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

disodiumtetrahydrate分?式:C?H??N?Na?O??P?分?量:390.13作?靶點(diǎn):Apoptosis;Autophagy作?通路:Apoptosis;Autophagy儲(chǔ)存?式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY?物活性ZoledronicAcid(Zoledronate)disodiumtetrahydrate第三代含氮?磷酸鹽,具有?效的抗?質(zhì)再吸收活性。ZoledronicAciddisodiumtetrahydrate能抑制破?細(xì)胞的分化和凋亡。ZoledronicAciddisodiumtetrahydrate也有抗癌作?[1]。體外研究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?邊的抑制劑?師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.體內(nèi)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.戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)2/3MasterofBioactiveMolecules—您?邊的抑制劑?師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

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