SCH-23390-hydrochloride-DataSheet-生命科學試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?Agonists?ScreeningLibrarieswww.MedChemESCH-23390hydrochlorideCat.No.:HY-19545ACASNo.:125941-87-9分?式:C??H??Cl?NO分?量:324.24作?靶點:DopamineReceptor;5-HTReceptor;PotassiumChannel作?通路:GPCR/GProtein;NeuronalSignaling;MembraneTransporter/IonChannel儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:≥32mg/mL(98.69mM)掃描?維碼，H2O:28.57mg/mL(88.11mM;Needultrasonic)運?溶解?案計算器*"≥"meanssoluble,butsaturationunknown.獲得適合您實驗體系的溶解?案MassSolvent1mg5mg10mgConcentration制備儲備液1mM3.0841mL15.4207mL30.8414mL5mM0.6168mL3.0841mL6.1683mL10mM0.3084mL1.5421mL3.0841mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存?式和期限。體內(nèi)實驗請根據(jù)您的實驗動物和給藥?式選擇適當?shù)娜芙?案。以下溶解?案都請先按照InVitro?式配制澄的儲備液，再依次添加助溶劑：為保證實驗結(jié)果的可靠性，澄的儲備液可以根據(jù)儲存條件，適當保存；體內(nèi)實驗的?作液，建議您現(xiàn)?現(xiàn)配，當天使?；以下溶劑前顯?的百分?指該溶劑在您配制終溶液中的體積占?；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的?式助溶1.請依序添加每種溶劑：10%DMSO40%PEG3005%Tween-8045%salineSolubility:≥2.08mg/mL(6.42mM);Clearsolution此?案可獲得≥2.08mg/mL(6.42mM，飽和度未知)的澄溶液。以1mL?作液為例，取100μL20.8mg/mL的澄DMSO儲備液加到400μLPEG300中，混合均勻；向上述體系中加?50μLTween-80，混合均勻；然后繼續(xù)加?450μL?理鹽?定容?1mL。1/3www.MedChemEwww.MedChemEBIOLOGICALACTIVITY?物活性SCH-23390hydrochloride(R-(+)-SCH-23390hydrochloride)?種有效的選擇性的多巴胺D1樣受體拮抗劑，其對D1和D5受體的Ki分別為0.2nM和0.3nM。SCH-23390hydrochloride也?種有效的?5-HT2C受體激動劑，Ki為9.3nM。SCH-23390hydrochloride與5-HT2和5-HT1C受體具有?親和?。SCH-23390hydrochloride還抑制G蛋?偶聯(lián)的內(nèi)向整流鉀(GIRK)通道，IC50為268nM。IC50&TargetD1ReceptorD5Receptor5-HT2CReceptorGIRK0.2nM(Ki)0.3nM(Ki)9.3nM(Ki)268nM(IC50)體外研究SCH-23390(1?μM)treatmentreversestheinhibitoryeffectsofIsosibiricinonNLRP3expressionandthecleavagesofcaspase-1andIL-1βintheLPS-inducedBV-2cells.SCH-23390couldreversetheIsosibiricin-mediatedinhibitionoftheNLRP3/caspase-1inflammasomepathway[4].體內(nèi)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.戶使?本產(chǎn)品發(fā)表的科研?獻?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關注MCE中國公眾號，

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