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Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEIbuprofensodiumCat.No.:HY-78131CCASNo.:31121-93-4Synonyms:(±)-Ibuprofensodium分⼦式:C₁₃H₁₇NaO₂分⼦量:228.26作⽤靶点:COX;Apoptosis作⽤通路:Immunology/Inflammation;Apoptosis储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性Ibuprofen((±)-Ibuprofen)sodium⼀种具有⼝服活性的COX-1选择性抑制剂,IC50值为13μM。Ibuprofensodium抑制细胞增殖、⾎管⽣成,并诱导细胞凋亡(apoptosis)。Ibuprofensodium⼀种⾮甾体抗炎试剂和⼀氧化氮(NO)供体。Ibuprofensodium可⽤于疼痛、肿胀、炎症、感染、免疫学、癌症的研究。IC50&TargetCOX-1COX-213μM(IC50)370μM(IC50)体外研究Ibuprofensodium(24h)inhibitsCOX-1andCOX-2activitywithIC50valuesof13μMand370μM[1].Ibuprofensodium(500μM,48h)inhibitscellproliferationandangiogenesis,andinducesapoptosisinAGScells(Adenocarcinomagastriccellline)[2].Ibuprofensodium(500μM,48h)downregulatestranscriptionofAkt,VEGF-A,PCNA,Bcl2,OCT3/4andCD44genes,butupregulatesRNAlevelsofwildtypeP53andBaxgenesinAGScell[2].Ibuprofensodium(500μM,24h)restoresmicrotubulereformation,microtubule-dependentintracellularcholesteroltransport,andinducesextensionofmicrotubulestothecellperipheryinbothcysticfibrosis(CF)cellmodelsandprimaryCFnasalepithelialcells[3].Ibuprofensodium(500μM,24h)enhancesUV-inducedcelldeathinMCF-7cellsandMDA-MB-231cellsbyaphotosensitizationprocess[4].CellViabilityAssay[2]CellLine:AGScells1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEConcentration:100-1000μMIncubationTime:24h,48hResult:InhibitedAGScellviabilitywithIC50valuesof630μM(trypanbluestaining,24h),456μM(neutralredassay,24h),549μM(trypanbluestaining,48h)and408μM(neutralredassay,48h).体内研究Ibuprofensodium(fedinanimalfeedings,300mg/kg,14days)reducesoveralltumorgrowthandenhancesanti-tumorimmunecharacteristicswithoutadverseautoimmunereactionsinamodelofpostpartumbreastcancer[5].Ibuprofensodium(subcutaneousinjection,60mg/kg,everyseconddayfor15days)reducestheriskofneuropathyinaratmodelofchronicOxaliplatin‑inducedperipheralneuropathy[6].Ibuprofensodium(oraladministration,20mg/kg,every12hours,5dosestotal)decreasesmusclegrowth(averagemusclefibercross-sectionalarea)withoutaffectingregulationofsupraspinatustendonadaptionstoexercise[7].Ibuprofensodium(oraladministration,35mg/kg,twicedaily)attenuatestheInflammatoryresponsetopseudomonasaeruginosainaratmodelofchronicpulmonaryinfection[8].AnimalModel:Syngeneic(D2A1)orthotopicBalb/cmousemodelofPPBC(postpartum)[5]Dosage:300mg/kg,dailyfor14daysAdministration:Fedinanimalfeedings(addedtopulverizedstandardchowandmixeddry,thenmixedwithwater,madeintochowpelletsanddriedthoroughly)Result:Suppresedtumorgrowth,reducedpresenceofimmaturemonocytesandincreasednumbersofTcells.EnhancedTh1associatedcytokinesaswellaspromotedtumorborderaccumulationofTcells.AnimalModel:Oxaliplatin‑inducedperipheralneuropathy[6]Dosage:60mg/kg,everyseconddayfor15daysAdministration:SubcutaneousinjectionResult:Loweredsensorynerveconductionvelocity(SNCV).户使⽤本产品发表的科研⽂献•CellRep.2019Dec17;29(12):3847-3858.e5.•EMBORep.2022Apr11;e53932.2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE•Chemosphere.2019Jun;225:378-387.•Cells.2022,11(12),1870.•Phytomedicine.1September2022,154427.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].NoreenY,etal.Developmentofaradiochemicalcyclooxygenase-1and-2invitroassayforidentificationofnaturalproductsasinhibitorsofprostaglandinbiosynthesis.JNatProd.1998Jan;61(1):2-7.[2].HassanAkrami,etal.Inhibitoryeffectofibuprofenontumorsurvivalandangiogenesisingastriccancercell.TumourBiol.2015May;36(5):3237-43.[3].SharonMRymut,etal.Ibuprofenregulationofmicrotubuledynamicsincysticfibrosisepithelialcells.AmJPhysiolLungCellMolPhysiol.2016Aug1;311(2):L317-27.[4].EmmanuelleBignon,etal.IbuprofenandketoprofenpotentiateUVA-inducedcelldeathbyaphotosensitizationprocess.SciRep.2017Aug21;7(1):8885.[5].NathanDPennock,etal.Ibuprofensupportsmacrophagedifferentiation,Tcellrecruitment,andtumorsuppressioninamodelofpostpartumbreastcancer.JImmunotherCancer.2018Oct1;6(1):98.[6].ThomasKrøigård,etal.Protectiveeffectofibuprofeninaratmodelofchronicoxaliplatin-inducedperipheralneuropathy.ExpBrainRes.2019Oct;237(10):2645-2651.[7].SarahIlkhanipourRooney,etal.IbuprofenDifferentiallyAffectsSupraspinatusMuscleandTendonAdaptationstoExerciseinaRatModel.AmJSportsMed.2016Sep;44(9):2237-45.[8].MWKonstan,etal.IbuprofenattenuatestheinflammatoryresponsetoPseudomonasaeruginosainaratmodelofchronicpulmonaryinfection.Implicationsforantiinflammatorytherapyincysticfibrosis

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