Nelfinavir-Mesylate-AG-1343-Mesylate-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemENelfinavirMesylateCat.No.:HY-15287ACASNo.:159989-65-8Synonyms:AG1343Mesylate分⼦式:C₃₃H₄₉N₃O₇S₂分⼦量:663.89作⽤靶点:HIVProtease;HIV作⽤通路:Anti-infection;MetabolicEnzyme/Protease储存⽅式:4°C,storedundernitrogen*Insolvent:-80°C,6months;-20°C,1month(storedunder

nitrogen)溶解性数据体外实验DMSO:100mg/mL(150.63mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM1.5063mL7.5314mL15.0627mL5mM0.3013mL1.5063mL3.0125mL10mM0.1506mL0.7531mL1.5063mL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(storedundernitrogen)。-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%salineSolubility:≥5mg/mL(7.53mM);Clearsolution1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥5mg/mL(7.53mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥5mg/mL(7.53mM);Clearsolution4.请依序添加每种溶剂：5%DMSO>>40%PEG300>>5%Tween-80>>50%salineSolubility:≥2.5mg/mL(3.77mM);Clearsolution5.请依序添加每种溶剂：5%DMSO>>95%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(3.77mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性NelfinavirMesylate(AG1343Mesylate)⼀种有效的⼝服⽣物可利⽤的HIV-1蛋⽩酶抑制剂(Ki=2nM)，⽤于HIV感染。NelfinavirMesylate(AG1343Mesylate)⼀种⼴谱的抗癌剂。IC50&TargetHIV-1体外研究Nelfinavir(AG1341)Mesylate(1-10μM;48hours)inhibitstheproliferationofmultiplemyelomacells[4].NelfinavirMesylateinhibits26Schymotrypsin-likeproteasomeactivity,impairsproliferationandtriggersapoptosisofthemyelomacelllinesandfreshplasmacells[4].NelfinavirMesylate(1-10μM;17hours)inducesapoptosisofmultiplemyelomacelllines[4].NelfinavirMesylate(5μM;0-24hours)decreasesthephosphorylationofAKT[4].NelfinavirMesylateactivatesthecleavageofcaspase-3,decreasesthephosphorylationofAKT,STAT-3,ERK1/2,andactivatesthepro-apoptoticpathwayoftheunfoldedproteinresponsesystem[4].NelfinavirisalsoaSARS-CoV3CLproinhibitorwithanIC50of35.93μM[5].CellProliferationAssay[4]CellLine:RPMI,LP1,U266,OPM2andMM1ScellsConcentration:1,2,5,10μMIncubationTime:48hoursResult:InhibitedtheproliferationofRPMI,LP1,U266,OPM2andMM1Scelllinesinadose-dependentmannerwithanIC50of1-5μM.ApoptosisAnalysis[4]CellLine:LP1andU266cellsConcentration:1-10μMIncubationTime:17hoursResult:Inducedadose-dependentincreaseinthepercentageofannexinV+/propidiumiodide+cells.2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEWesternBlotAnalysis[4]CellLine:U266cellsConcentration:5μMIncubationTime:0-24hoursResult:ThelevelofAKTphosphorylationinU266cellsdecreased.体内研究NelfinavirMesylate(75mg/kg;i.p.;5daysaweekfor21days)decreasesmultiplemyelomacellgrowthinNOD/SCIDmice[4].AnimalModel:NOD/SCIDmice(bearingU266-luccells)[4]Dosage:75mg/kgAdministration:I.p.;5daysaweekfor21daysResult:DecreasedMMcellgrowthinNOD/SCIDmice.户使⽤本产品发表的科研⽂献•SignalTransductTargetTher.2021May29;6(1):212.•NatCommun.2020Sep4;11(1):4417.•IntJAntimicrobAgents.2019Dec;54(6):814-819.•AntiviralRes.2022Jun;202:105311.•JMedChem.2021Mar11;64(5):2725-2738.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].QiSun,etal.Bardoxoloneandbardoxolonemethyl,twoNrf2activatorsinclinicaltrials,inhibitSARS-CoV-2replicationandits3C-likeprotease.SignalTransductTargetTher.2021May29;6(1):212.[2].MondalD,etal.Nelfinavirsuppressessignalingandnitricoxideproductionbyhumanaorticendothelialcells:protectiveeffectsofthiazolidinediones.OchsnerJ.2013Spring;13(1):76-90.[3].KaldorSW,etal.Nelfinavirmesylate(AG1343):apotent,orallybioavailableinhibitorofHIV-1protease.JMedChem.1997Nov21;40(24):3979-85.[4].GillsJJ,etal.Nelfinavir,AleadHIVproteaseinhibitor,isabroad-spectrum,anticanceragentthatinducesendoplasmicreticulumstress,autophagy,andapoptosisinvitroandinvivo.ClinCancerRes.2007Sep1;13(17):5183-94.[5].BonoC,etal.Thehumanimmunodeficiencyvirus-1proteaseinhibitornelfinavirimpairsproteasomeactivityandinhibitstheproliferationofmultiplemyelomacellsinvitroandinvivo.Haematologica.2012;97(7):1101‐1109.McePdfHeight3/3MasterofBioact