SB-334867-free-base-SB334867A-free-base-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemESB-334867freebaseCat.No.:HY-10895ACASNo.:792173-99-0Synonyms:SB334867Afreebase分?式:C??H??N?O?分?量:319.32作?靶點(diǎn):OrexinReceptor(OXReceptor)作?通路:GPCR/GProtein;NeuronalSignaling儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:50mg/mL(156.58mM;Needultrasonic)0.1MHCL:6mg/mL(18.79mM;ultrasonicandadjustpHto3withHCl)MassSolvent1mg5mg10mgConcentration制備儲備液1mM3.1317mL15.6583mL31.3165mL5mM0.6263mL3.1317mL6.2633mL10mM0.3132mL1.5658mL3.1317mL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(fù)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。-80°C儲存時，請在6個?內(nèi)使?，-20°C儲存時，請在1個?內(nèi)使?。體內(nèi)實驗請根據(jù)您的實驗動物和給藥?式選擇適當(dāng)?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(jié)果的可靠性，澄的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實驗的?作液，建議您現(xiàn)?現(xiàn)配，當(dāng)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)1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE1.請依序添加每種溶劑：0.5%CMC-Na/salinewaterSolubility:10mg/mL(31.32mM);Suspendedsolution;Needultrasonic2.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(7.83mM);Clearsolution3.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:2.5mg/mL(7.83mM);Suspendedsolution;Needultrasonic4.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(7.83mM);Clearsolution5.請依序添加每種溶劑：50%HP-β-CDinsalineSolubility:7.69mg/mL(24.08mM);Suspendedsolution;NeedultrasonicBIOLOGICALACTIVITY?物活性SB-334867freebase(SB334867Afreebase)?種優(yōu)良的選擇性?腦屏障通透性orexin-1(OX1)receptor拮抗劑，對OX2有選擇性(pKb=7.4)，對5-HT2B、5-HT2C的選擇性100倍，pKi值分別為5.4和5.3。SB-334867降低體內(nèi)?醇消耗量，抑制嗎啡誘導(dǎo)的對運(yùn)動活性的增敏。IC50&TargetOX2體外研究SB-334867(100?pM–?10?μM)inhibitstheorexin-A(10?nM)andorexin-B(100?nM)-inducedcalciumresponsesinaconcentration-dependentmanner,withapparentpKbvaluesof7.27±0.04and7.23±0.03,buthasnoeffectonthecalciumresponseelicitedbyUTP(3?μM),whichactivatesanendogenouspurinergicreceptorinCHO-OX1andCHO-OX2cells[4].體內(nèi)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?邊的抑制劑?師www.MedChemEAdministration:IntraperitonealinjectionResult:Reducedethanolconsumption,BECsandsuppressedsucroseintakeinmice.戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?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].?upinaM,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