Zileuton-A-64077-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEZileutonCat.No.:HY-14164CASNo.:111406-87-2Synonyms:A64077;Abbott64077分?式:C??H??N?O?S分?量:236.29作?靶點(diǎn):Lipoxygenase;Ferroptosis作?通路:MetabolicEnzyme/Protease;Apoptosis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:≥100mg/mL(423.21mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM4.2321mL21.1604mL42.3209mL5mM0.8464mL4.2321mL8.4642mL10mM0.4232mL2.1160mL4.2321mL請(qǐng)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(qǐng)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(qǐng)?jiān)?個(gè)?內(nèi)使?，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請(qǐng)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(qǐng)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)1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE1.請(qǐng)依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥10mg/mL(42.32mM);Clearsolution2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥10mg/mL(42.32mM);Clearsolution3.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥10mg/mL(42.32mM);ClearsolutionBIOLOGICALACTIVITY?物活性Zileuton有效，選擇性的5-脂氧合酶抑制劑，具有抗哮喘特性。IC50&Target5-LOX體外研究Inanti-CD3-treatedcells,IL-2decreasesinzileuton-treatedanduntreatedcellswithincreasingincubationtime.ZileutonlikelyreducesIL-2levelsbyinhibiting5-lipoxygenase,henceleukotrieneB4production,anIL-2inducer[2].體內(nèi)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.戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)2/3MasterofBioactiveMolecules—您?邊的抑制劑?師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