Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEGS-6201Cat.No.:HY-10081CASNo.:752222-83-6Synonyms:CVT-6883分?式:C??H??F?N?O?分?量:446.43作?靶點:AdenosineReceptor作?通路:GPCR/GProtein儲存?式:Powder-20°C3yearsInsolvent-80°C6months-20°C1month溶解性數據體外實驗DMSO:20mg/mL(44.80mM;ultrasonicandwarmingandheatto60°C)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.2400mL11.2000mL22.3999mL5mM0.4480mL2.2400mL4.4800mL10mM0.2240mL1.1200mL2.2400mL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；?旦配成溶液，請分裝保存，避免反復凍融造成的產品失效。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?內使?，-20°C儲存時，請在1個?內使?。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%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:2mg/mL(4.48mM);Suspendedsolution;Needultrasonic1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE2.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2mg/mL(4.48mM);ClearsolutionBIOLOGICALACTIVITY?物活性GS-6201(CVT-6883)?種選擇性的腺苷A2B受體拮抗劑。GS-6201對?腺苷A2B受體具有?親和?和選擇性(Ki=22nM)。GS-6201降低了??急性?肌梗死(AMI)后?臟中caspase-1的活性，并減弱了?臟重塑。GS-6201減弱了致敏??NECA，AMP或變應原誘導的?道反應性。IC50&TargetKi:22nM(humanA2Breceptors),1070nM(humanA3receptors),1940nM(humanA1receptors),3280nM(humanA2Areceptors)[1]體內研究GS-6201(CVT-6883)(4mg/kg;i.p.;every12hfor14days)significantlyreducesIL-6,TNF-α,E-selectin,ICAM-1,andVCAMplasmalevels[2].GS-6201(4mg/kg;i.p.;every12hfor14days)leadstoasignificantattenuationofleftandrightventricularenlargementanddysfunctionat7days,whichwasmaintainedat14daysandalsoat28days[2].GS-6201(2mg/kg;p.o.)treatmentshowstheCmax,dAUCandt1/2are1110ng/mL,6500ngh/mL,and4.25hours,respectively[1].AnimalModel:Adultout-bredmaleCD1mice(8-12weeksofage,AMImodel)[2]Dosage:4mg/kgAdministration:i.p.;every12hfor14daysResult:SignificantlyreducedIL-6,TNF-α,E-selectin,ICAM-1,andVCAMplasmalevels.AnimalModel:Sprague-Dawleyrats[1]Dosage:2mg/kgAdministration:p.o.(PharmacokineticAnalysis)Result:TheCmax,dAUCandt1/2were1110ng/mL,6500ngh/mL,and4.25hours,respectively.REFERENCES[1].ElzeinE,etal.DiscoveryofanovelA2Badenosinereceptorantagonistasaclinicalcandidateforchronicinflammatoryairwaydiseases.JMedChem.2008Apr10;51(7):2267-78.[2].ToldoS,etal.GS-6201,aselectiveblockeroftheA2Badenosinereceptor,attenuatescardiacremodelingafteracutemyocardialinfarctioninthemouse.JPharmacolExpTher.2012Dec;343(3):587-95.[3].MustafaSJ,etal.EffectofaspecificandselectiveA(2B)adenosinereceptorantagonistonadenosineagonistAMPandallergen-inducedairwayresponsivenessandcellularinfluxinamousemodelofasthma.JPharmacolExpTher.2007Mar;320(3):1246-51.2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEMcePdfHeightCaution:Producthasnotbeenfullyvalidatedf