EL244-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEEL244Cat.No.:HY-179580CASNo.:3047548-70-6分⼦式:C₂₅H₂₆Cl₂N₂O₅S分⼦量:537.46作⽤靶点:PPAR;Phosphodiesterase(PDE)作⽤通路:CellCycle/DNADamage;MetabolicEnzyme/Protease;VitaminDRelated/NuclearReceptor储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性EL244⼀种ATX抑制剂(IC50=50nM)和PPARγ激动剂(IC50=1.3μM;Kd=1.3μM)。EL244在⼈源HepG2细胞中显⽰出较低的细胞毒性(EC50=81.2μM)，且对⼼脏hERG钾离⼦通道的抑制作⽤极微(12%at25μM)。在体内，EL244能显著降低肺部溶⾎磷脂酸⽔平、减轻纤维化并恢复呼吸功能且全⾝吸收有限。EL244可⽤于特发性肺纤维化研究[1]。IC50&TargetPPAR-γ1.3μM(IC50)体内研究EL244(15mg/kg,15mg/kg,once)exhibitsfavorablelung-targetedpharmacokinetics,characterizedbyhighpulmonaryretention,slowlocalclearance,andlimitedsystemicabsorptionintheBLM(oropharyngealaspiration,0.8U/Kg)-inducedmicemodelofpulmonaryfibrosis[1].EL244(15mg/kg,inhaledadministration,oncedailyfor15days)beforeBLM(Bleomycin)(HY-108345)administrationhasanti-fibroticprophylacticeffectsintheBLM(oropharyngealaspiration,0.8U/Kg)-inducedmodelofpulmonaryfibrosisintheBLM(oropharyngealaspiration,0.8U/Kg)-inducedmicemodelofpulmonaryfibrosis[1].EL244(15mg/Kg,inhaledadministration,oncedailyfor7days)post-BLMadministrationhasanti-fibroticremedialeffectsintheBLM(oropharyngealaspiration,0.8U/Kg)-inducedmicemodelofpulmonaryfibrosis[1].EL244(30mg/kg,i.p.,once)demonstratesfavorablepharmacokinetics,achievingaplasmaconcentrationof40μMwithin1hour,maintaininglevelsaround35μMforupto3hours,andremainingdetectableatapproximately15μMeven9hourspost-dose,withitsmaximalpharmacodynamiceffectcoincidingatthe3-hourtimepointintheBLM(oropharyngealaspiration,0.8U/Kg)-inducedmicemodelofpulmonaryfibrosis1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE[1].AnimalModel:BLM(oropharyngealaspiration,0.8U/Kg)-inducedmice[1]Dosage:15mg/KgAdministration:Inhaledadministration,oncedailyfor7daysResult:Diminishedinflammation,Appearedfibroticregions.Restoredallassessedrespiratoryfunctionsandreducedvascularpermeability.Demonstratedstronganti-fibroticeffects,significantlyreducingsolublecollageninBALFandCol1a1expressioninlungtissue.Reducedcollagendepositionandfewerandsmallerfibroticregions.AnimalModel:BLM(oropharyngealaspiration,0.8U/Kg)-inducedmice[1]Dosage:15mg/KgAdministration:Inhaledadministration,oncedailyfor15daysResult:Improvedrespiratoryfunctions.ReducedBLM-inducedpulmonaryoedemaandinflammation.ReducedSolublecollagenlevelsinBALFandCol1a1mrnaexpressioninlungtissue.Attenuatedcollagendepositionandthereductionoffibroticregions.Notcausedanyappreciabletoxicityintheliver,asindicatedbytheALT/ASTlevels.REFERENCES[1].AlexiosN,etal.Anaerosoliseddual-actionAutotaxininhibitor-PPARγagonistforthetreatmentofpulmonaryfibrosis.Biorixiv.November13,2025.McePdfHeightCaution:Producthasnotbeenfullyvalidated