SEP-363856-hydrochloride-SEP-856-hydrochloride-DataSheet-生命科學(xué)試劑-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?Agonists?ScreeningLibrarieswww.MedChemESEP-363856hydrochlorideCat.No.:HY-136109CASNo.:1310422-41-3Synonyms:SEP-856hydrochloride分?式:C?H??ClNOS分?量:219.73作?靶點(diǎn):5-HTReceptor作?通路:GPCR/GProtein;NeuronalSignaling儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:62.5mg/mL(284.44mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM4.5510mL22.7552mL45.5104mL5mM0.9102mL4.5510mL9.1021mL10mM0.4551mL2.2755mL4.5510mL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(shí)驗(yàn)請根據(jù)您的實(shí)驗(yàn)動物和給藥?式選擇適當(dāng)?shù)娜芙?案，配制前請先配制澄的儲備液，再依次添加助溶劑(為保證實(shí)驗(yàn)結(jié)果的可靠性，體內(nèi)實(shí)驗(yàn)的?作液，建議您現(xiàn)?現(xiàn)配，當(dāng)天使?；澄的儲備液可以根據(jù)儲存條件，適當(dāng)保存；以下溶劑前的百分?指該溶劑在您配制終溶液中的體積占?)：1.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥6.25mg/mL(28.44mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥6.25mg/mL(28.44mM);Clearsolution3.請依序添加每種溶劑：10%DMSO>>90%cornoil1/3MasterofSmallMolecules—您?邊的抑制劑?師www.MedChemESolubility:≥6.25mg/mL(28.44mM);ClearsolutionBIOLOGICALACTIVITY?物活性SEP-363856(SEP-856)hydrochloride具有?服活性的、中樞神經(jīng)系統(tǒng)活性的抗精神病活性化合物，具有研究精神分裂癥的潛?。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)體外研究SEP-856(10μM)shows>50%inhibitionofspecificbindingatα2A,α2B,D2,5-HT1A,5-HT1B,5-HT1D,5-HT2A,5-HT2B,5-HT2C,and5-HT7receptors[1].體內(nèi)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?邊的抑制劑?師www.MedChemEREFERENCES[1].DedicN,etal.SEP-363856,aNovelPsychotropicAgentwithaUnique,Non-D2ReceptorMechanismofAction.JPharmacolExpTher.2019Oct;371(1):1-14.McePdfHeightCaution:Producthasnotbeenfullyvalidate