RANKL-IN-1-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors • ScreeningLibraries • Proteinswww.MedChemERANKL-IN-1Cat.No.:HY-175703分子式:C₄₀H₅₅N₅O分子量:621.9作用靶点:RANKL/RANK;ReactiveOxygenSpecies(ROS);NF-κB;p38MAPK;ERK;JNK;MMP作用通路:NF-κB;Immunology/Inflammation;MetabolicEnzyme/Protease;MAPK/ERKPathway;StemCell/Wnt储存方式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY生物活性RANKL-IN-1是一种选择性核因子-κB配体受体激活剂(RANKL)抑制剂，其KD值为7.6μM。RANKL-IN-1对破骨细胞生成具有抑制活性和选择性，其IC50值为0.07μM，SI为82.57。ANKL-IN-1直接与RANKL结合，并阻断RANKL诱导的NF-κB和MAPK通路的激活。RANKL-IN-1可用于代谢性疾病的研究，如骨质疏松症[1]。IC50&TargetMMP-9体外研究RANKL-IN-1(Compound19u)(50-400nM,4days)showsnosignificantcytotoxicityinRAW264.7cells[1].RANKL-IN-1(50-400nM,4days)inhibitsRANKL-inducedosteoclastogenesiswithoutaffectingosteoblastdifferentiationinRAW264.7cells[1].RANKL-IN-1(50-400nM,4days)reducesRANKL-inducedROSlevelsandinhibitsboneresorptioninRAW264.7cells[1].RANKL-IN-1(50-400nM,4days)inhibitstheexpressionofproteinsassociatedwithRANKL-inducedosteoclastdifferentiationinRAW264.7cells[1].Immunofluorescence[1]CellLine:RAW264.7cellsConcentration:50,100,200and400nMIncubationTime:4daysResult:DecreasedthesizeoftheF-actinring.1/3 MasterofBioactiveMolecules—您身边的抑制剂大师www.MedChemEReducedROSlevels.WesternBlotAnalysis[1]CellLine:RAW264.7cellsConcentration:50,100,200and400nMIncubationTime:4daysResult:DownregulatedtheproteinexpressionofTRAF6andphosphorylationofp65,p38,ERKandJNK.Downregulatedtheactivityofthec-Fos/NFATc1signalingandinhibitedtheexpressionofCTSKandMMP-9.体内研究RANKL-IN-1(Compound19u)(0.313-1.25μg/mL,96h)attenuatedbonelossinzebrafishosteoporosismodels[1].RANKL-IN-1(0.5-2mg/kg,p.o.,every2daysfor11weeks)preventssystemicbonelossinovariectomy-inducedosteoporosismicemodels[1].AnimalModel:Zebrafishosteoporosismodels[1]Dosage:0.313,0.625and1.25μg/mLAdministration:96hResult:Increasedzebrafishskullbonemass.AnimalModel:Ovariectomy-inducedosteoporosismicemodels[1]Dosage:0.5,1and2mg/kgAdministration:Orallyadministration,every2daysfor11weeksResult:Increasedthebonemineraldensity,bonevolumefraction,trabecularnumberandthetrabecularthickness.Reducedthetrabecularseparationandexpandedthemarrowcavityandtrabecularspacing.Reducedtotalcholesterolandtriglyceridelevelsandincreasedhigh-densitylipoproteincholesterollevels.HadnosignificantchangesinALT,ASTandBUNlevels.REFERENCES2/3 MasterofBioactiveMolecules—您身边的抑制剂大师www.MedChemEFuX,etal.Design,Synthesis,andBiologicalEvaluationofHeterocycle-FusedCelastrolDerivativesasPotentAntiosteoporosisAgentsbyBlockingRANKL-InducedActivationoftheNF-κBandMAPKSignalingPathways.JMedChem.2025Aug28;68(16):17678-17704.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformed