JNJ-54717793-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEJNJ-54717793Cat.No.:HY-134188CASNo.:1628843-99-1分⼦式:C₂₂H₁₈F₄N₆O分⼦量:458.41作⽤靶点:OrexinReceptor(OXReceptor)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:240mg/mL(523.55mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.1815mL10.9073mL21.8145mL5mM0.4363mL2.1815mL4.3629mL10mM0.2181mL1.0907mL2.1815mL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。-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%salineSolubility:≥6mg/mL(13.09mM);Clearsolution1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥6mg/mL(13.09mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性JNJ-54717793作为脑渗透剂，⼀种具有⼝服活性、选择性和⾼亲和⼒的orexin-1receptor(OX1R)拮抗剂(⾎浆EC50=85ng/mL)。JNJ-54717793的hOX1R和hOX2RKi值分别为16nM和700nM。JNJ-54717793是焦虑症的有效化合物[1][2]。IC50&TargethumanOX1RhumanOX2ROX1Receptor16nM(Ki)700nM(Ki)85ng/mL(EC50)体内研究JNJ-5471779(30mg/kg;p.o.;6hours)significantlyreducesthelatencyforrapideyemovement(REM)sleepandprolongsthetimespentinREMsleep[2].JNJ-5471779(3~30mg/kg;p.o.)attenuatesbradycardiaresponses[2].JNJ-5471779(5mg/kg;p.o.)showslowclearance[1].AnimalModel:OX2RKOmice[2]Dosage:30mg/kgAdministration:P.o.Result:Significantlyreducedthelatencyforrapideyemovement(REM)sleepandprolongedthetimespentinREMsleep.AnimalModel:Rat[2]Dosage:3~30mg/kgAdministration:P.o.Result:Attenuatedbradycardiaresponses.AnimalModel:Mouse[1]Dosage:5.0mg/kg(PharmacokineticAnalysis)Administration:P.o.Result:Clearancewasfoundtobelow.REFERENCES[1].PrévilleC,etal.SubstitutedAzabicyclo[2.2.1]heptanesasSelectiveOrexin-1Antagonists:DiscoveryofJNJ-54717793.ACSMedChem2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemELett.2020;11(10):2002-2009.Published2020Apr27.[2].BonaventureP,etal.EvaluationofJNJ-54717793aNovelBrainPenetrantSelectiveOrexin1ReceptorAntagonistinTwoRatModelsofPanicAttackProvocation.FrontPharmacol.2017;8:357.Published2017Jun9.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.