NP10679-DataSheet-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemENP10679Cat.No.:HY-148825分⼦式:C₂₃H₂₆F₃N₃O₃分⼦量:449.47作⽤靶点:iGluR;HistamineReceptor;PotassiumChannel;CytochromeP450;AdrenergicReceptor作⽤通路:MembraneTransporter/IonChannel;NeuronalSignaling;GPCR/GProtein;Immunology/Inflammation;MetabolicEnzyme/Protease储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性NP10679⼀种选择性、pH依赖性的GluN2B亚特异的N-methyl-D-aspartate(NMDA)受体抑制剂，具有较⾼的⼝服⽣物利⽤度和良好的脑穿透性。NP10679在pH6.9和7.6下，抑制GluN2B的IC50分别为23和142nM。NP10679histamineH1的拮抗剂和hERG通道抑制剂，IC50分别为73和620nM。NP10679是⼀种可逆的⼈肝脏CYP酶抑制剂。IC50&TargetH1ReceptorH1ReceptorAlpha-1AadrenergicAlpha-1Aadrenergic0.073μM(IC50)0.04μM(Ki)receptorreceptor0.154μM(IC50)0.603μM(Ki)Alpha-1BadrenergicAlpha-1DadrenergicAlpha-2Cadrenergicreceptorreceptorreceptor1.92μM(Ki)0.495μM(Ki)3.09μM(Ki)体外研究NP10679(1-1000nM)showspH-dependentlyeffectstoGluN2BwithIC50sof23and142nMatpH6.9and7.6,respectively[2].NP10679showsfunctionalinhibitionto5-HT2A,αadrenergicreceptor-1A(α1A),H1-histaminereceptor(H1)andhERGchannelwithIC50valuesof1.71,0.154,0.073and0.617μM,respectively[2].NP10679showsKivaluesof2.29,0.638,1.92,0.603,1.92,0.495,3.09,0.040and0.135for5-HT1D,5-HT2A,5-HT2B,α1A,α1B,α1D,α2C,H1andserotonintransporterSERT[2].体内研究NP10679(2,5and10mg/kg;i.p.,priortotransientischemia)reducesinfarctvolumesoftransientischemiamice[2].1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEAnimalModel:MaleC57BL/6middlecerebralarteryocclusion(MCAo)modeloftransientischemiamice[2]Dosage:2,5and10mg/kgAdministration:Intraperitonealinjection;2,5and10mg/kg,15minutespriortotransientischemiaResult:Dose-dependentlyreducedinfarctvolumeswithanED50of1mg/kg.REFERENCES[1].ZaczekR,etal.Phase1ClinicalResultsforNP10679,apH-sensitiveGluN2B-selectiveN-methyl-d-aspartateReceptorInhibitor.ClinPharmacolDrugDev.2023Jan15.[2].MyersSJ,etal.AGlutamateN-Methyl-d-Aspartate(NMDA)ReceptorSubunit2B-SelectiveInhibitorofNMDAReceptorFunctionwithEnhancedPotencyatAcidicpHandOralBioavailabilityforClinicalUse.JPharmacolExpTher.2021Oct;379(1):41-52.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresea