SB-334867-free-base-SB334867A-free-base-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemESB-334867freebaseCat.No.:HY-10895ACASNo.:792173-99-0Synonyms:SB334867Afreebase分⼦式:C₁₇H₁₃N₅O₂分⼦量:319.32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:50mg/mL(156.58mM;Needultrasonic)0.1MHCL:6mg/mL(18.79mM;ultrasonicandadjustpHto3withHCl)MassSolvent1mg5mg10mgConcentration制备储备液1mM3.1317mL15.6583mL31.3165mL5mM0.6263mL3.1317mL6.2633mL10mM0.3132mL1.5658mL3.1317mL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)1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE1.请依序添加每种溶剂：0.5%CMC-Na/salinewaterSolubility:10mg/mL(31.32mM);Suspendedsolution;Needultrasonic2.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(7.83mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:2.5mg/mL(7.83mM);Suspendedsolution;Needultrasonic4.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(7.83mM);Clearsolution5.请依序添加每种溶剂：50%HP-β-CDinsalineSolubility:7.69mg/mL(24.08mM);Suspendedsolution;NeedultrasonicBIOLOGICALACTIVITY⽣物活性SB-334867freebase(SB334867Afreebase)⼀种优良的选择性⾎脑屏障通透性orexin-1(OX1)receptor拮抗剂，对OX2有选择性(pKb=7.4)，对5-HT2B、5-HT2C的选择性100倍，pKi值分别为5.4和5.3。SB-334867降低体内⼄醇消耗量，抑制吗啡诱导的对运动活性的增敏。IC50&TargetOX2体外研究SB-334867(100ꢀpM–ꢀ10ꢀμM)inhibitstheorexin-A(10ꢀnM)andorexin-B(100ꢀnM)-inducedcalciumresponsesinaconcentration-dependentmanner,withapparentpKbvaluesof7.27±0.04and7.23±0.03,buthasnoeffectonthecalciumresponseelicitedbyUTP(3ꢀμM),whichactivatesanendogenouspurinergicreceptorinCHO-OX1andCHO-OX2cells[4].体内研究SB-334867(intraperitonealinjection;20mg/kg;20days)administers15minbeforemorphineinjectioncansignificantlydecreasetheeffectofthemorphinechallengedoseinmiceincomparisonwiththesporadicallymorphine-treatedgroup[2].SB-334867(intraperitonealinjection;3,10and30mg/kg)significantlyreducesethanolintakerelativetovehicleanddoesnoteffectwaterconsumptioninfemalePrats[3].SB-334867(intraperitonealinjection;3,10and30mg/kg)reducesethanolconsumptionatthe30mg/kgdose,highdosesuppressessucroseintakerelativetovehicle,anditresultsinlowerbloodethanolconcentrations(BECs)relativetoboththe10and30mg/kgdoses[3].AnimalModel:MaleSwissmice[2]Dosage:20mg/kgAdministration:IntraperitonealinjectionResult:Inhibitedtheacquisitionofmorphine-inducedsensitizationtolocomotoractivityofmice.AnimalModel:C57BL/6JMice[3]Dosage:3,10and30mg/kg2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEAdministration:IntraperitonealinjectionResult:Reducedethanolconsumption,BECsandsuppressedsucroseintakeinmice.户使⽤本产品发表的科研⽂献•FrontNeurosci.2016Jul26;10:355.•JInflammRes.2021May18;14:2007-2017.•DrugDesDevelTher.2022Jul5;16:2145-2160.•ResearchSquarePreprint.2021Jan.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].PorterRA,etal.1,3-Biarylureasasselectivenon-peptideantagonistsoftheorexin-1receptor.BioorgMedChemLett.2001Jul23;11(14):1907-10.[2].ŁupinaM,etal.SB-334867(anOrexin-1ReceptorAntagonist)EffectsonMorphine-InducedSensitizationinMice-aViewonReceptorMechanisms.[3].AndersonRI,etal.Orexin-1andorexin-2receptorantagonistsreduceethanolself-administrationinhigh-drinkingrodentmodels.FrontNeurosci.2014Feb25;8:33.[4].SmartD,etal.SB-334867-A:thefirstselectiveorexin-1receptorantagonist.BrJPharmacol.2001Mar;132(6):1179-82.McePdfHe