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当前位置： 首页 > 产品中心 > Small_molecule > Medchemexpress/Plerixafor（同义词：AMD3100；JM3100）/HY-10046/100mg
商品详细Medchemexpress/Plerixafor（同义词：AMD3100；JM3100）/HY-10046/100mg
Medchemexpress/Plerixafor（同义词：AMD3100；JM3100）/HY-10046/100mg
Medchemexpress/Plerixafor（同义词：AMD3100；JM3100）/HY-10046/100mg
商品编号： HY-10046-10mM*1mLinEthanol
品牌： MedChemExp
市场价： ¥1680.00
美元价： 1008.00
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
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商品介绍
PlerixaforisaselectiveCXCR4antagoNISTwithIC50of44nM.
Description

PlerixaforisaselectiveCXCR4antagonistwithIC50of44nM.

IC50&Target

IC50:44nM(CXCR4)[1]

InVitro

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

InVivo

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.

ClinicalTrial
ViewMoreCollapse
References

  • [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.

    [5].HeG,etal.SDF-1inMammaryFibroblastsofBovinewithMastitisInducesEMTandInflammatoryResponseofEpithelialCells.IntJBiolSci.2017May5;13(5):604-614.

CellAssay
[2]

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.

AnimalAdministration
[3][4]

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.

References

  • [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.

    [5].HeG,etal.SDF-1inMammaryFibroblastsofBovinewithMastitisInducesEMTandInflammatoryResponseofEpithelialCells.IntJBiolSci.2017May5;13(5):604-614.

MolecularWeight

502.78

Formula

C₂₈H₅₄N₈

CASNo.

110078-46-1

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

RoomtemperatureincontinentalUS;mayvaryelsewhere

Solvent&Solubility

Ethanol

Plerixafor(AMD3100)ispreparedinvehicle(normalsaline)[5].

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

References

  • [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.

    [5].HeG,etal.SDF-1inMammaryFibroblastsofBovinewithMastitisInducesEMTandInflammatoryResponseofEpithelialCells.IntJBiolSci.2017May5;13(5):604-614.

Purity:>98.0%