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蚂蚁淘在线 / 品牌中心 / Smartox / Smartox/SK2（K_Ca2.2）通道选择性阻断剂/10TAM001-01000/1mg

Smartox/SK2（K_Ca2.2）通道选择性阻断剂/10TAM001-01000/1mg

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￥10171.20

货号：10TAM001-01000

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商品描述

Tamapin isapeptidetoxinisolatedfromthevenomoftheIndianredscorpionMesobuthusTamulus. Tamapin isamidatedatitsC-terminaltyrosineresidue. Tamapin bindsto smallconductanceCa²⁺-activatedK⁺ channels(SKchannels) withhighaffinityandinhibitsSKchannel-mediatedcurrentsinpyramidalneuronsofthehippocampusaswellasincelllinesexpressingdistinctSKchannelsubunits.Contraryto Apamin or Leiurotoxin-1(Scyllatoxin), Tamapin isanexcellenttoxintodiscriminateamongSKchannelsubtypesbecauseitpresentsdifferentaffinitiesfor SK1(42nM),SK2(24pM)andSK3(1.7nM) channels.ThistoxinisalsothemostpotentSK2channelblockercharacterizedsofar(IC₅₀ forSK2channels=24pM).

Description:

Productcode:N/A.Categories:KCachannels,Potassiumchannels.Tag:SK.

AAsequence: Ala-Phe-Cys³-Asn-Leu-Arg-Arg-Cys⁸-Glu-Leu-Ser-Cys¹²-Arg-Ser-Leu-Gly-Leu-Leu-Gly-Lys-Cys²¹-Ile-Gly-Glu-Glu-Cys²⁶-Lys-Cys²⁸-Val-Pro-Tyr-NH₂Disulfidebridges: Cys³-Cys²¹;Cys⁸-Cys²⁶;Cys¹²-Cys²⁸
Length(aa): 31
Formula: C₁₄₆H₂₃₇N₄₄O₄₁S₆
MolecularWeight: 3459.00Da
Appearance: Whitelyophilizedsolid
Solubility: waterandsalinebuffer
CASnumber: notavailable
Source: Synthetic
Purityrate: >97%

Reference:

SmallconductanceCa2+-activatedK+channelsastargetsofCNSdrugdevelopment

Inmostcentralneurons,smallconductanceCa(2+)-activatedK(+)channels(SKchannels)contributetoafterhyperpolarizations(AHPs),whichcontrolneuronalexcitABIlity.ThemediumAHPhaspharmacologicalpropertiessimilartorecombinantSKchannels,consistentwiththehypothesisthatSKchannelsgeneratethisafterhyperpolarizationcomponent.ItisstillunclearhowrecombinantSKchannelsarefunctionallyrelatedtotheslowAHPcomponent.ClonedSKchannelsareheteromericcomplexesofSKchannelsubunitsandcalmodulin.ThechannelsareactivatedbyCa(2+)bindingtocalmodulinthatinducesconformationalchangesresultinginchannelopening.ChanneldeactivationisthereverseprocessbroughtaboutbydissociationofCa(2+)fromcalmodulin.Inthemammalianbrain,thethreeSKchannelsubunits(SK1-3)displaypartiallyoverlappingdistributions.MostofthehigherbrainregionssuchastheneocortexandhippocampusshowexpressionofbothgenesencodingSK1andSK2channels,whereasphylogeneticallyolderbrainregionssuchasthethalamus,basalganglia,cerebellum,andbrainstemshowhighlevelsofSK3geneexpression.Atpresent,itisstillunclearwhethernativeSKchannelsaregeneratedasheteromericorhomomericchannels.Peptidetoxinssuchasapaminandscyllatoxin,aswellasorganiccompoundssuchasquaternarysaltsofbicuculline,dequalinium,UCL1684andUCL1848serveasnon-specificSKchannelblockers.TheonlyknownexceptionssofararethescorpiontoxintamapinandthepeptideinhibitorLei-Dab(7),whichbindpreferentiallytoSK2.ElectrophysiologicalandbehavioralstudiesindicatethatblockadeofSKchannelsbyapaminincreasesexcitability,lowersthethresholdfortheinductionofsynapticplasticity,andfacilitateshippocampus-dependentmemory.ThepotentialvalueofpharmacologicalSKchannelmodulationinvariouspathologicalstatessuchasincreasedepileptiformactivity,cognitiveimpairment,pain,mooddisordersandschizophreniawillbediscussed.

BlankT., etal. (2004)SmallconductanceCa2+-activatedK+channelsastargetsofCNSdrugdevelopment. CurrDrugTargetsCNSNeurolDisord. PMID: 15180477

Tamapin,avenompeptidefromtheIndianredscorpion(Mesobuthustamulus)thattargetssmallconductanceCa²⁺-activatedK⁺channelsandafterhyperpolarizationcurrentsincentralneurons

ThebiophysicalpropertiesofsmallconductanceCa(2+)-activatedK(+)(SK)channelsarewellsuitedtounderlieafterhyperpolarizations(AHPs)shapingthefiringpatternsofaconspicuousnumberofcentralandperipheralneurons.Wehaveidentifiedanewscorpiontoxin(tamapin)thatbindstoSKchannelswithhighaffinityandinhibitsSKchannel-mediatedcurrentsinpyramidalneuronsofthehippocampusaswellasincelllinesexpressingdistinctSKchannelsubunits.ThistoxindistinguishedbetweentheSKchannelsunderlyingtheapamin-sensitiveI(AHP)andtheCa(2+)-activatedK(+)channelsmediatingtheslowI(AHP)(sI(AHP))inhippocampalneurons.Comparedwithrelatedscorpiontoxins,tamapindisplayedaunique,remarkableselectivityforSK2versusSK1(approximately1750-fold)andSK3(approximately70-fold)channelsandisthemostpotentSK2channelblockercharacterizedsofar(IC(50)forSK2channels=24pm).TamapinwillfacilitatethecharacterizationofthesubunitcompositionofnativeSKchannelsandhelpdeterminetheirinvolvementinelectricalandbiochemicalsignaling.

PedarzaniP etal. (2002)Tamapin,avenompeptidefromtheIndianredscorpion(Mesobuthustamulus)thattargetssmallconductanceCa²⁺-activatedK⁺ channelsandafterhyperpolarizationcurrentsincentralneurons. J.BiolChem. PMID: 12239213

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Smartox/SK2（KCa2.2）通道选择性阻断剂/10TAM001-01000/1mg

Description:

Reference:

SmallconductanceCa2+-activatedK+channelsastargetsofCNSdrugdevelopment

Tamapin,avenompeptidefromtheIndianredscorpion(Mesobuthustamulus)thattargetssmallconductanceCa2+-activatedK+channelsandafterhyperpolarizationcurrentsincentralneurons

Smartox/SK2（K_Ca2.2）通道选择性阻断剂/10TAM001-01000/1mg

Tamapin,avenompeptidefromtheIndianredscorpion(Mesobuthustamulus)thattargetssmallconductanceCa²⁺-activatedK⁺channelsandafterhyperpolarizationcurrentsincentralneurons