Seltorexant-hydrochloride-JNJ-42847922-hydrochloride-DataSheet-生命科學試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemESeltorexanthydrochlorideCat.No.:HY-109012ACASNo.:1293284-49-7Synonyms:JNJ-42847922hydrochloride分?式:C??H??ClFN?O分?量:443.91作?靶點:OrexinReceptor(OXReceptor)作?通路:GPCR/GProtein;NeuronalSignaling儲存?式:4°C,sealedstorage,awayfrommoisture*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoisture)溶解性數(shù)據(jù)體外實驗H2O:100mg/mL(225.27mM;Needultrasonic)DMSO:83.33mg/mL(187.72mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.2527mL11.2635mL22.5271mL5mM0.4505mL2.2527mL4.5054mL10mM0.2253mL1.1264mL2.2527mL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；?旦配成溶液，請分裝保存，避免反復凍融造成的產(chǎn)品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month(sealedstorage,awayfrommoisture)。-80°C儲存時，請在6個?內使?，-20°C儲存時，請在1個?內使?。體內實驗請根據(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%DMSO>>40%PEG300>>5%Tween-80>>45%saline1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:≥2.08mg/mL(4.69mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(4.69mM);Clearsolution3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(4.69mM);ClearsolutionBIOLOGICALACTIVITY?物活性Seltorexanthydrochloride(JNJ-42847922hydrochloride)?種具有?服活性的，?親和性以及選擇性的OX2R拮抗劑(?和??中的OX2R的pKi值分別為8.0和8.1)。Seltorexanthydrochloride穿過?腦屏障，迅速占據(jù)???腦中的OX2R結合位點[1]。IC50&TargethumanOX2RratOX2R8.0(pKi)8.1(pKi)體內研究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.戶使?本產(chǎn)品發(fā)表的科研?獻?BioorgChem.2022Jun;123:105779.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].BonaventureP,etal.CharacterizationofJNJ-42847922,aSelectiveOrexin-2ReceptorAntagonist,asaClinicalCandidatefortheTreatmentofInsomnia.JPharmacolExpTher.2015Sep;354(3):471-82.2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEMcePdfHeightCaution:Producthasnotbeenfullyvalidatedforme