PF-04957325-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEPF-04957325Cat.No.:HY-15426CASNo.:1305115-80-3分⼦式:C₁₄H₁₅F₃N₈OS分⼦量:400.38作⽤靶点:Phosphodiesterase(PDE)作⽤通路:MetabolicEnzyme/Protease储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:≥100mg/mL(249.76mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制备储备液1mM2.4976mL12.4881mL24.9763mL5mM0.4995mL2.4976mL4.9953mL10mM0.2498mL1.2488mL2.4976mL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>>40%PEG300>>5%Tween-80>>45%saline1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥2.5mg/mL(6.24mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(6.24mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(6.24mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性PF-04957325⼀种⾼效，选择性的PDE8抑制剂，抑制PDE8A和PDE8B的IC50值分别为0.7nM和0.3nM。IC50&TargetIC50:0.7nM(PDE8A),lessthan0.3nM(PDE8B)[1]体外研究PF-04957325isovertwoordersofmagnitudelessefficientthanPICLinsuppressingpolyclonalTeffcellproliferation,andshowsnoeffectoncytokinegeneexpressioninthesecells,despiteitsrobusteffectonTcelladhesion[1].PF-04957325isaselectivePDE8inhibitorandinhibitsbreastcancercellmigration[2].PF-04957325greatlypotentiatessteroidogenesisinWTadrenalcells.PF-04957325showsareportedIC50of0.7nMagainstPDE8A,0.2nMagainstPDE8B,and>1.5μMagainstallotherPDEisoforms[3].PF-04957325treatmentofWTLeydigcellsorMA10cellsincreasessteroidproductionbuthasnoeffectinPDE8A(-/-)/B(-/-)double-knockoutcells,confirmingtheselectivityofthedrug.Moreover,underbasalconditions,cotreatmentwithPF-04957325plusrolipram,aPDE4-selectiveinhibitor,synergisticallypotentiatessteroidproduction[4].PROTOCOLCellAssay[2]Breastcancercellsareinatotalvolumeof0.1mLoffreshmediumcontainingthetestreagentsorvehicle(PF-04957325).Followingincubationat37°Cfor72h,20μLofacombinedsolutionofMTS(2mg/mL)/PMS(0.92mg/mL)(20:1,mixedimmediatelybeforeuse)isaddedtoeachwell,andtheplatesincubatedforanadditional2hat37°C,protectedfromlight,followingwhichtheabsorbencyoftheformazanproductformedisdeterminedat492nmusingamicrotiterplatereader.AllreagentstestedaredissolvedinDMSOanddilutedintothecellculturemedium[2].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.户使⽤本产品发表的科研⽂献•SciSignal.2020Nov24;13(659):eaax0273.•EMBORep.2021Dec23;e53135.•CellChemBiol.2019Oct17;26(10):1393-1406.e7.•Endocrinology.2018May1;159(5):2142-2152.•PLoSOne.2019Aug23;14(8):e0215188.Seemorecustomervalidationsonwww.MedChemE2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEREFERENCES[1].VangAG,etal.DifferentialExpressionandFunctionofPDE8andPDE4inEffectorTcells:ImplicationsforPDE8asaDrugTargetinInflammation.FrontPharmacol.2016Aug23;7:259.[2].DongH,etal.InhibitionofbreastcancercellmigrationbyactivationofcAMPsignaling.BreastCancerResTreat.2015Jul;152(1):17-28.[3].TsaiLC,etal.Regulationofadrenalsteroidogenesisbythehigh-affinityphosphodiesterase8family.HormMetabRes.2012Sep;44(10):790-4.[4].Shimizu-AlbergineM,etal.cAMP-specificphosphodiesterases8Aand8B,essentialregulatorsofLeydigcellsteroidogenesis.MolPharmacol.2012Apr;81(4):556-66.McePdfHeightCau