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Discovery Antibodies/A-841720/5 mg/A-440-5 mg

价格
¥2740.00
货号:A-440-5mg
浏览量:127
品牌:Discovery
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商品描述
Cat#:A-435
  • LyophilizedPowder
  • BioassayTested
  • SourceSynthetic
    MW:342.46
    Purity:>98%
    Effectiveconcentration1-100nM.
      • A-794278
    Chemicalname3-cycloheptyl-9-(dimethylamino)pyrido[1,2]thieno[3,4-d]pyrimidin-4-one.
    MolecularformulaC18H22N4OS.
    CASNo.:869802-57-3.
    PubChemCID11537456
    ActivityA-794278isapotentandselectivenoncompetitivemGluR1antagoNIST,actingonmGluR1andmGluR5withIC50 valuesof4.1nMand147nM,respectively1Invivo itshowsanalgesicproperties,significantlyattenuatingspontaneouspost-operativepainbehaviorinrats(ED50 =50μmol/kg)2.
      • Zheng,G.Z. etal.(2005) J.Med.Chem. 48, 7374.
      • Zhu,C.Z. etal.(2008) Eur.J.Pharmacol. 580, 314.
    ShippingandstorageShippedatroomtemperature.Productassuppliedcanbestoredintactatroomtemperatureforseveralweeks.Forlongerperiods,itshouldbestoredat-20°C.Protectfromlightandmoisture.
    SolubilitySolubleinDMSO.Centrifugeallproductpreparationsbeforeuse(10000xg5min).
    Storageofsolutions-20°C.
      • A-794278
        AlomoneLabsA-794278 inhibitsmGluR1-mediatedCa2+ mobilizationinU2OScells.
        Dose-responseof A-794278 (#A-435)normalizedinhibitionofhumanmGluR1-mediated,L-glutamate-evokedCa2+ mobilization.Cellswereloadedwithcalcium-sensitivedye,incubatedwitharangeofA-794278concentrations,andstimulatedwith5µML-glutamate(EC80).ChangesinintracellularCa2+ followingstimulationweredetectedaschangesinmaximumrelativefluorescence(RLU)usingFLIPRTETRA™.IC50 wasdeterminedat4.16nM.
    References-Scientificbackground
    • 1.Zheng,G.Z. etal.(2005) J.Med.Chem. 48, 7374.
    • 2.Zhu,C.Z. etal.(2008) Eur.J.Pharmacol. 580, 314.
      • A-794278isapotent,non-competitiveantagonistofmGluR1.ItisatriazafluorenonederivativethatalsoantagonizesmGluR5receptors.ItdemonstratesIC50valuesof4.1nMand147nMformGluR1andmGluR5,respectively1.A-794278bindstoaputativeallostericrecognitionsitelocatedwithintheseven-transmembranedomainofthereceptor1,2.

        Glutamateisthemostabundantexcitatoryneurotransmitterinthecentralnervoussystem.Itmodulatestheactivityofmanytypesofsynapsesbyactivatinginpartmetabotropicglutamatereceptors(mGluRs).mGluRsconsistofthreegroups:I,II,andIIIwithatotalofeightsubtypes,mGluR1tomGluR8.mGluR1playsanimportantroleinthecentralsensitizationofpainandinavarietyoffunctionswithpotentialimplicationsinneurologicalandpsychiatricdisorders1,2.

    TargetmGluR1,mGluR5
    receivea5mgfreetrialsample!
    Lastupdate:25/09/2019

    A-794278(#A-435) 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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