

425.532

C27H27N3O2

>98% (HPLC)

In Vitro:?DMSO : 250 mg/mL (587.52 mM)

O=C(N[C@@H](CC1=CC=CC=C1)C(N(C)C2=CC=CC=C2)=O)CC3=C(C)NC4=C3C=CC=C4

2-Methyl-N-[(1S)-2-(methylphenylamino)-2-oxo-1-(phenylmethyl)ethyl]- 1H-indole-3-acetamide

(-20℃)

With Ice Pack

≥ 2 years