Galidesivir-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•Agonists•ScreeningLibrarieswww.MedChemEGalidesivirCat.No.:HY-18649ACASNo.:249503-25-1分⼦式:C₁₁H₁₅N₅O₃分⼦量:265.27作⽤靶点:DNA/RNASynthesis;SARS-CoV;Filovirus作⽤通路:CellCycle/DNADamage;Anti-infection储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验H2O:1.53mg/mL(5.77mM;Needultrasonicand扫描⼆维码，warming)运⽤溶解⽅案计算器获得适合您实验体系的溶解⽅案MassSolvent1mg5mg10mgConcentration制备储备液1mM3.7697mL18.8487mL37.6974mL5mM0.7539mL3.7697mL7.5395mL10mM---------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，并请注意储备液的保存⽅式和期限。BIOLOGICALACTIVITY⽣物活性Galidesivir(BCX4430)，⼀种腺苷类似物和直接作⽤的抗病毒药物，能破坏病毒RNA依赖的RNA聚合酶(RdRp)活性。Galidesivir在体外对多种RNA病毒病原体具有活性，包括丝状病毒和新兴的感染因⼦，如MERS-CoV、SARS-CoV和SARS-CoV-2。Galidesivir对⼀些负义RNA病毒的EC50在~3到~68μM。IC50&TargetRdRp体外研究CellularkinasesphosphorylateGalidesivir(BCX4430)toatriphosphatethatmimicsATP;viralRNApolymerasesincorporatethedrug'smonophosphatenucleotideintothegrowingRNAchain,causing1/3www.MedChemEwww.MedChemEprematurechaintermination[1].GalidesivireffectivelyinhibitstheinfectionofVerocellswithYFV.TheEC50determinedbytheneutralreduptakeassayis8.3μg/ml(24.5μM)[3].体内研究Galidesivir(BCX4430)isactiveafterintramuscular,intraperitoneal,andoraladministrationinavarietyofexperimentalinfections.InnonclinicalstudiesinvolvinglethalinfectionswithEbolavirus,Marburgvirus,RiftValleyfevervirus,andYellowFevervirus,Galidesivirhasdemonstratedpronouncedefficacy[1].Galidesivir(4mg/kg;i.p.;twicedailyfor7days)iseffectivelyinahamstermodelofyellowfever(YF)[4].AnimalModel:FemaleSyriangoldenhamsters(hamstersinfectedwithYFvirus)[4]Dosage:4mg/kgofbodyweightAdministration:I.p.;twicedailyfor7daysResult:SignificantlyimprovedthesurvivalofhamstersinfectedwithYFV.户使⽤本产品发表的科研⽂献•NucleicAcidsRes.2021Jan8;49(D1):D1113-D1121.•AntimicrobAgentsChemother.2019Feb26;63(3):e02093-18.•Microorganisms.2021Mar31;9(4):734.•AntiviralRes.2017Mar21;142:63-67.•Viruses.2020Jun10;12(6):628.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].ElfikyAA,etal.ICN-1229,Remdesivir,PSI-7977,Galidesivir,andGS1278againstSARS-CoV-2RNAdependentRNApolymerase(RdRp):Amoleculardockingstudy.LifeSci.2020Mar25:117592.[2].TaylorR,etal.BCX4430-Abroad-spectrumantiviraladenosinenucleosideanalogunderdevelopmentforthetreatmentofEbolavirusdisease.JInfectPublicHealth.2016;9(3):220-226.[3].WarrenTK,etal.Protectionagainstfilovirusdiseasesbyanovelbroad-spectrumnucleosideanalogueBCX4430.Nature.2014;508(7496):402-405.[4].JulanderJG,etal.BCX4430,anovelnucleosideanalog,effectivelytreatsyellowfeverinaHamstermodel.AntimicrobAgentsChemother.2014;58(11):6607-6614.McePdfHeight2/3www.MedChemEwww.MedChemE关注MCE中国公众号，

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