Zoledronic-acid-disodium-tetrahydrate-Zoledronate-disodium-tetrahydrate-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEZoledronicaciddisodiumtetrahydrateCat.No.:HY-13777BCASNo.:165800-07-7Synonyms:Zoledronatedisodiumtetrahydrate;CGP42446disodiumtetrahydrate;CGP42446Adisodiumtetrahydrate;ZOL446

disodiumtetrahydrate分⼦式:C₅H₁₈N₂Na₂O₁₁P₂分⼦量:390.13作⽤靶点:Apoptosis;Autophagy作⽤通路:Apoptosis;Autophagy储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性ZoledronicAcid(Zoledronate)disodiumtetrahydrate第三代含氮⼆磷酸盐，具有⾼效的抗⾻质再吸收活性。ZoledronicAciddisodiumtetrahydrate能抑制破⾻细胞的分化和凋亡。ZoledronicAciddisodiumtetrahydrate也有抗癌作⽤[1]。体外研究ZoledronicAciddisodiumtetrahydrate(0.1-1µM;48hours)increasesreceptoractivatorofnuclearfactorkBligand(RANKL)andsclerostinmRNAexpressionsinosteocyte-likeMLO-Y4cells[2].ZoledronicAciddisodiumtetrahydrateincreasestheexpressionofosteoclastogenesissupportingfactorfromMLO-Y4cells[2].ZoledronicAciddisodiumtetrahydrateenhancestheRANKLexpressionviaIL-6/JAK2/STAT3pathwayinMLO-Y4cells[2].ZoledronicaciddisodiumtetrahydrateinhibitsosteoclastdifferentiationandfunctionthroughtheregulationofNF-κBandJNKsignallingpathways[3].ZoledronicAciddisodiumtetrahydrate(10-100µM;1-7days)markedlyreducestheviabilityofMC3T3-E1cellsandinducesapoptosisinMC3T3-E1cells[4].ZoledronicAciddisodiumtetrahydrate(10-100µM;4days)inhibitscellviabilityduetotheinductionofapoptosis[4].ZoledronicAciddisodiumtetrahydrateexertsinhibitoryeffectsonthedifferentiationandmaturationofMC3T3-E1cellsatconcentrations[4].CellViabilityAssay[4]1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemECellLine:MC3T3-E1cellsConcentration:0.01µM,0.1µM,1µM,10µM,100µMIncubationTime:1day,3days,5days,7daysResult:Reducedcellsviabilityat10µMand100µM.ApoptosisAnalysis[4]CellLine:MC3T3-E1cellsConcentration:0.01µM,0.1µM,1µM,10µM,100µMIncubationTime:1days,4days,7daysResult:Increasedthenumberofearlyapoptoticcellsandlateapoptoticornecroticcellsatdose-dependentandtime-dependent(highconcentrations).WesternBlotAnalysis[4]CellLine:MC3T3-E1cellsConcentration:0.01µM,0.1µM,1µM,10µM,100µMIncubationTime:4daysResult:Down-regulatedtheproteinlevelofinactivecaspase-3andup-regulatedtheproteinlevelofactivecaspase-3attheconcentrationsof10and100µM.体内研究ZoledronicAciddisodiumtetrahydrate(0.05mg/kg;i.p.;weekly;for3weeks)increasesbonemineraldensityandcontent[5].ZoledronicAciddisodiumtetrahydrate(0.5-1mg/kg;i.p.;weekly;for3weeks)inhibitsbothosteoclastandosteoblastsfunctionandboneremodelinginvivointerferingwithbonemechanicalproperties[5].AnimalModel:Five-week-oldC57BL6mice[5]Dosage:0.05mg/kg,0.5mg/kg,1mg/kgAdministration:Intraperitonealinjection,weekly,for3weeksResult:Inhibitedbothosteoclastandosteoblastsfunctionandboneremodelingat0.5mg/kgand1mg/kg.户使⽤本产品发表的科研⽂献2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE•OxidMedCellLongev.2021Mar31.•IntImmunopharmacol.September2022,109030.•DisMarkers.2021Oct15;2021:5838582.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].LianweiWang,etal.Variouspathwaysofzoledronicacidagainstosteoclastsandbonecancermetastasis:abriefreview.BMCCancer.2020;20:1059.[2].HyungJoonKim,etal.ZoledronateEnhancesOsteocyte-MediatedOsteoclastDifferentiationbyIL-6/RANKLAxis.IntJMolSci.2019Mar;20(6):1467.[3].Xiao-LinHuang,etal.ZoledronicacidinhibitsosteoclastdifferentiationandfunctionthroughtheregulationofNF-κBandJNKsignallingpathways.IntJMolMed.2019Aug;44(2):582-592.[4].XINHUANG,etal.Dose-dependentinhibitoryeffectsofzoledronicacidonosteoblastviabilityandfunctioninvitro.MolMedRep.2016Jan;13(1):613-622.[5].SamanthaPozzi,etal.High-dosezoledronicacidimpactsboneremodelingwitheffectsonosteoblasticlineageandbonemechanicalproperties.ClinCancerRes.2009Sep15;15(18):5829-39.[6].SheaGKH,etal.OralZoledronicacidbisphosphonateforthetreatmentofchroniclowbackpainwithassociatedModicchanges:Apilotrandomizedcontrolledtrial.JOrthopRes.2022