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当前位置: 首页 > 产品中心 > Small_molecule > Medchemexpress/Apreplitant(同义词:MK-0869;MK-869;L-754030)/HY-10052/10mM*1mL二甲基亚砜
商品详细Medchemexpress/Apreplitant(同义词:MK-0869;MK-869;L-754030)/HY-10052/10mM*1mL二甲基亚砜
Medchemexpress/Apreplitant(同义词:MK-0869;MK-869;L-754030)/HY-10052/10mM*1mL二甲基亚砜
Medchemexpress/Apreplitant(同义词:MK-0869;MK-869;L-754030)/HY-10052/10mM*1mL二甲基亚砜
商品编号: HY-10052-10mM*1mLinDMSO
品牌: MedChemExp
市场价: ¥1420.00
美元价: 852.00
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
电子邮箱: info@ebiomall.com
商品介绍
AprepitantisaspecificNK-1RantagoNIST,usedasanantiemeticagent.
Description

AprepitantisaspecificNK-1Rantagonist,usedasanantiemeticagent.

InVitro

AprepitantdecreasesthemetabolicactivitywithanestimatedIC50valueof20µM.Aprepitantinducescell-growthinhibitionandG1cell-cyclearrest.AprepitantsignificantlyinducesapoptosisinNalm-6cells,andtheapoptosisismediatedthroughcaspase-3activation.Aprepitant(20µM)inducesp53accumulationandexpressionofpro-apoptoticp53targetgenes[2].Aprepitant(1,5,10µM)inhibitsHIVinfectioninMDMfrombothdepressedandnotdepressedHIVnegativeindividualsexvivoinadose-dependentmanner.IC90valueofaprepitantisequivalentto10μM,andtheIC50valueisabout5μM[4].

InVivo

AprepitantpreventstheincreaseofNK-1RexpressioninducedbyinvivoNHPinfectionwithB.burgdorferi.AprepitanttreatmentpreventsB.burgdorferi-inducedincreasesinCCL2proteinlevelsintheCSFofNHPs.AprepitanttreatmentpreventsB.burgdorferi-inducedincreasesinCCL2andCXCL13mRNAexpressioninthedorsalrootgangliaofNHPs,preventsB.burgdorferi-inducedincreasesinCCL2,CXCL13,IL-17A,andIL-6mRNAexpressioninthespinalcordofNHPs.AprepitanttreatmentattenuatesB.burgdorferiinfection-inducedreductionsinastrocyteactivity/numbers[1].Aprepitant(10mg/kg,i.p.)significantlyattenuatestheCPPexpressionandlocomotoractivationproducedbyAMPHandcocaineinmice.Incontrast,aprepitantsignificantlyenhancestheexpressionofCPPproducedbymorphinewhilesignificantlysuppressingthelocomotoractivityofthemiceconditionedwithmorphine.AprepitantdoesnotinducesignificantCPPorconditionedplaceaversionorlocomotoractivationorsuppression[3].Aprepitant(125mg/day,p.o.)resultsin1logreductioninplasmalevelsofviralRNAascomparedtonon-treatedcontrols[4].

ClinicalTrial
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References
  • [1].MartinezAN,etal.AprepitantlimitsinvivoneuroinflammatoryresponsesinarhesusmodelofLymeneuroborreliosis.JNeuroinflammation.2017Feb15;14(1):37.

    [2].BayatiS,etal.InhibitionoftachykininNK1receptorusingaprepitantinducesapoptoticcelldeathandG1arrestthroughAkt/p53axisinpre-Bacutelymphoblasticleukemiacells.EurJPharmacol.2016Nov15;791:274-283.

    [3].MannangattiP,etal.Differentialeffectsofaprepitant,aclinicallyusedneurokinin-1receptorantagonistontheexpressionofconditionedpsychostimulantversusopioidreward.Psychopharmacology(Berl).2017Feb;234(4):695-705.

    [4].BarrettJS,etal.PharmacologicrationalefortheNK1Rantagonist,aprepitantasadjunctivetherapyinHIV.JTranslMed.2016May26;14(1):148.

PreparingStockSolutions
ConcentrationVolumeMass1mg5mg10mg
1mM1.8712mL9.3558mL18.7115mL
5mM0.3742mL1.8712mL3.7423mL
10mM0.1871mL0.9356mL1.8712mL
Pleaserefertothesolubilityinformationtoselecttheappropriatesolvent.
CellAssay
[2]

AprepitantisdissolvedinDMSO.

TheinhibitoryeffectofaprepitantonmetabolicactivityofNalm-6cellsisassessedbyuptakeofthiazolylbluetetrazoliumbromide(MTT)byviablecells.Cellsareplatedonto96-wellplatesatadensityof5000cells/well.Aftertreatmentwithaprepitantat5,10,15,20and30µMfor24,36and48h,thecellsarefurtherincubatedwith100μLofMTT(0.5mg/mL)at37°Cfor3h.Untreatedcellsaredefinedasthecontrolgroup.Followingsolubilizationofprecipitatedformazanwith100μLofDMSO,theopticaldensitometryismeasuredwithanELISAreaderatawavelengthof578nm.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

AnimalAdministration
[1]

Fifteenrhesusmacaquesareanesthetizedandinoculatedintrathecallywith1×108livespiRochetesintothecisternamagna,whereasfiverhesusmacaquesareleftuninfectedandreceive1mLofRPMI1640mediumafterremovinganequivalentvolumeofCSF.TheestablishmentofinvivoB.burgdorferiinfectionisconfirmedbypositiveculturefromatleastnecropsytissuesample.Thefirstsetofanimalsarestudiedfor2weeksandincludedtwocontrolanimals(oneofwhichistreatedwithaprepitant),twoinfectedanduntreatedanimals,andtwoinfectedanimalsthataretreatedwithaprepitant.Thesecondsetofanimalsarestudiedfor4weeksandincludedthreecontrolanimals(oneofwhichistreatedwithaprepitant),fiveinfectedanduntreatedanimals,andfourinfectedanimalstreatedwithaprepitant.Animalsreceiveanaveragedoseofaprepitantof28 ± 6mg/kgperdayp.o.daily,anddrugtreatmentsarestarted2daysbeforeinoculation.ThesedosesareconsistentwithstandardveterinaryregimensforthechosendrugsinNHP,andthe4-weekdurationofthestudyprecludesthedevelopmentofneuralpathologythatoccursat8weeksfollowingB.burgdorferiinfection.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

References
  • [1].MartinezAN,etal.AprepitantlimitsinvivoneuroinflammatoryresponsesinarhesusmodelofLymeneuroborreliosis.JNeuroinflammation.2017Feb15;14(1):37.

    [2].BayatiS,etal.InhibitionoftachykininNK1receptorusingaprepitantinducesapoptoticcelldeathandG1arrestthroughAkt/p53axisinpre-Bacutelymphoblasticleukemiacells.EurJPharmacol.2016Nov15;791:274-283.

    [3].MannangattiP,etal.Differentialeffectsofaprepitant,aclinicallyusedneurokinin-1receptorantagonistontheexpressionofconditionedpsychostimulantversusopioidreward.Psychopharmacology(Berl).2017Feb;234(4):695-705.

    [4].BarrettJS,etal.PharmacologicrationalefortheNK1Rantagonist,aprepitantasadjunctivetherapyinHIV.JTranslMed.2016May26;14(1):148.

MolecularWeight

534.43

Formula

C₂₃H₂₁F₇N₄O₃

CASNo.

170729-80-3

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

RoomtemperatureincontinentalUS;mayvaryelsewhere

Solvent&Solubility

10mMinDMSO

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

Purity:99.32%