Zileuton-A-64077-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEZileutonCat.No.:HY-14164CASNo.:111406-87-2Synonyms:A64077;Abbott64077分⼦式:C₁₁H₁₂N₂O₂S分⼦量:236.29作⽤靶点:Lipoxygenase;Ferroptosis作⽤通路:MetabolicEnzyme/Protease;Apoptosis储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:≥100mg/mL(423.21mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制备储备液1mM4.2321mL21.1604mL42.3209mL5mM0.8464mL4.2321mL8.4642mL10mM0.4232mL2.1160mL4.2321mL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)1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥10mg/mL(42.32mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥10mg/mL(42.32mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥10mg/mL(42.32mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性Zileuton有效，选择性的5-脂氧合酶抑制剂，具有抗哮喘特性。IC50&Target5-LOX体外研究Inanti-CD3-treatedcells,IL-2decreasesinzileuton-treatedanduntreatedcellswithincreasingincubationtime.ZileutonlikelyreducesIL-2levelsbyinhibiting5-lipoxygenase,henceleukotrieneB4production,anIL-2inducer[2].体内研究Inzileuton(5mg/kg,p.o.)treatedI/Rrat,theeffectofzileutontodecreaseNF-κBexpressiondoesnotchangesignificantlyinthepresenceofCOXinhibitors,andthegrouprevealssignificantlylowerlevelofNF-κBstaining.Zileuton(5mg/kg,p.o.)treatmentgiventoI/Rratsdecreasesapoptoticindexsignificantly.ZileutonhasnosignificanteffectonincreasedserumTNF-αlevelsinI/Rgroup[1].Zileuton(1,200mg/kg)inhibitsthepolypformationinAPCΔ468colonandsmallintestine.Zileutontreatmentinhibitstheproliferationratesofnonepithelialcellsinpolyps,andincreasestheapoptosisratesinpolypsinrat.ThereissignificantincreaseinthenumberofapoptoticcellsintheZileuton-treatedcellsbothinsmallintestineandinthecolon.ThereducedproliferationratemaysignificantlycontributetothereductionofpolyposisinboththesmallintestineandcolonofZileuton-fedAPCΔ468mice[3].PROTOCOLAnimalRats:Ratsarerandomizedinto6groups(n=12pergroup):shamI/Rgroup,I/Rgroup,zileuton+I/Rgroup,Administration[1]zileuton+indomethacin+I/Rgroup,zileuton+ketorolac+I/Rgroup,andzileuton+nimesulide+I/Rgroup.5-LOXinhibitorzileuton(5mg/kg,orallytwicedaily)isgivenaloneorwithnon-selectiveCOXinhibitorindomethacin(5mg/kg,intraperitoneally),selectiveCOX-1inhibitorketorolac(10mg/kg,orally)orselectiveCOX-2inhibitornimesulide(10mg/kg,subcutaneously).COXinhibitorsaregiven15minutesbeforezileutonadministration.Alldrugsaregivenfor3dayspriortoI/RorshamI/Rprocedure.Doseofzileuton(5mg/kg,twicedaily)isusedinthisstudy.RatsinshamI/Rgroupreceivethevehicleofzileutonorally.Zileutonisdissolvedindimethylsulfoxide(DMSO)andfurtherdilutionsaremadeusingsalinetoachieveafinalDMSOconcentrationof1%.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.户使⽤本产品发表的科研⽂献2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE•EmergMicrobesInfect.2022Dec;11(1):1806-1818.•JCachexiaSarcopeniaMuscle.2022Jun9.•OxidMedCellLongev.2022Feb9;2022:4295208.•OxidMedCellLongev.2019Nov3;2019:7536803.•IntJMolSci.2022Apr28;23(9):4910.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].AbueidL,etal.Inhibitionof5-lipoxygenasebyzileutoninaratmodelofmyocardialinfarction.AnatolJCardiol.2016Nov10[2].KuvibidilaS,etal.HydroxyureaandZileutonDifferentiallyModulateCellProliferationandInterleukin-2SecretionbyMurineSpleenCells:PossibleImplicationontheImmuneFunctionandRiskofPainCrisisinPatientswithSickleCellDisease.Ochsner[3].GounarisE,etal.Zileuton,5-lipoxygenaseinhibitor,actsasachemopreventiveagentinintestinalpolyposis,bymodulatingpolypandsystemicinflammation.PLoSOne.2015Mar6;10