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Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEAmantadinesulfateCat.No.:HY-B0402BCASNo.:31377-23-8Synonyms:1-Adamantanaminesulfate;1-Aminoadamantanesulfate分?式:C??H??N.?/?H?O?S分?量:200.18作?靶點(diǎn):InfluenzaVirus;Orthopoxvirus;SARS-CoV;Apoptosis;CDK;Bcl-2Family作?通路:Anti-infection;Apoptosis;CellCycle/DNADamage儲(chǔ)存?式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY?物活性Amantadine(1-Adamantanamine)sulfate?種?服有效的抗甲型流感(influenzaA)病毒的抗病毒劑。Amantadinesulfate對(duì)NMDA、M2等多種離?通道均有抑制作?,對(duì)冠狀病毒離?通道也有抑制作?。Amantadinesulfate還具有抗正痘病毒(orthopoxvirus)和抗癌活性。Amantadinesulfate可?于帕?森病,術(shù)后認(rèn)知功能障礙(POCD)和COVID-19的研究。IC50&TargetCDK2Bcl-2Bax體外研究Amantadinesulfate(0-500μM,26h)inhibitsSARS-CoV-2replication,withIC50concentrationsbetween83and119μM[4].Amantadinesulfate(0-100μg/mL,24-72h)markedlyinhibitstheproliferationofHepG2andSMMC?7721cells[6].Amantadinesulfate(0-75μg/mL,48h)arreststhecellcycleattheG0/G1phaseandinducesapoptosis[6].Amantadinesulfate(0-75μg/mL,48h)reducesthelevelsofthecellcycle?relatedgenesandproteins(cyclinD1,cyclinEandCDK2),reducesBcl-2andincreasestheBaxproteinandmRNAlevels[6].CellViabilityAssay[4]CellLine:VeroE6cellsConcentration:500μM,100μM,20μM,4μM,and8nMIncubationTime:26h1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEResult:Causedaconcentration-dependentreduction(IC50=83μM)ofviralnucleicacidsinthesupernatant26hafterinfectionat10-500μM.Causedaconcentration-dependentreduction(IC50=119μM)ofviralnucleicacidsinthecytosol26hafterinfection.CellProliferationAssay[6]CellLine:HumanHCCcelllines(HepG2andSMMC-7721)andnormalhepatocellularcells(L02cells)Concentration:0,1,2,5,10,25,50and100μg/mLIncubationTime:24,48and72hResult:Inhibitedcellularproliferationinatime-anddose-dependentmannerinHepG2andSMMC-7721cells.CellCycleAnalysis[6]CellLine:HepG2andSMMC-7721cellsConcentration:0,10,25,50and75μg/mLIncubationTime:48hResult:SignificantlyincreasedthepopulationofHepG2andSMMC-7721cellsintheG0/G1phaseinadose-dependentmanner,andsignificantlydecreasedthenumberofHepG2cellsintheSphase.ApoptosisAnalysis[6]CellLine:HepG2andSMMC-7721cellsConcentration:0,10,25,50and75μg/mLIncubationTime:48hResult:MarkedlyincreasedthepercentageofapoptoticHepG2andSMMC-7721cells(early-andlate-stageapoptosis)inadose-dependentmanner.WesternBlotAnalysis[6]CellLine:HepG2andSMMC-7721cellsConcentration:0,10,25,50and75μg/mLIncubationTime:48hResult:ShoweddownregulationofcyclinD1,cyclinEandCDK2,andshowedadecreaseinBcl-2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE2levelsandanincreaseofBaxlevelsinHepG2andSMMC-7721cells.RT-PCR[6]CellLine:HepG2andSMMC-7721cellsConcentration:0,10,25,50and75μg/mLIncubationTime:48hResult:RevealedanincreaseinBaxanddecreaseinBcl-2genes.體內(nèi)研究Amantadinesulfate(25mg/kg,IP,oncedailyfor3days)inhibitssurgeryinducedneuroinflammationandlearningandmemoryimpairment[5].AnimalModel:Fischer344rats(Four-monthold,male,290-330g,15ratseachgroup)[5]Dosage:25mg/kgAdministration:IP,oncedailyfor3days(thefirstdoseat15minbeforesurgery)Result:Inhibitedsurgeryinducedneuroinflammationandlearningandmemoryimpairment,increasedGDNF(glialcellline-derivedneurotrophicfactor)thatwasco-localizedwithglialfibrillaryacidicprotein(anastrocyticmarker)inthehippocampus.戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?SignalTransductTargetTher.2021Mar27;6(1):134.?IntJNanomedicine.2019Nov27;14:9217-9234.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].SuzukiH,etal.Emergenceofamantadine-resistantinfluenzaAviruses:epidemiologicalstudy.JInfectChemother.2003;9(3):195-200.[2].HubsherG,etal.Amantadine:thejourneyfromfightingflutotreatingParkinsondisease.Neurology.2012;78(14):1096-1099.[3].DonaldFSmee,etal.Areviewofcompoundsexhibitinganti-orthopoxvirusactivityinanimalmodels.AntiviralRes.2003Jan;57(1-2):41-52.[4].FinkK,etal.AmantadineInhibitsSARS-CoV-2InVitro.Viruses.2021Mar24;13(4):539.[5].ZhangJ,etal.Amantadinealleviatespostoperativecognitivedysfunctionpossiblybyincreasingglialcellline-derivedneurotrophicfactorinrats.Anesthesiology.2014Oct;121(4):773-85.[6].LanZ,etal.Amantadineinhibitscellularproliferationandinducestheapoptosisofhepatocellularcancercellsinvitro.IntJMolMed.2015;36(3):904-910.McePdfHeight3/3MasterofBi

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