COX-2-IN-61-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemECOX-2-IN-61Cat.No.:HY-179700分⼦式:C₁₅H₁₃N₃O₃S₂分⼦量:347.41作⽤靶点:COX作⽤通路:Immunology/Inflammation储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性COX-2-IN-61⼀种⼝服有效的COX-2抑制剂，IC50为22µM，同时对COX-1也有抑制作⽤，IC50为43µM。COX-2-IN-61在Carrageenan(HY-125474)诱导的⼤⿏⾜⽖⽔肿模型中表现出抗炎作⽤，且安全性良好。COX-2-IN-61可⽤于炎症研究[1]。IC50&TargetCOX-1COX-243μM(IC50)22μM(IC50)体外研究COX-2-IN-61(compound4)formshydrogenbondswithArg513andAla527,andhydrophobicinteractionswithVal523,Met522,andVal349,whichcontributetoitsbindingtoCOX-2andanti-inflammatoryeffect[1].体内研究COX-2-IN-61(compound4)(50mg/kg,p.o.,singledose)demonstratessignificantanti-inflammatoryactivity,comparabletoCelecoxib(HY-14398),inaratCarrageenan-inducedpawedemamodel[1].COX-2-IN-61(50mg/kg,p.o.,dailyfor14days)showslowerulcerogenicity,cardiotoxicityandnephrotoxicityinrats,comparedtoCelecoxib[1].AnimalModel:MaleWistarrats(180-225g)inducedbyCarrageenan(1%,1mL)injection[1]Dosage:50mg/kgAdministration:p.o.,singledoseResult:Showedsignificantanti-inflammatoryactivity,with47%edemainhibitionat6hours.Demonstratedequalanti-inflammatoryactivitytoCelecoxibafter4hinterval.1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEAnimalModel:MaleWistarrats(180-225g)[1]Dosage:50mg/kgAdministration:p.o.,dailyfor14daysResult:Markedlyreducedhistopathologicaldamageofthestomach,heart,andkidney,comparedtoCelecoxib.Resultedinasignificantlylowerincreaseincardiacbiomarkers(CK-MB,troponinI,AST,LDH)andrenalinjurybiomarkers(creatinine,urea),comparedtoCelecoxib.REFERENCES[1].AbdelallEKA,etal.Synthesisandinsilicostudiesofnovelthiophene-celecoxibhybridwithexcellentcardiotoxicityandnephrotoxicitysafetyprofiles.EurJMedChem.2026;302(Pt2):118297.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:4