SEP-363856-hydrochloride-SEP-856-hydrochloride-DataSheet-生命科学试剂-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•Agonists•ScreeningLibrarieswww.MedChemESEP-363856hydrochlorideCat.No.:HY-136109CASNo.:1310422-41-3Synonyms:SEP-856hydrochloride分⼦式:C₉H₁₄ClNOS分⼦量:219.73作⽤靶点:5-HTReceptor作⽤通路:GPCR/GProtein;NeuronalSignaling储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:62.5mg/mL(284.44mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM4.5510mL22.7552mL45.5104mL5mM0.9102mL4.5510mL9.1021mL10mM0.4551mL2.2755mL4.5510mL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:≥6.25mg/mL(28.44mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥6.25mg/mL(28.44mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoil1/3MasterofSmallMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥6.25mg/mL(28.44mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性SEP-363856(SEP-856)hydrochloride具有⼝服活性的、中枢神经系统活性的抗精神病活性化合物，具有研究精神分裂症的潜⼒。IC50&Target5-HT1AReceptor5-HT1BReceptor5-HT1DReceptor5-HT2AReceptor2.3μM(EC50)15.6μM(EC50)0.262μM(EC50)>10μM(EC50)5-HT2CReceptor5-HT7ReceptorTAAR130μM(EC50)6.7μM(EC50)0.140μM(EC50)体外研究SEP-856(10μM)shows>50%inhibitionofspecificbindingatα2A,α2B,D2,5-HT1A,5-HT1B,5-HT1D,5-HT2A,5-HT2B,5-HT2C,and5-HT7receptors[1].体内研究SEP-856(0.3,1and10mg/kg,i.p.)isCNSactiveandexhibitsabehavioralsignaturesimilartoknownantipsychoticdrugs[1].SEP-856(0.3,1and10mg/kg,orallyonce)significantlyreducesPCP-inducedhyperactivity[1].OralSEP-856administration(1,3and10mg/kg)producesadosedependentdecreaseinREMsleep,increaseinlatencytoREMsleepandincreaseincumulativewake(W)time[1].AnimalModel:Acutetreatmentwithphencyclidine(PCP),whichinducesrobusthyperactivityinrodents[1].Dosage:0.3,1and3mg/kg.Administration:Orallyonce.Result:Resultedinadose-dependentinhibitionofPCP-inducedhyperactivityresponsesinC57Bl/6Jmice(1-wayANOVAF(5,59)=18.96,p<0.0001;Tukey’spost-hoctest,p<0.05)witha50%effectivedose(ED50)ofapproximately0.3mg/kg.AnimalModel:MaleSpragueDawleyrats[1].Dosage:1,2,and5mg/kg.Administration:I.V.injection.(PharmacokineticAnalysis).Result:Rapidlyabsorbedwithmaximumplasmaandbrainconcentrationsreachedwithin0.25to0.5hoursinmiceandratsandmaximumplasmaconcentrationsreachedwithin6±2.83hoursinmonkeys.Penetratedmouseandratbrainsafteroraladministration(10mg/kg),withaveragebrain-to-plasmaAUCratiosof~3respectively.2/3MasterofSmallMolecules—您⾝边的抑制剂⼤师www.MedChemEREFERENCES[1].DedicN,etal.SEP-363856,aNovelPsychotropicAgentwithaUnique,Non-D2ReceptorMechanismofAction.JPharmacolExpTher.2019Oct;371(1):1-14.McePdfHeightCaution:Producthasnotbeenfullyvalidate