Zanamivir-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEZanamivirCat.No.:HY-13210CASNo.:139110-80-8分⼦式:C₁₂H₂₀N₄O₇分⼦量:332.31作⽤靶点:InfluenzaVirus;Antibiotic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H2O:≥33.33mg/mL(100.30mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制备储备液1mM3.0092mL15.0462mL30.0924mL5mM0.6018mL3.0092mL6.0185mL10mM0.3009mL1.5046mL3.0092mL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：PBS1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:9.09mg/mL(27.35mM);Clearsolution;Needultrasonicandwarmingandheatto60°CBIOLOGICALACTIVITY⽣物活性Zanamivir流感病毒的神经氨酸酶抑制剂，对于流感病毒A和B的IC50值分别为0.95nM和2.7nM。IC50&TargetIC50:0.95nM(InfluenzaA);2.7nM(InfluenzaB)[1]体外研究Zanamivirinteractswithagroupofaminoacidsintheactivesiteofneuraminidase,whichareconservedinallinfluenzaAandBstrains.Zanamivirblockstheactionofneuraminidase,whichpreventsthecleavageofsialicacidonthecellreceptors,thuspreventingreleaseandspreadofthenewlyformedvirions[2].体内研究Zanamivirhasapoorbioavailabilityinoraladministration,withonly4–17%oftheagent.Oraldeliveryofzanamivirhasbeenaproblemduetoitsstronghydrophilicnaturethatlimitsitstransportacrosstheintestinalepithelium.Permeationenhancerssuchassodiumcholate,hydroxypropylβ-cyclodextrincouldbeusedwithzanamivirtoenhancetheintestinalpermeability[3].PROTOCOLAnimalRats:FormulationsPO-SC(ZanamivirwithSCforp.o.)andPO-C(Zanamivircontrolsolutionforp.o.)areAdministration[3]administeredorallyataZanamivirdoseof10mg/kg,andIV-R(referenceZanamivirsalinesolutionfori.v.)isadministeredi.v.atadoseof1mg/kgtoratsunderconsciouscondition.Bloodsamplesarecollectedpriortoandat0.5,1,2,3,4,6,8,and24hrafteradministration.Ateachsamplingpoint,threeratsfromeachgrouparesacrificedafterbloodcollectiontoextractthelungs.Thelungsarecleansedwithsalineafterextractionoflungsfromtheratsthroughachestincision.ThelungsarethentransferredintoE-tubeandstoredinthefreezer(-80°C)untilanalysis.Plasmasamplesareharvestedbycentrifugationat1,500×gfor10minandstoredat-20°Cuntilanalysis.TheanalysisofZanamivirinbothplasmaandlungsisperformedusingbefore-mentionedLC-MS/MSmethod[3].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.户使⽤本产品发表的科研⽂献•SignalTransductTargetTher.2021Apr24;6(1):165.•AntimicrobAgentsChemother.2020Jun23;64(7):e00222-20.•PLoSOne.2018Jul12;13(7):e0200761.•bioRxiv.2020Mar.•bioRxiv.July26,2018.Seemorecustomervalidationsonwww.MedChemEREFERENCES2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE[1].GubarevaLV,etal.Comparisonoftheactivitiesofzanamivir,oseltamivir,andRWJ-270201againstclinicalisolatesofinfluenzavirusandneuraminidaseinhibitor-resistantvariants.AntimicrobAgentsChemother.2001Dec;45(12):3403-8.[2].McKimm-BreschkinJL,etal.Managementofinfluenzavirusinfectionswithneuraminidaseinhibitors:detection,incidence,andimplicationsofdrugresistance.TreatRespirMed.2005;4(2):107-16.[3].ShanmugamS,etal.Zanamiviroraldelivery:enhancedplasmaandlungbioavailabilityinrats.BiomolTher(Seoul).2013Mar;21(2):161-9.McePdfHeightCaution: