Baloxavir-Baloxavir-acid-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEBaloxavirCat.No.:HY-109025ACASNo.:1985605-59-1Synonyms:Baloxaviracid;S-033447分⼦式:C₂₄H₁₉F₂N₃O₄S分⼦量:483.49作⽤靶点:InfluenzaVirus作⽤通路:Anti-infection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:41.67mg/mL(86.19mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.0683mL10.3415mL20.6830mL5mM0.4137mL2.0683mL4.1366mL10mM0.2068mL1.0341mL2.0683mL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:≥2.08mg/mL(4.30mM);Clearsolution1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE2.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(4.30mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性Baloxavir(Baloxaviracid)，衍⽣⾃前药Baloxavirmarboxil，甲型和⼄型流感病毒聚合酶PA亚内的⼀种⾸创，有效且选择性的帽依赖性核酸内切酶(CEN)抑制剂。Baloxavir抑制病毒RNA的转录和复制，并具有强⼤的抗病毒活性[1][2]。IC50&TargetInfluenzavirus[1]Cap-dependentendonuclease(CEN)[1][2]体外研究ThemedianEC50valuesatbaselineforBaloxavir(BXA)are17.96nMforA/H1N1pdm,4.48nMforA/H3N2,and18.67nMfortypeBvirus[1].Baloxavir(BXA)inhibitsviralRNAtranscriptionviaselectiveinhibitionofcap-dependentendonuclease(CEN)activityinenzymaticassays,andinhibitsviralreplicationininfectedcellswithoutcytotoxicityincytopathiceffectassays.BaloxavirshowsbroadpotencyagainstvarioussubtypesofinfluenzaAviruses(H1N2,H5N1,H5N2,H5N6,H7N9andH9N2).Additionally,serialpassagesofthevirusesinthepresenceofBaloxavirresultinisolationofPA/I38TvariantswithreducedBXAsusceptibility[2].Baloxavir(BXA)inhibitscap-dependentendonuclease(CEN)andCEN/RdRpactivitieswithIC50valuesof2.5nMand1.6nM,respectively,whilelowpotency(IC50>40nM)isobservedagainstRdRpactivity[2].Baloxavir(BXA)hasahighinhibitorypotencyagainstCENactivityofthetestedviralribonucleoproteincomplexes(vRNPs)frominfluenzaAandBviruseswithmeanIC50valuesof1.4-3.1nMand4.5-8.9nM,respectively,indicatingthatBaloxavirhasbroadspectrumactivities.BaloxavirshowshighpotencyagainstinfluenzaAandBviruseswithmeanEC90of0.46-0.98nMand2.2-3.4nM,respectively[2].户使⽤本产品发表的科研⽂献•NatMicrobiol.2020Jan;5(1):27-33.•NatCommun.2020Jan9;11(1):164.•ProcNatlAcadSciUSA.2020Apr14;117(15):8593-8601.•PLoSPathog.2022Jul13;18(7):e1010698.•JVirol.2020Oct27;94(22):e00319-20.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].OmotoS,etal.Characterizationofinfluenzavirusvariantsinducedbytreatmentwiththeendonucleaseinhibitorbaloxavirmarboxil.SciRep.2018Jun25;8(1):9633.[2].NoshiT,etal.Invitrocharacterizationofbaloxaviracid,afirst-in-classcap-dependentendonucleaseinhibitoroftheinfluenzaviruspolymerasePAsubunit.AntiviralRes.2018Dec;160:109-117.McePdfHeight2/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemECaution:Producthasnotbeen