ABT-702-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors • ScreeningLibraries • Proteinswww.MedChemEABT-702Cat.No.:HY-112482CASNo.:214697-26-4分子式:C₂₂H₁₉BrN₆O分子量:463.33作用靶点:AdenosineKinase;AdenosineReceptor作用通路:MetabolicEnzyme/Protease;NeuronalSignaling;GPCR/GProtein储存方式:Powder-20°C3yearsInsolvent-80°C6months-20°C1monthBIOLOGICALACTIVITY生物活性ABT-702是一种强效、具有口服活性且选择性的腺苷激酶(AK)抑制剂，其IC50值为1.7nM。ABT-702对腺苷激酶的选择性比对其他生物靶点(包括环氧合酶-1和-2)的选择性高出1300倍以上。ABT-702通过提高游离腺苷水平来减轻糖尿病视网膜病变中的炎症。ABT-702在体内表现出镇痛和抗炎作用。ABT-702可用于糖尿病视网膜病变的相关研究[1][2][3]。IC50&TargetIC50:1.7nM(Adenosinekinase,AK)[1]体外研究ABT-702(5-50μM,30min)inhibitsamadori-glycated-albumin(AGA)-inducedTNF-αreleaseinadose-dependentmannerinAGA-treatedmicroglialcellsviatheadenosineA2AAreceptor(A2AAR)[2].体内研究ABT-702(0.6-100µmol/kg,i.p.orp.o.,singledose)showsdose-dependentanalgesicandanti-inflammatoryeffectsinrats[1].ABT-702(1.5mg/kg,i.p.,twiceaweekfor8weeks)melioratesdiabeticretinopathyinmicebyattenuatingretinalinflammation,oxidativestress,andcelldeath[2].ABT-702(3mg/kg,i.p.,10minutespre-FDG)inducessignificantregionalhypometabolisminthecerebellum,mesencephalicregion,andmedullainrats[3].AnimalModel:Malerats[1]Dosage:0.6-100µmol/kg1/3 MasterofBioactiveMolecules—您身边的抑制剂大师www.MedChemEAdministration:i.p.,singledoseResult:Showedpotent,dose-dependentantinociceptiveeffectsacrossmultiplepainmodels,includinginflammatorythermalhyperalgesia,formalintest,andnerveinjury-inducedtactileallodynia.Demonstratedsignificantanti-inflammatoryeffectsbyreducingcarrageenan-inducedpawedema.Exhibitedanon-opioidmechanismofaction,asitseffectswerenotreversedbytheopioidantagonistnaloxone.Showedlesspotentialfordevelopingantinociceptivetolerancecomparedtomorphine.AnimalModel:Malerats[1]Dosage:5-100µmol/kgAdministration:p.o.,singledoseResult:Showedpotent,dose-dependentantinociceptiveeffectsacrossmultiplepainmodels,includinginflammatorythermalhyperalgesia,formalintest,andnerveinjury-inducedtactileallodynia.Demonstratedsignificantanti-inflammatoryeffectsbyreducingcarrageenan-inducedpawedema.Theantinociceptiveandanti-inflammatoryeffectswereblockedbyselectiveadenosinereceptorantagonists,confirminganadenosine-dependentmechanism.Exhibitedanon-opioidmechanismofaction.Showedlesspotentialfordevelopingantinociceptivetolerancecomparedtomorphine.Hadnosignificanteffectsonexploratorylocomotoractivityatloweranalgesicdoses.Reducedlocomotoractivitybutdidnotimpairmotorcoordinationathigherdoses.Hadnosignificanteffectsonheartrateormeanarterialpressureatdosesprovidingmaximalanti-hyperalgesia.AnimalModel:MaleC57BL/6J(8weeks)intraperitoneallyinjectedwithStreptozotocin(45mg/kg,5consecutivedays)toinducediabetes[2]Dosage:1.5mg/kgAdministration:i.p.,twiceaweekfor8weeksResult:Showednoeffectsonfinalbodyweightandbloodglucoselevelsindiabeticmice.Showedlowersignsofinflammation(ICAM-1,TNF-α,andmicroglialactivationmarkerIba1)comparedtocontrolanimalsreceivingthevehicle.SuppressedtheupregulationofA₂AreceptorandreducedENT1expression.Reducedoxidativeandnitrosativestressintheretina.BlockedthediabeticeffectonAKindiabeticmiceascomparedwithvehicle-treated2/3 MasterofBioactiveMolecules—您身边的抑制剂大师www.MedChemEdiabeticmice.Blockedcelldeath(decreasedcleavedcaspase-3andTUNEL-positivecells)indiabeticmicebutdidnotaffecttreatednormalcontrols.AnimalModel:Rats[3]Dosage:3mg/kgAdministration:i.p.,10minutespre-FDGResult:Showedsignificantregionalhypometabolisminthecerebellum,mesencephalicregion,andmedullacomparedtothevehicle-treatedrats.客户使用本产品发表的科研文献Cell.2025Oct30;188(22):6151-6169.e24.CellDeathDiscov.2023Jul26;9(1):262.NeurochemRes.2024Nov16;50(1):13.Seemorecustomervalidationsonwww.MedChemEREFERENCESElsherbinyNM,etal.ABT-702,anadenosinekinaseinhibitor,attenuatesinflammationindiabeticretinopathy.LifeSci.2013Jul30;93(2-3):78-88.JarvisMF,etal.ABT-702(4-amino-5-(3-bromophenyl)-7-(6-morpholinopyridin-3-yl)pyrido[2,3-d]pyrimidine),anovelorallyeffectiveadenosinekinaseinhibitorwithanalgesicandanti-inflammatoryproperties:I.Invitrocharacterizationandacuteantinociceptiveeffectsinthemouse.JPharmacolExpTher.2000Dec;295(3):1156-64.ParkinsonFE,etal.TheEffectofEndogenousAdenosineonNeuronalActivityinRats:AnFDGPETStudy.JNeuroimaging.