5-AIQ-5-Aminoisoquinolin-1-one-DataSheet-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemE5-AIQCat.No.:HY-W006566CASNo.:93117-08-9Synonyms:5-Aminoisoquinolin-1-one分⼦式:C₉H₈N₂O分⼦量:160.17作⽤靶点:PARP作⽤通路:CellCycle/DNADamage;Epigenetics储存⽅式:4°C,protectfromlight*Insolvent:-80°C,6months;-20°C,1month(protectfrom

light)BIOLOGICALACTIVITY⽣物活性5-AIQ(5-Aminoisoquinolin-1-one)⼀种⽔溶性的PARP-1抑制剂。5-AIQ多种药物中的⼀个重官能团。5-AIQ减少肝脏缺⾎再灌注相关的组织损伤，可⽤于肝脏缺⾎再灌注相关治疗条件的研究。IC50&TargetPARP-1体外研究5-AIQ(5000μg)significantlyreducesthenumberofcoloniesofTA98withoutmetabolicactivation,andTA98andTA1537withmetabolicactivation[1].体内研究5-AIQ(150and250mg/kg;p.o.;once)possessnosignificantlygenotoxicinvivosystembymicronucleustest[1].5-AIQ(3mg/kg;p.o.;5minpriortoonsetofliverischemia)reducesthetissueinjuryassociatedwithischemia-reperfusionoftheliver[2].AnimalModel:Malemice[1]Dosage:150and250mg/kgAdministration:Oraladministration;150and250mg/kg;onceResult:Showednoincreaseofmicronucleatedpolychromaticerythrocytes(MNPCE)inboth24hand48hafterboth125and250mg/kgdurationexposureascomparedtothecorrespondingcontrol.1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEAnimalModel:AnesthetisedmaleWistarratswithliverischemia(for30minutes)andreperfusion(for2hours)[2]Dosage:3mg/kgAdministration:Intravenousinjection;3mg/kg;5minpriortoonsetofliverischemiaResult:ReducedPARPactivationandshowedlessstainingforICAM-1.REFERENCES[1].VinodKR,ChandraS,SharmaSK.Evaluationof5-aminoisoquinoline(5-AIQ),anovelPARP-1inhibitorforgenotoxicitypotentialinvitroandinvivo.ToxicolMechMethods.2010Feb;20(2):90-5.[2].Mota-FilipeH,etal.ThenovelPARPinhibitor5-aminoisoquinolinonereducestheliverinjurycausedbyischemiaandreperfusionintherat.MedSciMonit.2002Nov;8(11):BR444-53.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:400-