ME-3277-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors • ScreeningLibraries • Proteinswww.MedChemEME-3277Cat.No.:HY-19248CASNo.:165948-72-1分子式:C₂₀H₂₀N₂O₈S分子量:448.45作用靶点:Integrin作用通路:Cytoskeleton储存方式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY生物活性ME-3277是一种强效的GPIIb/IIIa拮抗剂。ME-3277在兔大脑中动脉(MCA)光血栓闭塞模型中可减少脑梗死，且不增加颅内出血。ME-3277可用于急性脑梗死的相关研究[1]。IC50&TargetGPIIb/IIIa体内研究ME-3277(0.15,0.3,and0.6mg/kgbolus,followedby0.125,0.25,and0.5mg/kg/hinfusion,i.v.,30minpost-photochemicalreactionfor24h)reducescerebralinfarctionwithoutenhancingintracranialhemorrhageinphotothromboticocclusionofrabbitMCA[1].AnimalModel:Rabbits(2-3kg)inducedbyphotochemicalreaction[1]Dosage:0.15,0.3,and0.6mg/kgbolus,followedby0.125,0.25,and0.5mg/kg/hinfusionAdministration:i.v.,30minpost-photochemicalreactionfor24hResult:Inhibitedexvivoplateletaggregationsignificantlyandmaintainedthroughthe24-hourperiod,withinhibitionratiosofapproximately60,80,and90%atlow,middle,andhighdoses,respectively.Prolongedbleedingtimeat2or24hoursafterthephotochemicalreactionbutbylessthan2-foldatlowdose.Significantlyprolongedthebleedingtimebyabout3-foldatboth2hoursand24hoursathighdose.Increasedthetotalreflowtimeinadose-dependentmanner.1/2 MasterofBioactiveMolecules—您身边的抑制剂大师www.MedChemESignificantlyincreasedthetotalreflowtime(31.7%vs.3.8%invehicle)andhadatendencytoimprovethe24hourspatencyathighdose.Significantlydecreasedtheneurologicscoreto3.5atalowdose,4.5atamiddledose,and3.5atahighdose,respectively.Decreasedtheinfarctvolumeoftotalandcerebralcortexareato13.1%and4.7%atalowdose,16.4%and7.1%atamiddledose,and12.9%and5.2%atahighdose,respectively.Significantlydecreasedthehemorrhagicvolume.Thehemorrhagevolumenormalizedtoinfarctvolumedidnotdiffersignificantlyamongthetreatmentgroupsandthevehiclecontrolgroup.REFERENCESKawanoKI,etal.ME3277,aGPIIb/IIIaantagonistreducescerebralinfarctionwithoutenhancingintracranialhemorrhageinphotothromboticocclusionofrabbitmiddlecerebralartery.JCerebBloodFlowMetab.2000Jun;20(6):988-97.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearch