Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEA-804598Cat.No.:HY-100483CASNo.:1125758-85-1分?式:C??H??N?分?量:315.37作?靶點(diǎn):P2XReceptor作?通路:MembraneTransporter/IonChannel儲(chǔ)存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:≥32mg/mL(101.47mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM3.1709mL15.8544mL31.7088mL5mM0.6342mL3.1709mL6.3418mL10mM0.3171mL1.5854mL3.1709mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；?旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲(chǔ)備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲(chǔ)存時(shí)，請?jiān)?個(gè)?內(nèi)使?，-20°C儲(chǔ)存時(shí)，請?jiān)?個(gè)?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥?式選擇適當(dāng)?shù)娜芙?案。以下溶解?案都請先按照InVitro?式配制澄的儲(chǔ)備液，再依次添加助溶劑：(為保證實(shí)驗(yàn)結(jié)果的可靠性，澄的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的?作液，建議您現(xiàn)?現(xiàn)配，當(dāng)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(xiàn)沉淀、析出現(xiàn)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%saline1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:≥2.5mg/mL(7.93mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:2.5mg/mL(7.93mM);Clearsolution;Needultrasonic3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(7.93mM);ClearsolutionBIOLOGICALACTIVITY?物活性A-804598?個(gè)CNS滲透，競爭性和選擇性的P2X7受體拮抗劑，作?于??，??和?的P2X7受體，IC50s分別9nM,10nM和11nM。IC50&TargetIC50:9nM(mouseP2X7receptor),10nM(ratP2X7receptor),11nM(humanP2X7receptor)[1]體外研究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.體內(nèi)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.戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?CellCycle.2021Jan18;1-10.Seemorecustomervalidationsonwww.MedChemEREFERENCES2/3MasterofBioactiveMolecules—您?邊的抑制劑?師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