PlerixaforoctahydrochlorideisaselectiveCXCR4antagonistwithIC₅₀of44nM.

IC50:44nM(CXCR4)^[1]

TheCXCR4inhibitorPlerixafor(AMD3100)isapotentinhibitorofCXCL12-mediatedchemotaxis(IC₅₀,5.7nM)withapotencyslightlybetterthanitsaffinityforCXCR4.TreatingthecellswithCCX771orCXCL11hasnoeffectonCXCL12-mediatedMOLT-4orU937TEM.Incontrast,10μMPlerixaforinhibitsCXCL12-mediatedTEMinbothcellslines^[1].Plerixafor(10μM)-treatedcellsshowamoderatereductionincellproliferationcomparedtoCXCL12-stimulatedcells,whichdonotreachstatisticalsignificance^[2].

Plerixafor(2mg/kg)administrationtoUUOmiceexacerbatesrenalinterstitialTcellinfiltration,resultinginincreasedproductionofthepro-inflammatorycytokinesIL-6andIFN-γanddecreasedexpressionoftheanti-inflammatorycytokineIL-10^[3].BothperivascularandinterstitialfibrosisaresignificantlyreducedbytheCXCR4antagonist,Plerixafor(AMD3100)at8weeks^[4].LD50,mouse,SC:16.3mg/kg;LD50,rat,SC:>50mg/kg;LD50,mouseandrat,IVinjection:5.2mg/kg.

• [1].ZabelBA,etal.ElucidationofCXCR7-mediatedsignalingeventsandinhibitionofCXCR4-mediatedtumorcelltransendothelialmigrationbyCXCR7ligands.JImmunol.2009Sep1;183(5):3204-11.

  [2].MercurioL,etal.TargetingCXCR4byaselectivepeptideantagonistmodulatestumormicroenvironmentandmicrogliareactivityinahumanglioblastomamodel.JExpClinCancerRes.2016Mar25;35:55.

  [3].YangJ,etal.ContinuousAMD3100TreatmentWorsensRenalFibrosisthroughRegulationofBoneMarrowDerivedPro-AngiogenicCellsHomingandT-Cell-RelatedInflammation.PLoSOne.2016Feb22;11(2):e0149926.

  [4].ChuPY,etal.CXCR4AntagonismAttenuatestheDevelopmentofDiabeticCardiacFibrosis.PLoSOne.2015Jul27;10(7):e0133616.

PlerixaforisdissolvedinDMSOandthendilutedwithappropriatemedium^[2].

U87MGcellsareseededin96-wellplatesatthedensityof6×10³cellsin200μL/wellandtreatedwithCXCL12,PlerixafororwithpeptideR,asdescribedintheprevious“Treatments”section.MTT(5μg/mL)isaddedateachtimepoint(24,48,72h)duringthefinal2hoftreatment.Afterremovingcellmedium,100μLDMSOareaddedandopticaldensitiesmeasuredat595nmwithaLT-4000MSMicroplateReader.Measurementsaremadeintriplicatesfromthreeindependentexperiments^[2].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

PlerixaforispreparedinPBS(Mice)^[3].
Plerixafor(AMD3100)ispreparedinH₂O(Rat)^[4].

Mice^[3]
MaleC57bl/6mice(6-7weeksold,weighing20g)areused.Theanimalsareacclimatedtothehousingenvironment,whichisSPFandhadatemperatureof22°Canda12h/12hlight/darkcycleforaweek.Then,theyarerandomlydividedintofollowingexperimentalgroups,with8miceineachgroup:normal(nospecificintervention),UUO+AMD3100(micereceivedUUOsurgeryand2mg/kgAMD3100),andUUO+PBS(micereceivedUUOsurgeryandthesamevolumeofPBS).AMD3100andPBSareadministeredviaintraperitonealinjectioneverydayuntilsacrifice.
Rat^[4]
TheCXCR4antagonist,AMD3100dissolvedinH₂O,isdeliveredinthetype2diabeticsandratmodelatadoseof6mg/kgperdayfor8weeks.Incomplementarystudies,theeffectofCXCR4antagonism(AMD31006mg/kg/d)onregulatoryTcellnumbersisexamined.Forthesestudies,AMD3100orvehicleisdeliveredviaminipumpforaperiodofoneweek.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

• [1].ZabelBA,etal.ElucidationofCXCR7-mediatedsignalingeventsandinhibitionofCXCR4-mediatedtumorcelltransendothelialmigrationbyCXCR7ligands.JImmunol.2009Sep1;183(5):3204-11.

  [2].MercurioL,etal.TargetingCXCR4byaselectivepeptideantagonistmodulatestumormicroenvironmentandmicrogliareactivityinahumanglioblastomamodel.JExpClinCancerRes.2016Mar25;35:55.

  [3].YangJ,etal.ContinuousAMD3100TreatmentWorsensRenalFibrosisthroughRegulationofBoneMarrowDerivedPro-AngiogenicCellsHomingandT-Cell-RelatedInflammation.PLoSOne.2016Feb22;11(2):e0149926.

  [4].ChuPY,etal.CXCR4AntagonismAttenuatestheDevelopmentofDiabeticCardiacFibrosis.PLoSOne.2015Jul27;10(7):e0133616.

794.47

C₂₈H₆₂Cl₈N₈

155148-31-5

RoomtemperatureincontinentalUS;mayvaryelsewhere

H₂O:≥42mg/mL

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

Purity:98.90%

SelectBatch:HY-50912-18689HY-50912-07842

DataSheet(126KB)SDS(121KB)

COA(97KB)HNMR(188KB)LCMS(219KB)

HandlingInstructions(1252KB)

• [1].ZabelBA,etal.ElucidationofCXCR7-mediatedsignalingeventsandinhibitionofCXCR4-mediatedtumorcelltransendothelialmigrationbyCXCR7ligands.JImmunol.2009Sep1;183(5):3204-11.

  [2].MercurioL,etal.TargetingCXCR4byaselectivepeptideantagonistmodulatestumormicroenvironmentandmicrogliareactivityinahumanglioblastomamodel.JExpClinCancerRes.2016Mar25;35:55.

  [3].YangJ,etal.ContinuousAMD3100TreatmentWorsensRenalFibrosisthroughRegulationofBoneMarrowDerivedPro-AngiogenicCellsHomingandT-Cell-RelatedInflammation.PLoSOne.2016Feb22;11(2):e0149926.

  [4].ChuPY,etal.CXCR4AntagonismAttenuatestheDevelopmentofDiabeticCardiacFibrosis.PLoSOne.2015Jul27;10(7):e0133616.

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Medchemexpress/Plerixafor octahydrochloride(Synonyms: AMD3100 octahydrochloride; JM3100 octahydrochloride; SID791 octahydroch

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Medchemexpress/GSK126(Synonyms: EZH2 inhibitor; GSK2816126A)/HY-13470/50mg

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Medchemexpress/MLN4924(Synonyms: Pevonedistat)/HY-70062/5mg

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Medchemexpress/Cyclosporin A(Synonyms: Cyclosporine; Ciclosporin)/HY-B0579/10mM*1mL in DMSO

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Medchemexpress/(-)-Blebbistatin(Synonyms: (S)-(-)-Blebbistatin)/HY-13441/5mg

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Medchemexpress/Riociguat(Synonyms: BAY 632521)/HY-14779/200mg

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Medchemexpress/H-89 dihydrochloride(Synonyms: Protein kinase inhibitor H-89 dihydrochloride)/HY-15979A/100mg

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Medchemexpress/WIN 55,212-2 Mesylate(Synonyms: (R)-(+)-WIN 55212)/HY-13291/10mM*1mL in DMSO

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