PROTAC-11β-HSD1-Degrader-1-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEPROTAC11β-HSD1Degrader1Cat.No.:HY-179602分⼦式:C₅₉H₇₉N₁₁O₉S分⼦量:1118.39作⽤靶点:PROTACs;11β-HSD作⽤通路:PROTAC;MetabolicEnzyme/Protease储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性PROTAC11β-HSD1Degrader1⼀种⾼效的PROTAC，靶向11β-HSD1（11β-羟类醇脱氢酶1）。PROTAC11β-HSD1Degrader1可诱导11β-HSD1发⽣泛素-蛋⽩酶体依赖性降解。PROTAC11β-HSD1Degrader1可⽤于2型糖尿病(T2DM)的研究[1]。体外研究PROTAC11β-HSD1Degrader1(Compound25)(0.12-10μM,48h)caneffectivelydegrade11β-HSD1intheMV-4-11cellline[1].WesternBlotAnalysis[1]CellLine:MV-4-11cellConcentration:0.12μM,0.37μM,1.1μM,3μM,5μM,10μMIncubationTime:48hResult:Dose-dependentdegradationof11β-HSD1intheMV-4-11cellline.体内研究PROTAC11β-HSD1Degrader1(Compound25)(50mg/kg,i.p.,onceeverytwodaysfor2weeks)caneffectivelyimproveglucosehomeostasisinmicewithtype2diabetesinducedbyahigh-fatdiet[1].AnimalModel:6-week-oldmaleC57BL/6Jwild-typemicewerefedahigh-fatdietforeightweeks[1].Dosage:50mg/kgAdministration:I.p.,onceeverytwodaysfor2weeks1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEResult:Significantlyimprovedglucosetoleranceinmice.Enhancedglucose-stimulatedinsulinsecretion.Showedadecreasingtrendinbodyweightandrandombloodglucoselevels.REFERENCES[1].WangL,etal.Design,synthesis,andpharmacologicalevaluationofnovelPROTACdegraderstargeting11β-HSD1formetabolicdiseaseintervention[preprint].bioRxiv[Internet].2025Nov09McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:400-820-3792;021-5