Galidesivir-hydrochloride-BCX4430-hydrochloride-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEGalidesivirhydrochlorideCat.No.:HY-18649CASNo.:222631-44-9Synonyms:BCX4430hydrochloride;Immucillin-Ahydrochloride分⼦式:C₁₁H₁₆ClN₅O₃分⼦量:301.73作⽤靶点:DNA/RNASynthesis;SARS-CoV;Filovirus作⽤通路:CellCycle/DNADamage;Anti-infection储存⽅式:4°C,sealedstorage,awayfrommoisture*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoisture)溶解性数据体外实验DMSO:105mg/mL(347.99mM;Needultrasonic)H2O:≥41mg/mL(135.88mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制备储备液1mM3.3142mL16.5711mL33.1422mL5mM0.6628mL3.3142mL6.6284mL10mM0.3314mL1.6571mL3.3142mL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(sealedstorage,awayfrommoisture)。-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)1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥5.25mg/mL(17.40mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥5.25mg/mL(17.40mM);Clearsolution3.请依序添加每种溶剂：PBSSolubility:100mg/mL(331.42mM);Clearsolution;Needultrasonicandwarmingandheatto60°CBIOLOGICALACTIVITY⽣物活性Galidesivir(BCX4430)hydrochloride，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。Galidesivirhydrochloride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。Galidesivirhydrochloride对⼀些负义RNA病毒的EC50在~3到~68μM之间。IC50&TargetRdRpinhibitor体外研究CellularkinasesphosphorylateGalidesivir(BCX4430)hydrochloridetoatriphosphatethatmimicsATP;viralRNApolymerasesincorporatethedrug'smonophosphatenucleotideintothegrowingRNAchain,causingprematurechaintermination[1].GalidesivirhydrochlorideeffectivelyinhibitstheinfectionofVerocellswithYFV.TheEC50determinedbytheneutralreduptakeassayis8.3μg/ml(24.5μM)[3].体内研究Galidesivir(BCX4430)hydrochlorideisactiveafterintramuscular,intraperitoneal,andoraladministrationinavarietyofexperimentalinfections.InnonclinicalstudiesinvolvinglethalinfectionswithEbolavirus,Marburgvirus,RiftValleyfevervirus,andYellowFevervirus,Galidesivirhydrochloridehasdemonstratedpronouncedefficacy[1].Galidesivirhydrochloride(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.•AntiviralRes.2017Mar21;142:63-67.•AntimicrobAgentsChemother.2019Feb26;63(3):e02093-18.•Viruses.2020Jun10;12(6):628.2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE•Microorganisms.2021Mar31;9(4):734.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.McePdfHeightCa