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Smartox/Fluorescent (red) Kv1.3 blocker/SAT001-00100/1mg
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TMR-ShK peptidetoxinisasyntheticderivativeofthewell-known ShKtoxin(Stichodactylahelianthusneurotoxin) isolatedfromthevenomoftheCarribeanseaanemone Stoichactishelianthus.Wild-type ShK blockspotentlyKv1.3(KCNA3),Kv1.1(KCNA1),Kv1.4(KCNA4)andKv1.6(KCNA6)withaKdvalueof11pM,16pM,312pMand165pM,respectively.ThefluorescentTMR-labeledShKblocksKv1.3andKv1.1withKdvaluesof52pMand397pM,respectively. TMR-ShK canbeusedtoidentifylymphocytesexpressingKv1.3channelssuchaseffectivememoryTcells(TEM)inthecaseofautoimmunediseases(type1diabetes,mellitusorrheumatoidarthritis)whichoverexpressKv1.3channels.Description:Productcode:SAT001-00100.Categories:Kv1.3channel,Potassiumchannels.Tags:Kv1.3,TRAM-34.AAsequence: TMR-AEEAc-Arg-Ser-Cys3-Ile-Asp-Thr-Ile-Pro-Lys-Ser-Arg-Cys12-Thr-Ala-Phe-Gln-Cys17-Lys-His-Ser-Met-Lys-Tyr-Arg-Leu-Ser-Phe-Cys28-Arg-Lys-Thr-Cys32-Gly-Thr-Cys35-OHDisulfidebonds: Cys3-Cys35,Cys12-Cys28 andCys17-Cys32Length(aa): 35Formula: C200H310N57O55S7MolecularWeight: 4611.7DaAppearance:redlyophilizedsolidSolubility: waterorsalinebufferCASnumber: NASource: SyntheticPurityrate: >97%TMRfluorescentdye (5(6)-TAMRA): λex543nM, λem572nMReference:ANovelFluorescentToxintoDetectandInvestigateKv1.3ChannelUp-regulationinChronicallyActivatedTLymphocytesTlymphocyteswithunusuallyhighexpressionofthevoltage-gatedKv1.3channel(Kv1.3(high)cells)havebeenimplicatedinthepathogenesisofexperimentalautoimmuneencephalomyelitis,ananimalmodelformultiplesclerosis.WehavedevelopedafluoresceinatedanalogofShK(ShK-F6CA),themostpotentknowninhibitorofKv1.3,fordetectionofKv1.3(high)cellsbyflowcytometry.ShK-F6CAblockedKv1.3atpicomolarconcentrationswithaHillcoefficientof1andexhibited>80-foldspecificityforKv1.3overKv1.1andotherK(V)channels.Inflowcytometryexperiments,ShK-F6CAspecificallystainedKv1.3-expressingcellswithadetectionlimitofapproximately600channelspercell.RatandhumanTcellsthathadbeenrepeatedlystimulated7-10timeswithantigenwerereADIlydistinguishedonthebasisoftheirhighlevelsofKv1.3channels(>600channels/cell)andShK-F6CAstainingfromrestingTcellsorcellsthathadundergone1-3roundsofactivation.FunctionalKv1.3expressionlevelsincreasedsubstantiallyinamyelin-specificratTcelllinefollowingmyelinantigenstimulation,peakingat15-20handthendecliningtobaselineoverthenext7days,inparallelwiththeacquisitionandlossofencephalitogenicity.Bothcalcium-andproteinkinaseC-dependentpathwayswererequiredfortheantigen-inducedKv1.3up-regulation.ShK-F6CAmightbeusefulforrapidandquantitativedetectionofKv1.3(high)expressingcellsinnormalanddiseasedtissues,andtovisualizethedistributionoffunctionalchannelsinintactcells.BeetonC.,etal.(2003)ANovelFluorescentToxintoDetectandInvestigateKv1.3ChannelUp-regulationinChronicallyActivatedTLymphocytes.JBC.PMID:12511563

Smartox Biotechnology 是全球唯一一家专门生产动物毒液多肽毒素,用于细胞离子通道功能研究的生物医药公司。多肽毒素在生物制药领域具有重要的使用价值。Smartox Biotechnology 于 2009 年由来自 Grenoble 神经科学研究所 (Grenoble Institute of Neuroscience) 的 Michel de waard 博士创立, Smartox Biotechnology 专门研究动物毒液,制作合成多种毒液中的多肽成分(常称为毒素)。 De Waard 博士研究离子通道与毒素多肽的关系,尤其是鉴定、开发毒素多肽作为治疗性分子或细胞穿透肽 (cell penetrating peptides, CPP) 。其研究团队在毒液分离,药理性活性肽鉴定、富半胱氨酸肽定性、制作和优化等方面具有独特、丰富的经验。 2010 年, Smartox Biotechnolgy 被法国研究部 (Ministry of Research) 授予“新兴企业 OSEO 奖 (OSEO prize for emerging businesses) ”。 

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