Hotline:400-820-3792Inhibitors?Agonists?ScreeningLibrariesSCH442416Cat.No.:HY-103169CASNo.:316173-57-6分?式:C??H??N?O?分?量:389.41作?靶點:AdenosineReceptor作?通路:GPCR/GProtein儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數據體外實驗DMSO:62.5mg/mL(160.50mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.5680mL12.8399mL25.6799mL5mM0.5136mL2.5680mL5.1360mL10mM0.2568mL1.2840mL2.5680mL請根據產品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存?式和期限。體內實驗請根據您的實驗動物和給藥?式選擇適當的溶解?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：為保證實驗結果的可靠性，澄的儲備液可以根據儲存條件，適當保存；體內實驗的?作液，建議您現?現配，當天使?；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沉淀、析出現象，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%DMSO40%PEG3005%Tween-8045%salineSolubility:0.2mg/mL(0.51mM);Clearsolution;Needultrasonic此?案可獲得0.2mg/mL(0.51mM)的澄溶液。以1mL?作液為例，取100μL2.0mg/mL的澄DMSO儲備液加到400μLPEG300中，混合均勻；向上述2.體系中加?50μLTween-80，混合均勻；然后繼續加?450μL?理鹽?定容?1mL。請依序添加每種溶劑：10%DMSO90%cornoilSolubility:≥0.2mg/mL(0.51mM);Clearsolution1/3此?案可獲得≥0.2mg/mL(0.51mM，飽和度未知)的澄溶液，此?案不適?于實驗周期在半個?以上的實驗。以1mL?作液為例，取100μL2.0mg/mL的澄DMSO儲備液加到900μL??油中，混合均勻。BIOLOGICALACTIVITY?物活性SCH442416?種有效，選擇性和可透過?腦屏障的腺苷A2A受體(A2AR)拮抗劑，對?和??A2AR的Ki值分別為0.048和0.5nM。SCH442416在A1R，A2BR和A3R(Ki=1111，10000，10000nM)上顯?出超過23000倍的選擇性。SCH442416可?于在??和靈長類動物?腦中對腺苷A2A受體成像。IC50&TargetIC50:0.048nM(hA2AR),0.5nM(rA2AR)[1]體外研究SCH442416isselectiveforA2AR(Ki=0.50nM)inratstriatalmembranesoverA1RandA3R(Ki=1815and>10000,respectively)[1].SCH442416(0.1-10?μM)increasestheglutaminesynthetase(GS)andglutamateaspartatetransporter(GLAST)proteinsexpressionofMüllercellsinGroup1?μM[5].體內研究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/