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Discovery Antibodies/NPS 2390/5 mg/N-340-5 mg

价格
¥940.00
货号:N-340-5mg
浏览量:127
品牌:Discovery
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商品描述
Cat#:N-340
  • LyophilizedPowder
  • BioassayTested
  • SourceSynthetic
    MW:307.4
    Purity:>98%
    Effectiveconcentration10nM–1uM.
      • NPS 2390
    ChemicalnameN-(1-adamantyl)quinoxaline-2-carboxamide.
    MolecularformulaC19H21N3O.
    CASNo.:226878-01-9.
    PubChemCID7067728
    ActivityNPS2390,aquinoxalinederivative,isapotentandselectivenon-competitiveantagoNISTofGroupImGluRs,actingonmGluR1andmGluR5withIC50 valuesofto5.2and82nM,respectively,whilehavingnoeffectonmGluR2,mGluR8andothertargetsat30μM1-3.
      • MABIre,D. etal.(2005) J.Med.Chem48, 2134.
      • Lavreysen,H. etal.(2003) Mol.Pharmacol63, 1082.
      • VanWagenen,B.C. etal. (2000) Abstr.Soc.Neurosci. PresentationNo. 618, 3.
    ShippingandstorageShippedatroomtemperature.Productassuppliedcanbestoredintactatroomtemperatureforseveralweeks.Forlongerperiods,itshouldbestoredat-20°C.
    SolubilityUpto25mMinDMSO.Centrifugeallproductpreparationsbeforeuse(10000xg5min).
    Storageofsolutions-20°C.
      • NPS 2390
        AlomoneLabsNPS2390inhibitsmGluR1-mediatedCa2+ mobilizationinU2OScells.
        DoseresponseofnormalizedinhibitionofhumanmGluR1mediated,L-GlutamateevokedCa2+ mobilizationby NPS2390 (#N-340).IC50 wasdeterminedat56.7nM.hmGluR1-expressingcellswereloadedwithcalcium-sensitivedye,incubatedwitharangeofconcentrationsofNPS2390,andstimulatedby15µML-Glutamate(EC80).ChangesinintracellularCa2+ followingstimulationweredetectedaschangesinmaximumrelativefluorescence(RLU)usingFLIPRTETRA™.
    References-Scientificbackground
    • 1.Mabire,D. etal.(2005) J.Med.Chem48, 2134.
    • 2.Lavreysen,H. etal.(2003) Mol.Pharmacol63, 1082.
    • 3.VanWagenen,B.C. etal. (2000) Abstr.Soc.Neurosci. PresentationNo. 618, 3.
    • 4.O"Brien,J.A. etal. (2003) Mol.Pharmacol. 64, 731.
    • 5.Satow,A. etal. (2008) J.Pharmacol.Exp.Ther. 326, 577.
    • 6.Eom,H.S. etal. (2016) PLoSOne 11, e0147538.
    • 7.Lu,Y.M. etal. (1996) J.Neurosci. 17, 5196.
      • NPS2390,aquinoxalinederivative,isasynthetic,potent,selectiveandnon-competitiveantagonistofgroupImetabotropicglutamatereceptorscomprisingmGluR1andmGluR5receptorswithIC50valuesof5.2and8.2nMrespectively7.ThecompoundshowsverylowaffinitytowardsothermGluRreceptors.

        SeveralstudiessuggestthatNPS2390actsonasitethatisdifferentfromtheglutamatebindingpocket.ItislikelythatthecompoundactsatthetransmembranesegmentVIIregionofthereceptors1-3.

        Metabotropicglutamatereceptors(mGluRs)areGproteincoupledreceptors(GPCR)thatplayanimportantroleinsynapticplasticityandotherneuro-physiologicalandpathologicalprocessesincludingamajorroleincentralsensitizationandneuropathicpain.Type1mGluRsaremainlyfoundinsomatodendriticdomainsandpostsynapticallyregulateneuronalexcitabilityandsynaptictransmissionthroughseveralintracellularsecondmessengersystems4,5.ThemGlu1receptorsplayanimportantroleinmotorlearningandmotorcoordinationwhereasmGlu5receptorscontributetoinductionoflong-termpotentiationandassociativelearning6.

    TargetmGluR1,mGluR5receptors
    receivea5mgfreetrialsample!
    Lastupdate:25/09/2019

    NPS2390(#N-340) isahighlypure,synthetic,andbiologicallyactivecompound.

    Forresearchpurposesonly,notforhumanuse
    Discovery Antibodies的Cyclin dependant kinase 2 (CDK2) is a serine/threonine protein kinase which controls both G1/S and G2/M transitions. CDKs along with cyclins and CDK inhibitors regulate cell cycle progression. Specific cyclins activate different CDKs; in early G1, CDK2 pairs with cyclin E to promote entry into the S phase before switching to partner with cyclin A to drive the cell through S phase. Once activated CDKs phosphorylate downstream proteins to initiate signalling cascades. CDK2 phosphorylates and inactivates the RB1 (pRb) tumour suppressor family of proteins.CDK的活动受到严格控制。CDK2活性可以被包括P21在内的一系列抑制剂抑制。细胞周期失调和增殖控制的丧失与细胞转化和癌症密切相关。CDK2在DNA损伤反应(DDR)中的细胞周期停滞中也似乎起着积极作用,它的抑制作用会阻碍DDR,并使细胞对电离辐射敏感,从而诱导细胞死亡。该抗体与AlexaFluor®488偶联。AlexaFluor®488是一种流行的鲜绿色荧光染料,具有高pH稳定性。
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