SCH-23390-hydrochloride-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•Agonists•ScreeningLibrarieswww.MedChemESCH-23390hydrochlorideCat.No.:HY-19545ACASNo.:125941-87-9分⼦式:C₁₇H₁₉Cl₂NO分⼦量:324.24作⽤靶点:DopamineReceptor;5-HTReceptor;PotassiumChannel作⽤通路:GPCR/GProtein;NeuronalSignaling;MembraneTransporter/IonChannel储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:≥32mg/mL(98.69mM)扫描⼆维码，H2O:28.57mg/mL(88.11mM;Needultrasonic)运⽤溶解⽅案计算器*"≥"meanssoluble,butsaturationunknown.获得适合您实验体系的溶解⽅案MassSolvent1mg5mg10mgConcentration制备储备液1mM3.0841mL15.4207mL30.8414mL5mM0.6168mL3.0841mL6.1683mL10mM0.3084mL1.5421mL3.0841mL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。以下溶解⽅案都请先按照InVitro⽅式配制澄的储备液，再依次添加助溶剂：为保证实验结果的可靠性，澄的储备液可以根据储存条件，适当保存；体内实验的⼯作液，建议您现⽤现配，当天使⽤；以下溶剂前显⽰的百分⽐指该溶剂在您配制终溶液中的体积占⽐；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的⽅式助溶1.请依序添加每种溶剂：10%DMSO40%PEG3005%Tween-8045%salineSolubility:≥2.08mg/mL(6.42mM);Clearsolution此⽅案可获得≥2.08mg/mL(6.42mM，饱和度未知)的澄溶液。以1mL⼯作液为例，取100μL20.8mg/mL的澄DMSO储备液加到400μLPEG300中，混合均匀；向上述体系中加⼊50μLTween-80，混合均匀；然后继续加⼊450μL⽣理盐⽔定容⾄1mL。1/3www.MedChemEwww.MedChemEBIOLOGICALACTIVITY⽣物活性SCH-23390hydrochloride(R-(+)-SCH-23390hydrochloride)⼀种有效的选择性的多巴胺D1样受体拮抗剂，其对D1和D5受体的Ki分别为0.2nM和0.3nM。SCH-23390hydrochloride也⼀种有效的⼈5-HT2C受体激动剂，Ki为9.3nM。SCH-23390hydrochloride与5-HT2和5-HT1C受体具有⾼亲和⼒。SCH-23390hydrochloride还抑制G蛋⽩偶联的内向整流钾(GIRK)通道，IC50为268nM。IC50&TargetD1ReceptorD5Receptor5-HT2CReceptorGIRK0.2nM(Ki)0.3nM(Ki)9.3nM(Ki)268nM(IC50)体外研究SCH-23390(1ꢀμM)treatmentreversestheinhibitoryeffectsofIsosibiricinonNLRP3expressionandthecleavagesofcaspase-1andIL-1βintheLPS-inducedBV-2cells.SCH-23390couldreversetheIsosibiricin-mediatedinhibitionoftheNLRP3/caspase-1inflammasomepathway[4].体内研究SCH-23390canabolishgeneralizedseizuresevokedbythechemoconvulsants.SCH-23390hasalsobeenusedinstudiesofotherneurologicaldisordersinwhichthedopaminesystemhasbeenimplicated,suchaspsychosisandParkinson'sdisease.Apartfromthestudyofneurologicaldisorders,SCH-23390hasbeenextensivelyusedasatoolinthetopographicaldeterminationofbrainD1receptorsinrodents,nonhumanprimates,andhumans[1].SCH-23390isaveryshort-actingcompoundwithaneliminationhalf-lifeofaround25minfollowingadministrationof0.3mg/herat[1].SCH-23390augmentsdopamine-inducedductusconstrictioninCD-1mousevesselsundernewbornO2conditions[5].PROTOCOLAnimalRats:Allratsreceiveacclimatizationsalineinjectionsthetwoafternoons1priorto2theirtestday.AttheendAdministration[5]oftheTrainingphase,rats(n=15or16rats/group)areassignedtoone3ofthreeconditions(0,1,or10μg/kgIPinjectionsofSCH23390).ThedayfollowingtheTrainingphase,ratsaretestedintheoperant6conditioningchambersforsaccharincue-reactivity(saccharinseeking)[5].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.户使⽤本产品发表的科研⽂献•NatCommun.2020Feb18;11(1):941.•Microbiome.2020Aug20;8(1):120.•ActaPharmacolSin.2020Feb;41(2):173-180.•IntImmunopharmacol.2020Nov;88:106963.Seemorecustomervalidationsonwww.MedChemEREFERENCES2/3www.MedChemEwww.MedChemE[1].BourneJA,etal.SCH23390:thefirstselectivedopamineD1-likereceptorantagonist.CNSDrugRev.2001Winter;7(4):399-414.[2].MillanMJ,etal.The"selective"dopamineD1receptorantagonist,SCH23390,isapotentandhighefficacyagonistatclonedhumanserotonin2Creceptors.Psychopharmacology(Berl).2001Jun;156(1):58-62.[3].KuzhikandathilEV,etal.ClassicD1dopaminereceptorantagonistR-(+)-7-chloro-8-hydroxy-3-methyl-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepinehydrochloride(SCH23390)directlyinhibitsGprotein-coupledinwardlyrectifyingpotassiumchannels.MolPharmacol.2002Jul;62(1):119-26.[4].WangYH,etal.IsosibiricininhibitsmicroglialactivationbytargetingthedopamineD1/D2receptor-dependentNLRP3/caspase-1inflammasomepathway.ActaPharmacolSin.2020Feb;41(2):173-180.[5].CrockettSL,etal.Roleofdopamineandselectivedopaminereceptoragonistsonmouseductusarteriosustoneandresponsiveness.PediatrRes.2019Dec9.McePdfHeight关注MCE中国公众号，

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