ICI-63197-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors • ScreeningLibraries • Proteinswww.MedChemEICI-63197Cat.No.:HY-103024CASNo.:27277-00-5分子式:C₉H₁₃N₅O分子量:207.23作用靶点:Phosphodiesterase(PDE)作用通路:MetabolicEnzyme/Protease储存方式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY生物活性ICI-63197是一种磷酸二酯酶3(PDE3)和PDE4抑制剂，Ki值分别为9µM和10µM。ICI-63197对PDE1和PDE2具有选择性。ICI-63197具有抗抑郁作用[1][2]。IC50&TargetPDE3/PDEⅢPDEⅣPDEⅠPDEⅡ9μM(Ki)10μM(Ki)487μM(Ki)>1000μM(Ki)体外研究Inrabbitisolatedpulmonaryarterypreviouslyincubatedwith[3H]-noradrenaline,ICI-63197(30μM)significantlyenhancesthestimulation-inducedoutflowofradioactivity[3].Atastimulationfrequencyof2Hzinmouseatria,ICI-63197(30μM)showsnoeffectonthestimulation-inducedoutflow[3].体内研究Thirtyandninetyminutesafterintraperitonealadministration,ICI63197,0.48-29.9µmol/kg,dose-dependentlyantagonizedtheReserpineinducedhypothermiainmice[2].ICI-63197potentiatesthelocomotorstimulatoryeffectofdopamineoroftheergotdopamineagonistLisurideadministereddirectlyintothenucleusaccumbensofrats.ICI-63197haspropertyofenhancingcentralnoradrenergictransmission[2].REFERENCESMHoey,etal.Identificationandselectiveinhibitionoffourdistinctsolubleformsofcyclicnucleotidephosphodiesteraseactivityfromkidney.BiochemPharmacol.1990Jul15;40(2):193-202.HWachtel.Potentialantidepressantactivityofrolipramandotherselectivecyclicadenosine3',5'-monophosphatephosphodiesteraseinhibitors.Neuropharmacology.1983Mar;22(3):267-72.1/2 MasterofBioactiveMolecules—您身边的抑制剂大师www.MedChemEHJohnston,etal.Prejunctionalbeta-adrenoceptorsinrabbitpulmonaryarteryandmouseatria:effectofalpha-adrenoceptorblockadeandphosphodiesteraseinhibition.BrJPharmacol.1986Mar;87(3):553-62.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:400-82