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Medchemexpress/GW 4064/HY-50108/100mg
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Medchemexpress/GW 4064/HY-50108/100mg
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GW4064isapotentFXRagoNISTwithEC50of65nM.
Description

GW4064isapotentFXRagonistwithEC50of65nM.

IC50&Target

EC50:65nM(FXR)[1]

InVitro

TreatmentwithdifferentconcentrationsofGW4064(1,2.5,5,10μM)reducesthelipidaccumulationinthecells.Concordantly,GW4064treatmentsignificantlyrepressesoleicacid-inducedCD36proteinlevelsinadose-dependentmanner.Takentogether,thesedataindicatethatpreventionofhepaticlipidaccumulationislikelyduetoaninhibitionofCd36expressionbylong-termGW4064treatment[2].

InVivo

GW4064suppressesweightgaininC57BL/6micefedwitheitherahigh-fatdiet(HFD)orhigh-fat,high-cholesteroldiet.GW4064treatmentofmiceonHFDsignificantlyrepressesdiet-inducedhepaticsteatosisasevidencedbylowertriglycerideandfreefattyacidlevelintheliver.GW4064markedlyreduceslipidtransporterCD36expressionwithoutaffectingexpressionofgenesthataredirectlyinvolvedinlipogenesis.GW4064treatmentattenuateshepaticinflammationwhilehavingnoeffectonwhiteADIposetissue[2].GW4064(30mg/kg)treatmentresultsinsubstantial,statisticallysignificantreductionsinserumactivitiesofALT,AST,LDH,andALPintheANIT-treatedrats.SerumbileacidlevelsarealsosignificantlyreducedbyGW4064treatment.BilirubinlevelsaredecreasedintheGW4064-treatedrats,butstatisticalsignificanceisnotachieved.Notably,GW4064ismuchmoreeffectiveindecreasingtheseMarkersofliverdamagethanTUDCA,whichreducesonlyLDHlevels[3].

References
  • [1].AkwABI-AmeyawA,etal.ConformationallyconstrainedfarnesoidXreceptor(FXR)agonists:Naphthoicacid-basedanalogsofGW4064.BioorgMedChemLett,2008,18(15),4339-4343.

    [2].MaY,etal.SyntheticFXRagonistGW4064preventsdiet-inducedhepaticsteatosisandinsulinresistance.PharmRes.2013May;30(5):1447-57.

    [3].LiuY,etal.HepatoprotectionbythefarnesoidXreceptoragonistGW4064inratmodelsofintra-andextrahepaticcholestasis.JClinInvest.2003Dec;112(11):1678-87.

PreparingStockSolutions
ConcentrationVolumeMass1mg5mg10mg
1mM1.8422mL9.2108mL18.4216mL
5mM0.3684mL1.8422mL3.6843mL
10mM0.1842mL0.9211mL1.8422mL
Pleaserefertothesolubilityinformationtoselecttheappropriatesolvent.
CellAssay
[2]

GW4064isdissolvedinDMSOandstored,andthendilutedwithappropriatemediabeforeuse[2].

Mouselivercells(BNLCL.2)aremaintainedinahumidifiedincubatorunder5%CO2at37°CinDulbecco"sModifiedEagle"sMedium(DMEM)supplementedwith10%fetalbovineserum(FBS)and1%Penicillin/Streptomycin.Whencellsaredividedintosix-wellplatesandreach~90%confluence,sub-confluentcellsarewashedthreetimeswithphosphatebufferedsaline(PBS)andreplacedwithserum-freeDMEMsupplementedwith1%fattyacid-freeBSA.Oleicacid(finalconcentration500μM)andGW4064atvariousconcentrationsareaddedandincubatedfor24h.Cellsarethenfixedwith4%formaldehydeforOilRedOstainingorharvestedforproteinandwesternblotanalysis[2].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

AnimalAdministration
[2][3]

GW4064isdissolvedinDMSOanddiluted(Mice)[2].
GW4064ispreparedincornoil(Rat)[3].

Mice[2]
Fifteen-week-oldmaleC57BL/6micearefedahigh-fatdietwithorwithoutadditional0.2%CholesterolandreceivedtwiceweeklyinjectionsofGW4064(50mg/kg,intra-peritoneal)orcarriersolution(DMSO)solutionfor6weeks.AnimalsareweighedweeklyandtheirbodycompositionisdeterminedusingEchoMRI-100TMfromEchoMedicalSystems.
Rat[3]
Animals.AdultmaleCRL:CD(SD)IGSratsweighing300-350g,areused.Theratsreceiveasingleanalgesicdoseofoxymorphonefollowingsurgery.Twenty-fourhoursafterlaparotomy,groupsofrats(n=6)receiveintraperitonealinjectionsoncedailyfor4days.Bileduct-ligated(BDL)ratsaretreatedwith5mL/kgcornoilasvehicle,30mg/kgGW4064incornoil,or15mg/kgTUDCAincornoil.Sham-operatedanimalsreceived5mL/kgcornoilvehicle.Fourhoursafterthefinaldose,serumandliversarecollectedforanalysis.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

References
  • [1].Akwabi-AmeyawA,etal.ConformationallyconstrainedfarnesoidXreceptor(FXR)agonists:Naphthoicacid-basedanalogsofGW4064.BioorgMedChemLett,2008,18(15),4339-4343.

    [2].MaY,etal.SyntheticFXRagonistGW4064preventsdiet-inducedhepaticsteatosisandinsulinresistance.PharmRes.2013May;30(5):1447-57.

    [3].LiuY,etal.HepatoprotectionbythefarnesoidXreceptoragonistGW4064inratmodelsofintra-andextrahepaticcholestasis.JClinInvest.2003Dec;112(11):1678-87.

MolecularWeight

542.84

Formula

C₂₈H₂₂Cl₃NO₄

CASNo.

278779-30-9

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

RoomtemperatureincontinentalUS;mayvaryelsewhere

Solvent&Solubility

DMSO:≥150mg/mL

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

Purity:99.42%