DC371739-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors • ScreeningLibraries • Proteinswww.MedChemEDC371739Cat.No.:HY-163794CASNo.:2135765-21-6分子式:C₂₉H₃₀N₂O₄分子量:470.56作用靶点:ANGPTL;PCSK9作用通路:MetabolicEnzyme/Protease储存方式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY生物活性DC371739是一种有效的，具有口服活性的PCSK9抑制剂。DC371739可降低PCSK9和ANGPTL3的mRNA表达。DC371739可降低PCSK9的蛋白表达并增加LDLR的蛋白表达。DC371739具有用于高脂血症研究的潜力[1][2]。体外研究DC371739(0-10µM,0-24h)increasestheratioofDiI-LDLuptakeinadose-andtime-dependentmannerinHepG2cells[2].DC371739(0-5µM;4,24,48h)decreasesthemRNAexpressionofPCSK9andANGPTL3inHepG2cells[2].DC371739(0-10µM;24h)decreasestheproteinexpressionofPCSK9andincreasestheproteinexpressionofLDLR[2].DC371739(5µM;24h)inhibitsANGPTL3transcriptionandexpressionbytargetingHNF-1α[2].RT-PCR[2]CellLine:HepG2cellsConcentration:0-5µMIncubationTime:4,24,48hResult:DecreasedthemRNAexpressionofPCSK9andANGPTL3inadoseandtimedependentmanner.WesternBlotAnalysis[2]1/2 MasterofBioactiveMolecules—您身边的抑制剂大师www.MedChemECellLine:HepG2,LO2cellsConcentration:0.5,1,2.5,5,10µMIncubationTime:24hResult:DecreasedtheproteinexpressionofPCSK9andincreasedtheproteinexpressionofLDLRinadose-dependentmanner.体内研究DC371739(10,30,100mg/kg;p.o.;dailyfor21days)decreasestheplasmalevelsoftotalcholesterol(TC),LDL-cholesterol(LDL-C)andtriglycerideinhamsters[2].AnimalModel:Six-week-oldhealthymaleSyriangoldenhamsters(HFD-fed)[2]Dosage:10,30,100mg/kgAdministration:P.o.;dailyfor21daysResult:DecreasedtheserumTClevelsofthehamsterstreatedwith10,30,or100mg/kgby29.46%,35.65%,and38.69%,theserumLDL-Clevelsweresignificantlylowerby23.25%,31.04%,and35.03%,respectively,ledtosignificantlylowerserumTGlevelsby49.57%,57.52%,and78.16%.REFERENCESBaoX,etal.Targetingproproteinconvertasesubtilisin/kexintype9(PCSK9):frombenchtobedside.SignalTransductTargetTher.2024Jan8;9(1):13.WangJ,etal.Identificationandevaluationofalipid-loweringsmallcompoundinpreclinicalmodelsandinaPhaseItrial.CellMetab.2022May3;34(5):667-680.e6.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchus