GS-6201-Standard-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors • ScreeningLibraries • Proteinswww.MedChemEGS-6201(Standard)Cat.No.:HY-10081RCASNo.:752222-83-6分子式:C₂₁H₂₁F₃N₆O₂分子量:446.43作用靶点:AdenosineReceptor;ReferenceStandards作用通路:GPCR/GProtein;Others储存方式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY生物活性GS-6201(Standard)是GS-6201(HY-10081)的分析标准品。本产品用于研究及分析应用。GS-6201(CVT-6883)是一种选择性的腺苷A2B受体拮抗剂。GS-6201对人腺苷A2B受体具有高亲和力和选择性(Ki=22nM)。GS-6201降低了小鼠急性心肌梗死(AMI)后心脏中caspase-1的活性，并减弱了心脏重塑。GS-6201减弱了致敏小鼠NECA，AMP或变应原诱导的气道反应IC50&TargetKi:22nM(humanA2Breceptors),1070nM(humanA3receptors),1940nM(humanA1receptors),3280nM(humanA2Areceptors)[1]REFERENCESElzeinE,etal.DiscoveryofanovelA2Badenosinereceptorantagonistasaclinicalcandidateforchronicinflammatoryairwaydiseases.JMedChem.2008Apr10;51(7):2267-78.ToldoS,etal.GS-6201,aselectiveblockeroftheA2Badenosinereceptor,attenuatescardiacremodelingafteracutemyocardialinfarctioninthemouse.JPharmacolExpTher.2012Dec;343(3):587-95.MustafaSJ,etal.EffectofaspecificandselectiveA(2B)adenosinereceptorantagonistonadenosineagonistAMPandallergen-inducedairwayresponsivenessandcellularinfluxinamousemodelofasthma.JPharmacolExpTher.2007Mar;320(3):1246-51.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:400-820-3792Fax:0