Seltorexant-hydrochloride-JNJ-42847922-hydrochloride-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemESeltorexanthydrochlorideCat.No.:HY-109012ACASNo.:1293284-49-7Synonyms:JNJ-42847922hydrochloride分⼦式:C₂₁H₂₃ClFN₇O分⼦量:443.91作⽤靶点:OrexinReceptor(OXReceptor)作⽤通路:GPCR/GProtein;NeuronalSignaling储存⽅式:4°C,sealedstorage,awayfrommoisture*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoisture)溶解性数据体外实验H2O:100mg/mL(225.27mM;Needultrasonic)DMSO:83.33mg/mL(187.72mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.2527mL11.2635mL22.5271mL5mM0.4505mL2.2527mL4.5054mL10mM0.2253mL1.1264mL2.2527mL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；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存⽅式和期限：-80°C,6months;-20°C,1month(sealedstorage,awayfrommoisture)。-80°C储存时，请在6个⽉内使⽤，-20°C储存时，请在1个⽉内使⽤。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%DMSO>>40%PEG300>>5%Tween-80>>45%saline1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥2.08mg/mL(4.69mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(4.69mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(4.69mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性Seltorexanthydrochloride(JNJ-42847922hydrochloride)⼀种具有⼝服活性的，⾼亲和性以及选择性的OX2R拮抗剂(⼈和⼤⿏中的OX2R的pKi值分别为8.0和8.1)。Seltorexanthydrochloride穿过⾎脑屏障，迅速占据⼤⿏⼤脑中的OX2R结合位点[1]。IC50&TargethumanOX2RratOX2R8.0(pKi)8.1(pKi)体内研究Seltorexanthydrochloride(JNJ-42847922hydrochloride)(3-30mg/kg;p.o.)dose-dependentlyinducesandprolongssleepinmaleSprague-Dawleyrats[1].Thesleep-promotingeffectsofSeltorexanthydrochloride(30mg/kg;p.o.;perdayfor7days)aremaintainedupon7-dayrepeateddosinginrats[1].AnimalModel:MaleSprague-Dawleyrats(350-450g)[1]Dosage:30mg/kgAdministration:p.o.;perdayfor7daysResult:Thereducedsleeponset(non–rapideyemovement(NREM)latency)andtheincreasedNREMsleepdurationweremaintainedupon7-dayrepeateddosingwithJNJ-42847922.TheprolongationofNREMsleeptimewasduetoasignificantincreaseinNREMboutdurationthroughoutthetreatmentperiodassessedonD1andD7.Rapideyemovement(REM)sleepwasonlymarginallyaffectedonD4oftreatment,resultinginasmallbutsignificantreductioninREMsleeplatencyandanincreaseinREMsleepduration.户使⽤本产品发表的科研⽂献•BioorgChem.2022Jun;123:105779.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].BonaventureP,etal.CharacterizationofJNJ-42847922,aSelectiveOrexin-2ReceptorAntagonist,asaClinicalCandidatefortheTreatmentofInsomnia.JPharmacolExpTher.2015Sep;354(3):471-82.2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEMcePdfHeightCaution:Producthasnotbeenfullyvalidatedforme