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当前位置： 首页 > 产品中心 > Small_molecule > Medchemexpress/Dexamethasone(Synonyms: MK 125; NSC 34521; Prednisolone F)/HY-14648/1g
商品详细Medchemexpress/Dexamethasone(Synonyms: MK 125; NSC 34521; Prednisolone F)/HY-14648/1g
Medchemexpress/Dexamethasone(Synonyms: MK 125; NSC 34521; Prednisolone F)/HY-14648/1g
Medchemexpress/Dexamethasone(Synonyms: MK 125; NSC 34521; Prednisolone F)/HY-14648/1g
商品编号： HY-14648-10mM*1mLinDMSO
品牌： MedChemExp
市场价： ¥1980.00
美元价： 1188.00
产地： 美国(厂家直采)
公司：
产品分类： 小分子
公司分类： Small_molecule
联系Q Q： 3392242852
电话号码： 4000-520-616
电子邮箱： info@ebiomall.com
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商品介绍
DexamethasoneisaglucocorticoidreceptoragoNIST.
Description

Dexamethasoneisaglucocorticoidreceptoragonist.

IC50&Target

Glucocorticoidreceptor[1]

InVitro

Dexamethasoneregulatesseveraltranscriptionfactors,includingactivatorprotein-1,nuclearfactor-AT,andnuclearfactor-kB,leADIngtotheactivationandrepressionofkeygenesinvolvedintheinflammatoryresponse[1].Dexamethasonepotentlyinhibitsgranulocyte-macrophagecolonystimulatingfactor(GM-CSF)releasefromA549cellswithEC50of2.2nM.Dexamethasone(EC50=36nM)inducestranscriptionoftheβ2-receptorisfoundtocorrelatewithglucocorticoidreceptor(GR)DNAbindingandoccurredat10-100foldhigherconcentrationsthantheinhibitionofGM-CSFrelease.Dexamethasone(IC50=0.5nM)inhibitsa3×κB(NF-κB,IκBα,andI-κBβ),whichisassociatedwithinhibitionofGM-CSFrelease[2].

InVivo

IthaspreviouslybeenreportedthattreatmentwithDexamethasoneatadoseof2×5mg/kgefficientlyinhibitslipopolysaccharide(LPS)-inducedinflammation.Inourexperimentalsystem,treatmentwithasingledoseofDexamethasone10mg/kg(i.p.)significantlydecreasesrecruitmentofgranulocytesaswellasspontaneousproductionofoxygenradicalscomparedwithanimalsexposetoLPSandinjectedwithsolventalone(saline).Theeffectsarestatisticallysignificantwhenadministeredboth1hbeforeand1hafterinhalationofLPS.ThenumberofgranulocytesinBALFdecreasedtolevelscomparabletohealthyanimals(givenanaerosolofwater)[3].RatstreatedwithDexamethasoneconsumelessfoodandweighedlessthancontrolrats.Treatedratsalsoweighlessthanpair-fedanimalsthoughtheirfoodintakeissimilar.FivedaysofDexamethasoneinjectionresultinasignificantincreaseinboththelivermass(+42%)andthelivertobodyweightratio(+65%).Thewetweightofgastrocnemiusmuscledecreases20%after5daysoftreatment,butitremainsunaffectedrelativetobodyweight(g/100gbodyweight),indicatingthatmuscleweightlossparalleledbodyweightloss[4].

References

  • [1].LaLoneCA,etal.Effectsofaglucocorticoidreceptoragonist,Dexamethasone,onfatheadminnowreproduction,growth,anddevelopment.EnvironToxicolChem.2012Mar;31(3):611-22.

    [2].AdcockIM,etal.Ligand-induceddifferentiationofglucocorticoidreceptor(GR)trans-repressionandtransactivation:preferentialtargettingofNF-kappaBandlackofI-kappaBinvolvement.BrJPharmacol.1999Jun;127(4):1003-11.

    [3].RocksénD,etal.Differentialanti-inflammatoryandanti-oxidativeeffectsofDexamethasoneandN-acetylcysteineinendotoxin-inducedlunginflammation.ClinExpImmunol.2000Nov;122(2):249-56.

    [4].RousselD,etal.Dexamethasonetreatmentspecificallyincreasesthebasalprotonconductanceofratlivermitochondria.FEBSLett.2003Apr24;541(1-3):75-9.

    [5].MaherHM,etal.Simultaneousdeterminationofselectedtyrosinekinaseinhibitorswithcorticosteroidsandantiemeticsinratplasmabysolidphaseextractionandultra-performanceliquidchromatography-tandemmassspectrometry:Applicationtopharmacokineticinteractionstudies.JPharmBiomedAnal.2016May30;124:216-27.

    [6].QixiongZhang,etal.Structure-PropertyCorrelationsofReactiveOxygenSpecies-ResponsiveandHydrogenPeroxide-EliminatingMaterialswithAnti-OxidantandAnti-InflammatoryActivities.ChemMater.2017,29(19):8221-8238.

PreparingStockSolutions
ConcentrationVolumeMass1mg5mg10mg
1mM2.5480mL12.7402mL25.4803mL
5mM0.5096mL2.5480mL5.0961mL
10mM0.2548mL1.2740mL2.5480mL
Pleaserefertothesolubilityinformationtoselecttheappropriatesolvent.
AnimalAdministration
[3][4]

Dexamethasoneispreparedinsaline(Mice)[3].
Dexamethasoneispreparedin0.9%NaCl(Rat)[4].

Mice[3]
FemaleC57Bl/6JBommice(age10-12weeks)areusedinallexperiments.Dexamethasoneisadministeredasasingleinjectionof1or10mg/kg.Dexamethasoneisdissolvedinsalineand400μLareinjectedintraperitoneally,either1hbeforeor1hafterLPSexposure.Inoneexperiment,N-acetylcysteine(NAC)(100and500mg/kg)isinjectedsuccessivelyevery4•5h,starting1hbeforechallenge(fiveinjectionsintotal).AcontrolgroupofLPS-exposedanimalsareinjectedintraperitoneallywithsolventalone(saline).Intratrachealadministrationisperformedbyinstillationof100μLNAC(50,100or500mg/kg)orDexamethasone(10mg/kg)intothelungsofmiceanaesthetizedwith15mg/kgRapinovet(i.v.).
Rat[4]
MaleSprague-Dawleyratsareused.Dexamethasone-treatedratsareinjectedintraperitoneallyoncedailywithDexamethasone(1.5mg/kgbodyweight)for5daysandareallowedtofeedadlibitum.TheDexamethasonedose(1.5mg/kg/day)andthedurationoftreatment(5days)arespecificallychosenasthistreatmentinducedareproducIBLeandmarkedcatabolicstate.Controlratsreceivednotreatmentandarefedadlibitum.InordertotakeintoaccountthedecreaseinfoodintakeinducedbyDexamethasonetreatment,athirdgroupofpair-fedratsareused.TheseratsareprovidedwiththesameamountoffoodasDexamethasone-injectedratsandaretreatedwithadailyisovolumicintraperitonealinjectionofNaCl(0.9%)for5days.AfterthefinalinjectionofDexamethasoneorNaCl,theanimalsarefastedovernightpriortobeingkilledbydecapitation.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

References

  • [1].LaLoneCA,etal.Effectsofaglucocorticoidreceptoragonist,Dexamethasone,onfatheadminnowreproduction,growth,anddevelopment.EnvironToxicolChem.2012Mar;31(3):611-22.

    [2].AdcockIM,etal.Ligand-induceddifferentiationofglucocorticoidreceptor(GR)trans-repressionandtransactivation:preferentialtargettingofNF-kappaBandlackofI-kappaBinvolvement.BrJPharmacol.1999Jun;127(4):1003-11.

    [3].RocksénD,etal.Differentialanti-inflammatoryandanti-oxidativeeffectsofDexamethasoneandN-acetylcysteineinendotoxin-inducedlunginflammation.ClinExpImmunol.2000Nov;122(2):249-56.

    [4].RousselD,etal.Dexamethasonetreatmentspecificallyincreasesthebasalprotonconductanceofratlivermitochondria.FEBSLett.2003Apr24;541(1-3):75-9.

    [5].MaherHM,etal.Simultaneousdeterminationofselectedtyrosinekinaseinhibitorswithcorticosteroidsandantiemeticsinratplasmabysolidphaseextractionandultra-performanceliquidchromatography-tandemmassspectrometry:Applicationtopharmacokineticinteractionstudies.JPharmBiomedAnal.2016May30;124:216-27.

    [6].QixiongZhang,etal.Structure-PropertyCorrelationsofReactiveOxygenSpecies-ResponsiveandHydrogenPeroxide-EliminatingMaterialswithAnti-OxidantandAnti-InflammatoryActivities.ChemMater.2017,29(19):8221-8238.

MolecularWeight

392.46

Formula

C₂₂H₂₉FO₅

CASNo.

50-02-2

Storage
Powder-20°C3years
 4°C2years
Insolvent-80°C6months
 -20°C1month
Shipping

RoomtemperatureincontinentalUS;mayvaryelsewhere

Solvent&Solubility

DMSO:≥56mg/mL

Invivo:insolubleinsaline(<0.1="">
Dexamethasone(DEX)sUSPensionispreparedseparatelybytrituratinganappropriateweightofDexamethasonewithaqueousmethylcellulose(0.5%,w/v)toformsuspensionswithconcentrationsof1.2mg/mL(DEX)[5].
Dexamethasone(DXM)ispreparedinsaline[6].

*"<1 mg/ml"="" means="" slightly="" soluble="" or="" insoluble.="" "≥"="" means="" soluble,="" but="" saturation="">

References

  • [1].LaLoneCA,etal.Effectsofaglucocorticoidreceptoragonist,Dexamethasone,onfatheadminnowreproduction,growth,anddevelopment.EnvironToxicolChem.2012Mar;31(3):611-22.

    [2].AdcockIM,etal.Ligand-induceddifferentiationofglucocorticoidreceptor(GR)trans-repressionandtransactivation:preferentialtargettingofNF-kappaBandlackofI-kappaBinvolvement.BrJPharmacol.1999Jun;127(4):1003-11.

    [3].RocksénD,etal.Differentialanti-inflammatoryandanti-oxidativeeffectsofDexamethasoneandN-acetylcysteineinendotoxin-inducedlunginflammation.ClinExpImmunol.2000Nov;122(2):249-56.

    [4].RousselD,etal.Dexamethasonetreatmentspecificallyincreasesthebasalprotonconductanceofratlivermitochondria.FEBSLett.2003Apr24;541(1-3):75-9.

    [5].MaherHM,etal.Simultaneousdeterminationofselectedtyrosinekinaseinhibitorswithcorticosteroidsandantiemeticsinratplasmabysolidphaseextractionandultra-performanceliquidchromatography-tandemmassspectrometry:Applicationtopharmacokineticinteractionstudies.JPharmBiomedAnal.2016May30;124:216-27.

    [6].QixiongZhang,etal.Structure-PropertyCorrelationsofReactiveOxygenSpecies-ResponsiveandHydrogenPeroxide-EliminatingMaterialswithAnti-OxidantandAnti-InflammatoryActivities.ChemMater.2017,29(19):8221-8238.

Purity:98.70%