TCS-OX2-29-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemETCS-OX2-29Cat.No.:HY-100452CASNo.:372523-75-6分?式:C??H??N?O?分?量:397.51作?靶點(diǎn):OrexinReceptor(OXReceptor)作?通路:GPCR/GProtein;NeuronalSignaling儲(chǔ)存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:25mg/mL(62.89mM;Needultrasonic)Ethanol:25mg/mL(62.89mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM2.5157mL12.5783mL25.1566mL5mM0.5031mL2.5157mL5.0313mL10mM0.2516mL1.2578mL2.5157mL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(chǔ)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(chǔ)備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲(chǔ)存時(shí)，請?jiān)?個(gè)?內(nèi)使?，-20°C儲(chǔ)存時(shí)，請?jiān)?個(gè)?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請根據(jù)您的實(shí)驗(yàn)動(dòng)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(chǔ)備液，再依次添加助溶劑：(為保證實(shí)驗(yàn)結(jié)果的可靠性，澄的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)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.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:≥2.5mg/mL(6.29mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(6.29mM);Clearsolution3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(6.29mM);ClearsolutionBIOLOGICALACTIVITY?物活性TCS-OX2-29?種有效的，?親和?和選擇性的OX2R拮抗劑，其IC50值為40nM，pKI值為7.5。與OX1相?，TCS-OX2-29對OX2的選擇性約?了250倍。IC50&TargetOX2Receptor體外研究TCS-OX2-29inhibitsorexinAinducedIP3accumulationandERK1/2phosphorylationinCHOcellstransfectedwiththeOX2receptor[2].體內(nèi)研究TCS-OX2-29(5-10mg/kg;intraperitonealinjection;adultmaleNMRImice)treatmentsuppressesconditionedplacepreference(CPP)acquisitionandexpressioninbothna?veanddependentmicesignificantly[3].AnimalModel:440adultmaleNMRImice(25-30g)[3]Dosage:5mg/kgand10mg/kgAdministration:Intraperitonealinjection(Pharmacokineticstudy)Result:Suppressedconditionedplacepreference(CPP)acquisitionandexpressioninbothna?veanddependentmicesignificantly.戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?JPinealRes.2019Jan;66(1):e12530.?MedSciMonit.2019Apr19;25:2886-2895.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].HiroseMetal.N-acyl6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline:thefirstorexin-2receptorselectivenon-peptidicantagonist.BioorgMedChemLett,2003Dec15,13(24):4497-9.[2].RMouldetal.Bindingkineticsdifferentiatesfunctionalantagonismoforexin-2receptorligands.BrJPharmacol.2014Jan;171(2):351-363.[3].TabaeizadehM,etal.ThedifferentialeffectsofOX1RandOX2Rselectiveantagonistsonmorphineconditionedplacepreferenceinna?veversusmorphine-dependentmice.BehavBrainRes.2013Jan15;237:41-8.2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEMcePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalap