PF-3450074-PF-74-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEPF-3450074Cat.No.:HY-120072CASNo.:1352879-65-2Synonyms:PF-74分⼦式:C₂₇H₂₇N₃O₂分⼦量:425.52作⽤靶点:HIV作⽤通路:Anti-infection储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:250mg/mL(587.52mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.3501mL11.7503mL23.5007mL5mM0.4700mL2.3501mL4.7001mL10mM0.2350mL1.1750mL2.3501mL请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存⽅式和期限：-80°C,6months;-20°C,1month。-80°C储存时，请在6个⽉内使⽤，-20°C储存时，请在1个⽉内使⽤。体内实验请根据您的实验动物和给药⽅式选择适当的溶解⽅案。以下溶解⽅案都请先按照InVitro⽅式配制澄的储备液，再依次添加助溶剂：(为保证实验结果的可靠性，澄的储备液可以根据储存条件，适当保存；体内实验的⼯作液，建议您现⽤现配，当天使⽤；以下溶剂前显⽰的百分⽐指该溶剂在您配制终溶液中的体积占⽐；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的⽅式助溶)1.请依序添加每种溶剂：10%DMSO>>90%cornoil1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥6.25mg/mL(14.69mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性PF-3450074(PF-74)HIV-1⾐蛋⽩(HIV-1CA)的特异性抑制剂，对HIV分离株表现出⼴谱抑制作⽤，显⽰出亚微尔级别的效价(EC50=8-640nM)。PF-3450074(PF-74)在HIV-1感染的早期阶段起作⽤，通过与CPSF6和NUP153的结合直接竞争来抑制病毒复制，并阻断病毒⽣命周期的脱膜，组装和逆转录步骤。CPSF6：核宿主因⼦裂解和聚腺苷酸特异性因⼦6；NUP153：核孔蛋⽩153。IC50&TargetHIV-1(NL4.3strain)0.72μM(IC50)体外研究PF-3450074(PF-74)exhibitsanti-viralactivitiesagainstHIVwildtypeNL4-3andHIVT107NmutantwithEC50valuesof0.72μMand4.5μM,respectively[1].PF-3450074(PF-74)displaysagoodpotencyinprimaryhumanperipheralbloodmononuclearcells(PBMCs),inhibitsHIV-193RW025,HIV-1JR-CSFandHIV-193MW965withIC50valuesof1.5±0.9μM;0.6±0.20μM;and0.6±0.10μM,respectively.ThiscompoundshowsMedianIC50andCC50valuesof0.9±0.5μMand90.5±5.9μM,respectively[1].TheKDfortheinteractionbetweenPF-74andtheCAhexamer,derivedinthesamemannerasforNUP153,isdeterminedtobe176±78nM[1].PF-3450074(PF-74)(10μM;8hours)resultsinamarkedreductioninlateproductsofreversetranscriptioninHeLa-P4cellswithDNaseI-treatedstocksofEnv-defectiveHIV-1(R9.Env-)[2].RT-PCR[2]CellLine:HeLa-P4cellsConcentration:10μMIncubationTime:8hoursResult:InhibitedHIV-1reversetranscriptionintargetcells.户使⽤本产品发表的科研⽂献•Metabolites.2022,12(8),752.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].XuJP,etal.ExploringModificationsofanHIV-1CapsidInhibitor:Design,Synthesis,andMechanismofAction.JDrugDesRes.2018;5(2).pii:1070.Epub2018Aug13.[2].ShiJ,etal.Small-moleculeinhibitionofhumanimmunodeficiencyvirustype1infectionbyviruscapsiddestabilization.JVirol.2011Jan;85(1):542-9.McePdfHeight2/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemECaution:Producthasnotbeenfullyvalidatedformedicalappli