Trimetazidine-DataSheet-生命科学试剂-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•Agonists•ScreeningLibrarieswww.MedChemETrimetazidineCat.No.:HY-B0968ACASNo.:5011-34-7分⼦式:C₁₄H₂₂N₂O₃分⼦量:266.34作⽤靶点:Autophagy作⽤通路:Autophagy储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCOA.BIOLOGICALACTIVITY⽣物活性Trimetazidine⼀种选择性的长链3-ketoylcoenzymeAthiolase抑制剂，IC50值为75nM，可抑制游离脂β-氧化。Trimetazidine⼀种有效的抗⼼绞痛剂和⼀种细胞保护剂，具有抗氧化，抗炎，抗伤害和胃保护作⽤。Trimetazidine诱导⾃噬(autophagy)，还⼀种HADHA抑制剂。IC50&TargetIC50:75nM(longchain3-ketoylcoenzymeAthiolase)[2]β-oxidation[2]Autophagy[3]3-hydroxyacyl-CoAdehydrogenase(HADHA)[4]体外研究Trimetazidine(1-100μM;24hours;HUVECs)couldenhancetheviabilityoftheinjuredHUVECsinducedbyoxidationinacertaindose-dependentmanner[1].CellViabilityAssay[1]CellLine:Humanumbilicalveinendothelialcells(HUVECs)Concentration:1μM,10μM,100μMIncubationTime:24hoursResult:EnhancedtheviabilityoftheinjuredHUVECsinducedbyoxidation.体内研究Trimetazidine(5-20mg/kg;oraladministration;1hour;Swissalbinomalemice)in10and20mg/kgdosessignificantlyraisestheseizure-thresholdcurrentintheICEStestinthemice[5].1/2MasterofSmallMolecules—您⾝边的抑制剂⼤师www.MedChemEAnimalModel:Swissalbinomalemice(24-35g)[4]Dosage:5mg/kg,10mg/kgand20mg/kg;10mL/kgbodyweightAdministration:Oraladministration;1hourResult:In10and20mg/kgdosessignificantlyraisedtheseizure-thresholdcurrentintheICEStest.•MolCell.2020Sep4;S1097-2765(20)30578-5.•AnatolJCardiol.2019;22:00-00.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].ShenghuHe,etal.Protectiveeffectsoftrimetazidineagainstvascularendothelialcellinjuryinducedbyoxidation.JournalofGeriatricCardiology,December2008,Vol5No4.[2].KantorPF,etal.Theantianginaldrugtrimetazidineshiftscardiacenergymetabolismfromfattyacidoxidationtoglucoseoxidationbyinhibitingmitochondriallong-chain3-ketoacylcoenzymeAthiolase.CircRes.2000Mar17;86(5):580-8.[3].JainS,etal.Trimetazidineexertsprotectionagainstincreasingcurrentelectroshockseizuretestinmice.Seizure.2010Jun;19(5):300-2.[4].ChruscielP,etal.Definingtheroleoftrimetazidineinthetreatmentofcardiovasculardisorders:someinsightsonitsroleinheartfailureandperipheralarterydisease.Drugs.2014Jun;74(9):971-80.[5].HossainF,etal.InhibitionofFattyAcidOxidationModulatesImmunosuppressiveFunctionsofMyeloid-DerivedSuppressorCellsandEnhancesCancerTherapies.CancerImmunolRes.2015Nov;3(11):1236-47.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplica