Xanthine-oxidase-IN-21-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEXanthineoxidase-IN-21Cat.No.:HY-180271分⼦式:C₂₀H₂₂N₂O₃分⼦量:338.4作⽤靶点:XanthineOxidase;NF-κB;TNFReceptor;InterleukinRelated;URAT1;GLUT作⽤通路:MetabolicEnzyme/Protease;NF-κB;Apoptosis;Immunology/Inflammation;MembraneTransporter/IonChannel储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性Xanthineoxidase-IN-21，⼀种Genipin(HY-17389)衍⽣物，⼝服有效的嘌呤氧化酶(XOD)的混合竞争性抑制剂，IC50为0.68μM。Xanthineoxidase-IN-21通过降低α-SMA表达来减轻肾纤维化，并通过NF-κB通路调节抑制促炎细胞因⼦IL-1β、IL-6和TNF-α。Xanthineoxidase-IN-21还能抑制URAT1和GLUT9的表达，促进尿酸排泄，降低⾎尿酸⽔平。Xanthineoxidase-IN-21具有显著的肝肾保护作⽤，可⽤于⾼尿酸⾎症的研究。IC50&TargetXanthineoxidaseNF-κBIL-1βIL-60.68μM(IC50)体外研究Xanthineoxidase-IN-21(compound5b)(0.1,1,10,100,and200μM;24h)isnon-cytotoxicitytoHK-2cells[1].体内研究Xanthineoxidase-IN-21(compound5b)(10-30mg/kg,oral,daily,for2weeks)reducesuricacidlevels,protectsliverandkidneyfunction,andamelioratesinflammationandfibrosisinHyperuricemicmice[1].AnimalModel:AhyperuricemiamodelwasestablishedinKM(male,20g)byinjectionofAdenine(HY-B0152)andPotassiumoxonate(PO)(HY-17511)[1]Dosage:10mg/kg,20mg/kg,30mg/kgAdministration:Oral;daily;for2weeksResult:Significantlyreducedserumuricacid(UA)levels,creatinine(Cr),andbloodureanitrogen1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE(BUN)inhyperuricemicmice.AlsodecreasedthelevelsofASTandALT,indicatingprotectionofliverandkidneyfunction.Amelioratedkidneyandliverdamage,reducedinflammatorycytokinelevels(IL-1β,IL-6,TNF-α),anddecreasedtheexpressionofpro-inflammatorymarkers(p-ERK,p-p38,p65NF-κB).Reducedtheexpressionofuricacidtransporters(URAT1,GLUT9)andinhibitedXODactivity,whichisakeytargetinhyperuricemia.REFERENCES[1].SunH,etal.Synthesisandbiologicalevaluationofgenipinderivativesasnovelxanthineoxidaseinhibitorsfortheanti-hyperuricemiaandhepatorenalprotectionactivity.BioorgChem.2025;167:109279.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly