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蚂蚁淘在线 / 品牌中心 / MCE / Medchemexpress/WIN 55,212-2 Mesylate(Synonyms: (R)-(+)-WIN 55212)/HY-13291/100mg

Medchemexpress/WIN 55,212-2 Mesylate(Synonyms: (R)-(+)-WIN 55212)/HY-13291/100mg

价格
￥1380.00
货号：HY-13291-10mM*1mLinDMSO
浏览量：127
品牌：MCE
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商品描述
WIN55,212-2(Mesylate)isapotentaminoalkylindolecannABInoid(CB)receptoragoNISTwithKisof62.3and3.3nMforhumanrecombinantCB1andCB2receptors,respectively.

CustomerValidation

  • •FrontMolNeurosci.2017Aug7;10:247.
Description

WIN55,212-2(Mesylate)isapotentaminoalkylindolecannabinoid(CB)receptoragonistwithKisof62.3and3.3nMforhumanrecombinantCB1andCB2receptors,respectively.

IC50&Target

Ki:62.3nM(humanrecombinantCB1),3.3nM(humanrecombinantCB2)

InVitro

WIN55,212-2ismorepotentinCHO-CB2cellsthaninCHO-CB1cellsbyafactorof6O.WIN55,212-2hasnoeffectonarachidonicacidreleaseinCHO-CB2orcontrolCHOcells.WIN55,212-2failstostimulateanyincreaseinintracellularCa2+upto10μM[1].Inprimaryculturesofratcerebralcortexneurons,WIN55,212-2(0.01--100nM)increasesextracellularglutamatelevels,displayingabell-shapedconcentration-responsecurve.ThefacilitatoryeffectofWIN55,212-2(1nM)isfullycounteractedbySR141716A(10nM),bythereplacementofthenormalKrebsRinger-bicarbonatebufferwithalowCa2+medium(0.2mM)andbytheIP(3)receptorantagonistxestosponginC(1μM)[2].WIN55,212-2evokesCGRPreleasefromTGneuronsinvitro(EC50=26μM)inaconcentration-andcalcium-dependentmanner.WIN55,212-2-2neitherinhibitscapsaicin-evokesCGRPreleasenordoesitinhibitforskolin-,isoproteranol-orprostaglandinE2-stimulatedcAMPaccumulation.WIN55,212-2significantlyinhibits(EC50=1.7μM)50mmK+-evokedCGRPreleasebyapproximately70%.WIN55,212-2inhibitionof50mmK+-evokedCGRPreleaseisnotreversedbyantagonistsofcannabinoidtype1(CB1)receptor,butismimicksinmagnitudeandpotency(EC50=2.7μM)byitscannabinoid-inactiveenantiomerWIN55,212-2-3[3].

InVivo

IntheprefrontalcortexWIN55,212-2(0.1and1mg/kgi.p.)increasesdialysateglutamatelevelsfromoftheawakerat,whilethelower(0.01mg/kg)andthehigher(2mg/kg)dosesareineffective.FurThermore,theWIN55,212-2(0.1mg/kg)-inducedincreaseofdialysateglutamatelevelsiscounteractedbypretreatmentwiththeselectiveCB(1)receptorantagonistSR141716A(0.1mg/kg,i.p.)andbythelocalperfusionwithalow-calciumRingersolution(Ca2+0.2mM)[2].WIN55,212-2(0.5,1,3,5,10and15mg/kg,i.p.)doesnotaltertheseizurethresholdatlowdoses,whilehigherdosesofthedrugsignificantlyincreasesthethresholdinadose-dependentmanner.TheanticonvulsanteffectofWIN55,212-2,whichisobservedwithdosesashighas5mg/kg,canbeobservedwithdosesaslowas0.5mg/kgingroupspre-treatedwith20mg/kgofpioglitazone[4].

References

  • [1].FelderCC,etal.ComparisonofthepharmacologyandsignaltransductionofthehumancannabinoidCB1andCB2receptors.MolPharmacol.1995Sep;48(3):443-50.

    [2].FerraroL,etal.ThecannabinoidreceptoragonistWIN55,212-2regulatesglutamatetransmissioninratcerebralcortex:aninvivoandinvitrostudy.CerebCortex.2001Aug;11(8):728-33.

    [3].PriceTJ,etal.Cannabinoidreceptor-independentactionsoftheaminoalkylindoleWIN55,212-2ontrigeminalsensoryneurons.BrJPharmacol.2004May;142(2):257-66.

    [4].PayandemehrB,etal.InvolvementofPPARreceptorsintheanticonvulsanteffectsofacannabinoidagonist,WIN55,212-2.ProgNeuropsychopharmacolBiolPsychiatry.2015Mar3;57:140-5.

PreparingStockSolutions
ConcentrationVolumeMass1mg5mg10mg
1mM1.9135mL9.5674mL19.1347mL
5mM0.3827mL1.9135mL3.8269mL
10mM0.1913mL0.9567mL1.9135mL
Pleaserefertothesolubilityinformationtoselecttheappropriatesolvent.
AnimalAdministration
[3]

WIN55,212-2isformulatedin1%aqueoussolutionofDMSO.

Inexperiment1,differentdosesofWIN55,212-2(0.5,1,3,5,10and15mg/kg)areinjected60minpriortothedeterminationofclonicseizurethresholdinducedbyintravenousadministrationofPTZsolution.Controlanimalsreceivethesamevolumeofthevehicle(1%aqueoussolutionofDMSO).Thedosesandtimepointarechosenonthebasisofpilotstudies.Inexperiment2,inordertoconfirmtheanticonvulsanteffectsofpioglitazone,differentdoses(10,20,40and80mg/kg)areadministered4hpriortoPTZindistinctgroupsofmice.Thecorrespondingcontrolgroupreceivetheappropriatevehicle(CMC1%)atthesametimepoint.Inexperiment3,TheadditiveantiepilepticeffectsofWIN55,212-2andpioglitazoneareexamined;micereceiveacuteadministrationofpioglitazone(10or20mg/kg)3hbeforeWIN55,212-2(0.5or1mg/kg)and4hbeforePTZ.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

References

  • [1].FelderCC,etal.ComparisonofthepharmacologyandsignaltransductionofthehumancannabinoidCB1andCB2receptors.MolPharmacol.1995Sep;48(3):443-50.

    [2].FerraroL,etal.ThecannabinoidreceptoragonistWIN55,212-2regulatesglutamatetransmissioninratcerebralcortex:aninvivoandinvitrostudy.CerebCortex.2001Aug;11(8):728-33.

    [3].PriceTJ,etal.Cannabinoidreceptor-independentactionsoftheaminoalkylindoleWIN55,212-2ontrigeminalsensoryneurons.BrJPharmacol.2004May;142(2):257-66.

    [4].PayandemehrB,etal.InvolvementofPPARreceptorsintheanticonvulsanteffectsofacannabinoidagonist,WIN55,212-2.ProgNeuropsychopharmacolBiolPsychiatry.2015Mar3;57:140-5.

MolecularWeight

522.61

Formula

C₂₈H₃₀N₂O₆S

CASNo.

131543-23-2

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

RoomtemperatureincontinentalUS;mayvaryelsewhere

Solvent&Solubility

DMSO:≥34mg/mL

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

Purity:98.98%