Galidesivir-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?Agonists?ScreeningLibrarieswww.MedChemEGalidesivirCat.No.:HY-18649ACASNo.:249503-25-1分?式:C??H??N?O?分?量:265.27作?靶點(diǎn):DNA/RNASynthesis;SARS-CoV;Filovirus作?通路:CellCycle/DNADamage;Anti-infection儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)H2O:1.53mg/mL(5.77mM;Needultrasonicand掃描?維碼，warming)運(yùn)?溶解?案計(jì)算器獲得適合您實(shí)驗(yàn)體系的溶解?案MassSolvent1mg5mg10mgConcentration制備儲備液1mM3.7697mL18.8487mL37.6974mL5mM0.7539mL3.7697mL7.5395mL10mM---------請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存?式和期限。BIOLOGICALACTIVITY?物活性Galidesivir(BCX4430)，?種腺苷類似物和直接作?的抗病毒藥物，能破壞病毒RNA依賴的RNA聚合酶(RdRp)活性。Galidesivir在體外對多種RNA病毒病原體具有活性，包括絲狀病毒和新興的感染因?，如MERS-CoV、SARS-CoV和SARS-CoV-2。Galidesivir對?些負(fù)義RNA病毒的EC50在~3到~68μM。IC50&TargetRdRp體外研究CellularkinasesphosphorylateGalidesivir(BCX4430)toatriphosphatethatmimicsATP;viralRNApolymerasesincorporatethedrug'smonophosphatenucleotideintothegrowingRNAchain,causing1/3www.MedChemEwww.MedChemEprematurechaintermination[1].GalidesivireffectivelyinhibitstheinfectionofVerocellswithYFV.TheEC50determinedbytheneutralreduptakeassayis8.3μg/ml(24.5μM)[3].體內(nèi)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.戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?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關(guān)注MCE中國公眾號，

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