Trimetazidine-DataSheet-生命科學(xué)試劑-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?Agonists?ScreeningLibrarieswww.MedChemETrimetazidineCat.No.:HY-B0968ACASNo.:5011-34-7分?式:C??H??N?O?分?量:266.34作?靶點(diǎn):Autophagy作?通路:Autophagy儲(chǔ)存?式:PleasestoretheproductundertherecommendedconditionsintheCOA.BIOLOGICALACTIVITY?物活性Trimetazidine?種選擇性的長(zhǎng)鏈3-ketoylcoenzymeAthiolase抑制劑，IC50值為75nM，可抑制游離脂β-氧化。Trimetazidine?種有效的抗?絞痛劑和?種細(xì)胞保護(hù)劑，具有抗氧化，抗炎，抗傷害和胃保護(hù)作?。Trimetazidine誘導(dǎo)?噬(autophagy)，還?種HADHA抑制劑。IC50&TargetIC50:75nM(longchain3-ketoylcoenzymeAthiolase)[2]β-oxidation[2]Autophagy[3]3-hydroxyacyl-CoAdehydrogenase(HADHA)[4]體外研究Trimetazidine(1-100μM;24hours;HUVECs)couldenhancetheviabilityoftheinjuredHUVECsinducedbyoxidationinacertaindose-dependentmanner[1].CellViabilityAssay[1]CellLine:Humanumbilicalveinendothelialcells(HUVECs)Concentration:1μM,10μM,100μMIncubationTime:24hoursResult:EnhancedtheviabilityoftheinjuredHUVECsinducedbyoxidation.體內(nèi)研究Trimetazidine(5-20mg/kg;oraladministration;1hour;Swissalbinomalemice)in10and20mg/kgdosessignificantlyraisestheseizure-thresholdcurrentintheICEStestinthemice[5].1/2MasterofSmallMolecules—您?邊的抑制劑?師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