Medchemexpress/Plerixafor(Synonyms: AMD3100; JM3100)/HY-10046/100mg_蚂蚁淘，【正品极速】生物医学科研用品轻松购|ebiomall 蚂蚁淘商城

商品信息

联系客服

Medchemexpress/Plerixafor(Synonyms: AMD3100; JM3100)/HY-10046/100mg

郑重提醒：

无质量问题不接受退换货，下单前请仔细核对信息。

下单后请及时联系客服核对商品价格，订单生效后再付款。

Medchemexpress/Plerixafor(Synonyms: AMD3100; JM3100)/HY-10046/100mg

品牌 /

MedChemExpress

货号 /

HY-10046-10mM*1mLinEthanol

官网地址

美元价：

登录查看

(友情提示：该价格仅为参考，欢迎联系客服询价！)

数量：

免费咨询热线

4000-520-616

商品介绍售后保障相关文章商品咨询

联系客服

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°C	3years
	4°C	2years
Insolvent	-80°C	6months
	-20°C	1month

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%

SelectBatch: