Gala-SR-Gala-SR1078-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEGala-SRCat.No.:HY-179514CASNo.:3092129-97-7Synonyms:Gala-SR1078分⼦式:C₂₄H₂₂F₉NO₈分⼦量:623.42作⽤靶点:ROR作⽤通路:MetabolicEnzyme/Protease;VitaminDRelated/NuclearReceptor储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性Gala-SR⼀种RORα激动剂。Gala-SR通过增强昼夜节律的振幅来改节律紊乱。Gala-SR可⽤于⽛周炎的研究[1]。IC50&TargetRORα体外研究Gala-SR(1-100μM,24-72h)significantlyimprovedHumanU2OScellcompatibilitythroughgalactosemodification[1].Gala-SR(5μM,24h)significantlyupregulatesthemRNAexpressionofG6PaseandFGF21,directtargetgenesofRORα/γ,inHepG2cells[1].Gala-SR(5μM)selectivelyenhancesRORαtranscriptionalactivationactivityinHEK293Tcells[1].Gala-SR(5μM,24h)showssignificantlyreducedactivationeffectsontheG6PaseandFGF21genesafterRORαisknockeddown[1].Gala-SR(5μM)targetsandactivatesRORαprimarilythroughitshydrolyzablegalactosemodification[1].Gala-SR(2-5μM)significantlyenhancesthebioluminescencelevelsandrhythmicamplitudeoftheBMAL1andPer2reportergenesinU2OScells,andenhancestheexpressionoftheBMAL1protein[1].RealTimeqPCR[1]CellLine:HepG2cellsConcentration:5μM1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEIncubationTime:24hResult:UpregulatedthemRNAexpressionofG6PaseandFGF21,directtargetgenesofRORα/γ,inHepG2cells.体内研究Gala-SR(10mg/kg,1hbeforelightoff,i.p.,oncedailyfor2weeks)significantlyenhancestheamplitudeofactivityrhythmandtotalactivityinmice[1].Gala-SR(10mg/kg,lightson,once)enhancesliverluciferasesignalinginPER2::LUCknock-inmice,indicatingenhancedBMAL1expression[1].Gala-SR(10mg/kg,i.p.,oncedailyfor3weeks)restorestheamplitudeofperiodontaltissuerhythminperiodontalmicewithperiodontitis,inhibitstheNF-κBinflammatorypathway,andalleviatesperiodontitis-relatedboneloss[1].AnimalModel:C57BL/6Jmicewerefirstacclimatizedtoa12-hourlight/12-hourdark(L:D)conditionfor2weeks,andthenswitchedtocontinuousdarkness(D:D)toinducecircadianrhythmdisorder[1].Dosage:10mg/kgAdministration:1hourbeforetheendofthelightexposure,i.p.,oncedailyfor2weeksResult:Significantlyenhancedtheamplitudeoftheactivityrhythmandthetotalactivitylevelinmice.AnimalModel:PER2::LUCgeneknock-inmice[1].Dosage:10mg/kgAdministration:I.p.,once,lightstarttimeResult:EnhancedliverluciferasesignalingindicatesincreasedBMAL1expression.AnimalModel:MaleC57BL/6mice,2monthsold,werehousedunderdisruptedconditionsfor4weeks,andaligaturewasplacedaroundthecervixofthemaxillarysecondmolartoestablishthemurineperiodontitismodel[1].Dosage:10mg/kgAdministration:I.p.,oncedailyfor3weeksResult:Significantlyreducedalveolarboneresorption(increasedbonevolume/totalvolume,reducedboneresorptionheight).Reducedinflammatorycellinfiltrationandosteoclastactivity.Downregulatedpro-inflammatoryfactors(TNF-α,IL-6)andupregulatesanti-inflammatory2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEfactors(IL-10).REFERENCES[1].FengG,etal.Galactose-modifiedsmallmoleculemodulatortargetsRORαtoenhancecircadianrhythmandalleviateperiodontitis-associatedalveolarboneloss.BoneRes.2025Oct30;13(1):91.McePdfHeightCaution:Producthasnotbe