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当前位置： 首页 > 产品中心 > Small_molecule > Medchemexpress/FPS-ZM1/HY-19370/50mg
商品详细Medchemexpress/FPS-ZM1/HY-19370/50mg
Medchemexpress/FPS-ZM1/HY-19370/50mg
Medchemexpress/FPS-ZM1/HY-19370/50mg
商品编号： HY-19370-10mM*1mLinDMSO
品牌： MedChemExp
市场价： ¥1100.00
美元价： 660.00
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
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商品介绍
FPS-ZM1isahigh-affinityRAGEspecificinhibitorwithaKiof25nM.

CustomerValidation

  • •BrainBehavImmun.2017Jan;59:322-332.
Description

FPS-ZM1isahigh-affinityRAGEspecificinhibitorwithaKiof25nM.

IC50&Target

Ki:25nM(RAGE)[1]

InVitro

FPS-ZM1inhibitsAβ/RAGEbindinginCHOcellswithapproximately2-foldgreateraffinitythanitsparentmolecule,FPS2.FPS-ZM1inhibitsbindingofotherknownRAGEligandstosRAGE,includingS100calcium-bindingproteinBandamphoterin.FPS-ZM1ismoreeffectivethanFPS2inreducingAβ40-inducedincreasesinBACE1mRNAandproteinlevelsandthegenerationofsAPPβ,anAPPcleavageproductofBACE1indicativeofBACE1activity[1].

InVivo

FPS-ZM1isnontoxictomiceandreADIlycrossedtheblood-brainbarrier.InagedAPPsw/0miceoverexpressinghumanAβ-precursorprotein,atransgenicmousemodelofADwithestablishedAβpathology,FPS-ZM1inhibitsRAGE-mediatedinfluxofcirculatingAβ40andAβ42intothebrain.Inbrain,FPS-ZM1bindsexclusivelytoRAGE,whichinhibitsβ-secretaseactivityandAβproductionandsuppressesmicrogliaactivationandtheneuro-inflammatoryresponse[1].FPS-ZM1treatmentreducesthelevelofAβ1-40andAβ1-42inAGEsRats.ItInhibitsAGEs-mediatedincreaseofAβ-metabolism-relatedproteinsanddownregulatesAGEs-mediatedincreaseofpro-inflammatorycytokinesinthehippocampus.FPS-ZM1up-Regulatesanti-oxidantdefensesystemandattenuatedAGEsinducedmemoryimpairmentinAGEsrats[2].

References

  • [1].DeaneR,etal.AmultimodalRAGE-specificinhibitorreducesamyloidβ-mediatedbraindisorderinamousemodelofAlzheimerdisease.JClinInvest.2012Apr;122(4):1377-92.

    [2].HongY,etal.EffectsofRAGE-SpecificInhibitorFPS-ZM1onAmyloid-βMetabolismandAGEs-InducedInflammationandOxidativeStressinRatHippocampus.NeuRochemRes.2016May;41(5):1192-9.

    [3].LianYJ,etal.Ds-HMGB1andfr-HMGBinducedepressivebehaviorthroughneuroinflammationincontrasttononoxid-HMGB1.BrainBehavImmun.2017Jan;59:322-332.

PreparingStockSolutions
ConcentrationVolumeMass1mg5mg10mg
1mM3.0502mL15.2509mL30.5018mL
5mM0.6100mL3.0502mL6.1004mL
10mM0.3050mL1.5251mL3.0502mL
Pleaserefertothesolubilityinformationtoselecttheappropriatesolvent.
KinaseAssay
[1]

HumansRAGEisimmobilized(10μg/mL)overnightat4°Cin96-wellmicrotiterplatesandblockedwith3%bovineserumalbumin.125I-labeledAβ40,HMGB1,orS100Bat5nMintheabsenceandpresenceofvariousconcentrationsofFPS2orFPS-ZM1(10to1,000nM)isaddedtothewellscontainingimmobilizedsRAGEandincubatedfor1houratroomtemperatureinPBS.WellsarewashedwithcoldPBStoremoveunboundradiolabeledligands,andtheradioactivityisanalyzed[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

CellAssay
[1]

TodeterminewhetherFPS2andFPS-ZM1aretoxictoCHOcells,thecellsaretreatedfor72hourswithdifferentconcentrationsofinhibitorsrangingfrom10nMto10μM.ThecellulartoxicityisdeterminedusingtheWST-8AssayKit[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

AnimalAdmiNISTration
[1][2]

Rat:Startingfrom1weekbeforeintrahippocampalinjection,FZM1andAGEs+FZM1ratsareintraperitoneallyinjectedwithFPS-ZM1(1mg/kg/datavolumeof2mL)for4weeks;ratsintheAGEsandthecontrolgroupsareintraperitoneallyinjectedwithnormalsalinewiththesamevolumefor4weeks.ThreeweeksafterAGEsintrahippocampalinjection,theescapelatencytimeofratsisassayedwithMorriswatermazetest,andthenallratsaresacrificed[2].

Mouse:FPS2orFPS-ZM1areadministeredi.v.(1mg/kg)viathefemoralveinandarterialbloodsamples(30μL)collectedat1,5,10,15,and20minutesviathecannulatedfemoralartery.Plasmaisseparatedbycentrifugationat4°Candimmediatelystoredat–80°Cuntilanalysis[1].

MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

References

  • [1].DeaneR,etal.AmultimodalRAGE-specificinhibitorreducesamyloidβ-mediatedbraindisorderinamousemodelofAlzheimerdisease.JClinInvest.2012Apr;122(4):1377-92.

    [2].HongY,etal.EffectsofRAGE-SpecificInhibitorFPS-ZM1onAmyloid-βMetabolismandAGEs-InducedInflammationandOxidativeStressinRatHippocampus.NeurochemRes.2016May;41(5):1192-9.

    [3].LianYJ,etal.Ds-HMGB1andfr-HMGBinducedepressivebehaviorthroughneuroinflammationincontrasttononoxid-HMGB1.BrainBehavImmun.2017Jan;59:322-332.

MolecularWeight

327.85

Formula

C₂₀H₂₂ClNO

CASNo.

945714-67-0

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

RoomtemperatureincontinentalUS;mayvaryelsewhere

Solvent&Solubility

10mMinDMSO

FPS-ZM1ispreparedinvehicle(normalsaline)[3].

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

References

  • [1].DeaneR,etal.AmultimodalRAGE-specificinhibitorreducesamyloidβ-mediatedbraindisorderinamousemodelofAlzheimerdisease.JClinInvest.2012Apr;122(4):1377-92.

    [2].HongY,etal.EffectsofRAGE-SpecificInhibitorFPS-ZM1onAmyloid-βMetabolismandAGEs-InducedInflammationandOxidativeStressinRatHippocampus.NeurochemRes.2016May;41(5):1192-9.

    [3].LianYJ,etal.Ds-HMGB1andfr-HMGBinducedepressivebehaviorthroughneuroinflammationincontrasttononoxid-HMGB1.BrainBehavImmun.2017Jan;59:322-332.

Purity:99.31%