SCH442416-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•Agonists•ScreeningLibrariesSCH442416Cat.No.:HY-103169CASNo.:316173-57-6分⼦式:C₂₀H₁₉N₇O₂分⼦量:389.41作⽤靶点:AdenosineReceptor作⽤通路:GPCR/GProtein储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:62.5mg/mL(160.50mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.5680mL12.8399mL25.6799mL5mM0.5136mL2.5680mL5.1360mL10mM0.2568mL1.2840mL2.5680mL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，并请注意储备液的保存⽅式和期限。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%DMSO40%PEG3005%Tween-8045%salineSolubility:0.2mg/mL(0.51mM);Clearsolution;Needultrasonic此⽅案可获得0.2mg/mL(0.51mM)的澄溶液。以1mL⼯作液为例，取100μL2.0mg/mL的澄DMSO储备液加到400μLPEG300中，混合均匀；向上述2.体系中加⼊50μLTween-80，混合均匀；然后继续加⼊450μL⽣理盐⽔定容⾄1mL。请依序添加每种溶剂：10%DMSO90%cornoilSolubility:≥0.2mg/mL(0.51mM);Clearsolution1/3此⽅案可获得≥0.2mg/mL(0.51mM，饱和度未知)的澄溶液，此⽅案不适⽤于实验周期在半个⽉以上的实验。以1mL⼯作液为例，取100μL2.0mg/mL的澄DMSO储备液加到900μL⽟⽶油中，混合均匀。BIOLOGICALACTIVITY⽣物活性SCH442416⼀种有效，选择性和可透过⾎脑屏障的腺苷A2A受体(A2AR)拮抗剂，对⼈和⼤⿏A2AR的Ki值分别为0.048和0.5nM。SCH442416在A1R，A2BR和A3R(Ki=1111，10000，10000nM)上显⽰出超过23000倍的选择性。SCH442416可⽤于在⼤⿏和灵长类动物⼤脑中对腺苷A2A受体成像。IC50&TargetIC50:0.048nM(hA2AR),0.5nM(rA2AR)[1]体外研究SCH442416isselectiveforA2AR(Ki=0.50nM)inratstriatalmembranesoverA1RandA3R(Ki=1815and>10000,respectively)[1].SCH442416(0.1-10ꢀμM)increasestheglutaminesynthetase(GS)andglutamateaspartatetransporter(GLAST)proteinsexpressionofMüllercellsinGroup1ꢀμM[5].体内研究SCH-442416(0.017mg/kg;i.p.)completelyabrogatestheCGS-21680-induceddecreaseinskeletalmuscleinjury[3].SCH-442416(1μM•2μL;i.v.)increasestheGSandGLASTproteinexpressioninrats[5].SCH442416(1μM)significantlyattenuatestheadenosine-induceddilation(from15.3to5.6μm)[4].REFERENCES[1].ToddeS,et,al.Design,radiosynthesis,andbiodistributionofanewpotentandselectiveligandforinvivoimagingoftheadenosineA(2A)receptorsystemusingpositronemissiontomography.JMedChem.2000Nov16;43(23):4359-62.[2].MorescoRM,et,al.InvivoimagingofadenosineA2Areceptorsinratandprimatebrainusing[11C]SCH442416.EurJNuclMedMolImaging.2005Apr;32(4):405-13.[3].ZhengJ,et,al.ProtectiverolesofadenosineA1,A2A,andA3receptorsinskeletalmuscleischemiaandreperfusioninjury.AmJPhysiolHeartCircPhysiol.2007Dec;293(6):H3685-91.[4].MaimonN,et,al.Pre-exposuretoadenosine,actingviaA(2A)receptorsonendothelialcells,alterstheproteinkinaseAdependenceofadenosine-induceddilationinskeletalmuscleresistancearterioles.JPhysiol.2014Jun15;592(12):2575-90.[5].YuJ,et,al.A2ARAntagonistsUpregulateExpressionofGSandGLASTinRatHypoxiaModel.BiomedResInt.2020Oct26;2020:2054293.McePdfHeight2/