A-804598-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEA-804598Cat.No.:HY-100483CASNo.:1125758-85-1分⼦式:C₁₉H₁₇N₅分⼦量:315.37作⽤靶点:P2XReceptor作⽤通路:MembraneTransporter/IonChannel储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:≥32mg/mL(101.47mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制备储备液1mM3.1709mL15.8544mL31.7088mL5mM0.6342mL3.1709mL6.3418mL10mM0.3171mL1.5854mL3.1709mL请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存⽅式和期限：-80°C,6months;-20°C,1month。-80°C储存时，请在6个⽉内使⽤，-20°C储存时，请在1个⽉内使⽤。体内实验请根据您的实验动物和给药⽅式选择适当的溶解⽅案。以下溶解⽅案都请先按照InVitro⽅式配制澄的储备液，再依次添加助溶剂：(为保证实验结果的可靠性，澄的储备液可以根据储存条件，适当保存；体内实验的⼯作液，建议您现⽤现配，当天使⽤；以下溶剂前显⽰的百分⽐指该溶剂在您配制终溶液中的体积占⽐；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的⽅式助溶)1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%saline1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥2.5mg/mL(7.93mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:2.5mg/mL(7.93mM);Clearsolution;Needultrasonic3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(7.93mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性A-804598⼀个CNS渗透，竞争性和选择性的P2X7受体拮抗剂，作⽤于⼩⿏，⼤⿏和⼈的P2X7受体，IC50s分别9nM,10nM和11nM。IC50&TargetIC50:9nM(mouseP2X7receptor),10nM(ratP2X7receptor),11nM(humanP2X7receptor)[1]体外研究Pre-incubationwithA-804598(0.1-10μM;1hour)significantlyattenuatesBzATP-inducedcelllossinaconcentration-dependentmanner.3μMA-804598exhibitsthegreatestprotectiveeffectagainstBzATP-inducedcytotoxicity[2].CellCytotoxicityAssay[2]CellLine:microglialcellConcentration:0.1,0.3,1,3,10μMIncubationTime:1hourResult:ProtectedagainstBzATP-inducedcytotoxicityinbothinactivatedandactivatedmicroglia.体内研究AchronitreatmentwithA-804598(intraperitonealinjection;30mg/kg;fivetimesaweek)decreasestheexpressionofLC3B-IIandSQSTM1/p62inlumbarspinalcordatendstageofdisease[3].AnimalModel:AdultB6.Cg-Tg(SOD1-G93A)1Gur/Jfemalemice[3]Dosage:30mg/kgAdministration:Intraperitonealinjection;fivetimesaweekResult:DecreasedSQSTM1/p62expression.户使⽤本产品发表的科研⽂献•CellCycle.2021Jan18;1-10.Seemorecustomervalidationsonwww.MedChemEREFERENCES2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE[1].Donnelly-RobertsDLetal.[3H]A-804598([3H]2-cyano-1-[(1S)-1-phenylethyl]-3-quinolin-5-ylguanidine)isanovel,potent,andselectiveantagonistradioligandforP2X7receptors.Neuropharmacology,2009Jan,56(1):223-9.[2].YingboHeetal.TheroleofmicroglialP2X7:modulationofcelldeathandcytokinerelease.Neuroinflammation,2017Jul,14(1):135.[3].PaolaFabbrizioetal.P2X7ReceptorActivationModulatesAutophagyinSOD1-G93AMouseMicroglia.CellNeurosci,2017Aug,11:249.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformed