Keap1-Nrf2-IN-20-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEKeap1-Nrf2-IN-20Cat.No.:HY-158055分⼦式:C₄₂H₆₇N₁₁O₁₉分⼦量:1030.04作⽤靶点:Keap1-Nrf2作⽤通路:NF-κB储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性Keap1-Nrf2-IN-20(CompoundZC9)Keap-Nrf2通路的抑制剂，KD2为51nM。Keap1-Nrf2-IN-20具有良好的细胞通透性、细胞活性和代谢稳定性(⾎中的半衰期为t1/2>24h)[1]。体外研究Keap1-Nrf2-IN-20(15-60μM)inhibitsexpressionsofTNF-αandIL-6inLPS(HY-D1056)-inducedinflammationinmouseperitonealmacrophages,exhibitsanti-inflammatoryefficacy[1].体内研究Keap1-Nrf2-IN-20(20-80mg/kg,tailveininjection,singledose)attenuatesLPS-inducedacutelunginjuryinC57BL/6micemodel[1].Keap1-Nrf2-IN-20(56mg/kg,iv,singledose)exhibitsasatisfactorypharmacokineticprofilsinSpragueDawleyrats,thehalftime(T1/2),clearancerate(CL),areaundercurve(AUC)andapparentdistributionvolume(V)are0.22h,3.90L/h/kg,14344.57h·ng/mLand1.26L/kg,respectively[1].AnimalModel:LPS-inducedacutelunginjuryinC57BL/6micemodel[1]Dosage:20-80mg/kgAdministration:tailveininjection,singledoseResult:Maintainedintactalveolarstructure,reducedinflammatorycellinfiltration,bleedingpointsorcongestion.REFERENCES[1].ZouJ,etal.,CyclicPeptideKeap1-Nrf2Protein-ProteinInteractionInhibitors:Design,Synthesis,andInVivoTreatmentofAcuteLung1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEInjury.JMedChem.2024Mar28;67(6):4889-4903.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:400-820-3792;021-589559