Clozapine-N-oxide-dihydrochloride-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•Agonists•ScreeningLibrarieswww.MedChemEClozapineN-oxidedihydrochlorideCat.No.:HY-17366ACASNo.:2250025-93-3分⼦式:C₁₈H₂₁Cl₃N₄O分⼦量:415.74作⽤靶点:mAChR;DopamineReceptor;DrugMetabolite作⽤通路:GPCR/GProtein;NeuronalSignaling;MetabolicEnzyme/Protease储存⽅式:4°C,storedundernitrogen*Insolvent:-80°C,6months;-20°C,1month(storedunder

nitrogen)溶解性数据体外实验DMSO:300mg/mL(721.60mM;Needultrasonic)H2O:100mg/mL(240.53mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.4053mL12.0267mL24.0535mL5mM0.4811mL2.4053mL4.8107mL10mM0.2405mL1.2027mL2.4053mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存⽅式和期限。体内实验请根据您的实验动物和给药⽅式选择适当的溶解⽅案，配制前请先配制澄的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的⼯作液，建议您现⽤现配，当天使⽤；澄的储备液可以根据储存条件，适当保存；以下溶剂前的百分⽐指该溶剂在您配制终溶液中的体积占⽐)：1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥7.5mg/mL(18.04mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥7.5mg/mL(18.04mM);Clearsolution1/2MasterofSmallMolecules—您⾝边的抑制剂⼤师www.MedChemEBIOLOGICALACTIVITY⽣物活性ClozapineN-oxidedihydrochloride⼀种Clozapine的主代谢产物，也⼀种⼈毒蕈碱设计受体(DREADDs)激动剂。ClozapineN-oxidedihydrochloride可特异性激活DREADD受体hM3Dq。ClozapineN-oxidedihydrochloride可以穿过⾎脑屏障。Clozapine⼀种有效的多巴胺拮抗剂，也⼀种有效的选择性毒蕈碱M4受体(muscarinicM4receptor)(EC50为11nM)激动剂。IC50&TargetHumanmuscarinicdesignerreceptors(DREADDs)[1]体外研究ClozapineN-oxide(CNO)canbindtonon-DREADDreceptorsatconcentrationsrequiredforDREADDactivation,andundergoesreverse-metabolismtoitsparentcompoundclozapine,anatypicalantipsychoticthatactsatavarietyofpharmacologicaltargetsandproducesnumerousphysiologicalandbehavioraleffects[2].体内研究Afterasingleintraperitoneal(i.p.)injectionofClozapineN-oxide(1mg/kg)intomice,ClozapineN-oxide(CNO)plasmalevelspeakat15minandareverylowafter2h.Despitetheshortplasmahalf-lifeofCNOinmice,thebiologicaleffectsthathavebeendescribedafteracutetreatmentofDREADD-expressingexperimentalanimalsareusuallymuchlonger(6-10h)[1].•NatCommun.2020Jun5;11(1):2847.•BiolPsychiatry.2017May1;81(9):737-747.•ProcNatlAcadSciUSA.2019Aug13;116(33):16583-16592.•TranslPsychiatry.2020Jun20;10(1):202.•FASEBJ.2020Jul19.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].WessJ,etal.NoveldesignerreceptorstoprobeGPCRsignalingandphysiology.TrendsPharmacolSci.2013Jul;34(7):385-92.[2].ManvichDF,etal.TheDREADDagonistclozapineN-oxide(CNO)isreverse-metabolizedtoclozapineandproducesclozapine-likeinteroceptivestimuluseffectsinratsandmice.SciRep.2018Mar1;8(1):3840.[3].vanderPeetPL,etal.GramscalepreparationofclozapineN-oxide(CNO),asyntheticsmallmoleculeactuatorformuscarinicacetylcholineDREADDs.MethodsX.2018Mar23;5:257-267.[4].SilvaRR,etal.EvaluationofFunctionalSelectivityofHaloperidol,Clozapine,andLASSBio-579,anExperimentalCompoundWithAntipsychotic-LikeActionsinRodents,atGProteinandArrestinSignalingDownstreamoftheDopamineD2Receptor.FrontPharmacol.2019Jun4;10:628.[5].ZornSH,etal.ClozapineisapotentandselectivemuscarinicM4receptoragonist.EurJPharmacol.1994Nov15;269(3):R1-2.McePdfHeightCaution:Producthasnotbee