TCS-OX2-29-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemETCS-OX2-29Cat.No.:HY-100452CASNo.:372523-75-6分⼦式:C₂₃H₃₁N₃O₃分⼦量:397.51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:25mg/mL(62.89mM;Needultrasonic)Ethanol:25mg/mL(62.89mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.5157mL12.5783mL25.1566mL5mM0.5031mL2.5157mL5.0313mL10mM0.2516mL1.2578mL2.5157mL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%saline1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥2.5mg/mL(6.29mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(6.29mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(6.29mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性TCS-OX2-29⼀种有效的，⾼亲和⼒和选择性的OX2R拮抗剂，其IC50值为40nM，pKI值为7.5。与OX1相⽐，TCS-OX2-29对OX2的选择性约⾼了250倍。IC50&TargetOX2Receptor体外研究TCS-OX2-29inhibitsorexinAinducedIP3accumulationandERK1/2phosphorylationinCHOcellstransfectedwiththeOX2receptor[2].体内研究TCS-OX2-29(5-10mg/kg;intraperitonealinjection;adultmaleNMRImice)treatmentsuppressesconditionedplacepreference(CPP)acquisitionandexpressioninbothnaïveanddependentmicesignificantly[3].AnimalModel:440adultmaleNMRImice(25-30g)[3]Dosage:5mg/kgand10mg/kgAdministration:Intraperitonealinjection(Pharmacokineticstudy)Result:Suppressedconditionedplacepreference(CPP)acquisitionandexpressioninbothnaïveanddependentmicesignificantly.户使⽤本产品发表的科研⽂献•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.ThedifferentialeffectsofOX1RandOX2Rselectiveantagonistsonmorphineconditionedplacepreferenceinnaïveversusmorphine-dependentmice.BehavBrainRes.2013Jan15;237:41-8.2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEMcePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalap