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蚂蚁淘在线 / 品牌中心 / Smartox / Smartox//07APE002-01000/1mg

Smartox//07APE002-01000/1mg

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￥7488.00

货号：07APE002-01000

浏览量：127

品牌：Smartox

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商品描述

ASIC3selectiveinhibitor

APETx2 isatoxinthatwasoriginallyisolatedfromAnthopleuraelegantissima(Seaanemone).APETx2 selectivelyblockstheH(+)-gatedsodiumchannelASIC3(ACCN3).TheblockageisrapidandreversIBLe.ThistoxindoesnotblockisoformASIC1a(unlike Psalmotoxin1)andisoformASIC1bofASIC1(ACCN2),norASIC2(ACCN1).ItalsoinhibitstheheteromericASIC2b-ASIC3channel,and haslessaffinityforASIC1b-ASIC3,ASIC1a-ASIC3,andnoeffectontheASIC2a-ASIC3channels.IC₅₀ is63nMonASIC3channel.IC₅₀ is117nMonASIC2b-ASIC3heteromericchannel.IC₅₀ is0.9µMonASIC1b-ASIC3heteromericchannel.IC₅₀ is2µMonASIC1a-ASIC3heteromericchannel.Interestingly,recentstudiesdemonstratedthat APETx2also inhibitsNa_v1.8currents withanIC₅₀ ofaround2µM.

APETx2 #07APE002 ASIC3 channel blocker

Fig1: Dose-responsecurveoftheeffectofsyntheticAPETx2#07APE002onratASIC3currentrecordedinXenopusoocytes.Inthissystem,anIC₅₀of80.5nMwasdeterminedforAPETx2(N=5).

Description:

Productcode:07APE002.Category:ASICchannels.Tags:ASIC,pain.

AAsequence: H-Gly-Thr-Ala-Cys⁴-Ser-Cys⁶-Gly-Asn-Ser-Lys-Gly-Ile-Tyr-Trp-Phe-Tyr-Arg-Pro-Ser-Cys²⁰-Pro-Thr-Asp-Arg-Gly-Tyr-Thr-Gly-Ser-Cys³⁰-Arg-Tyr-Phe-Leu-Gly-Thr-Cys³⁷-Cys³⁸-Thr-Pro-Ala-Asp-OH
(DisulfidebondsbetweenCys⁴-Cys³⁷,Cys⁶-Cys³⁰ andCys²⁰-Cys³⁸)
Length(aa): 42
Formula: C₁₉₆H₂₈₀N₅₄O₆₁S₆MolecularWeight: 4561.13Da
Appearance:Whitelyophilizedsolid
Solubility: waterandsalinebuffer
CASnumber: notavailable
Source: Synthetic
Purityrate: >98%

Reference:

Citations

PeigneurS, etal.(2012)Anaturalpointmutationchangesbothtargetselectivityandmechanismofactionofseaanemonetoxins. FASEBJ. PubMedlink
BlanchardMG,RashLD,KellenbergerS.(2011)Inhibitionofvoltage-gatedNa(+)currentsinsensoryneuronsbytheseaanemonetoxinAPETx2. BrJPharmacol. PubMedlink
TsuchimochiH,YamauchiK,McCordJL,KaufmanMP.(2011)BlockadeofAcidSensingIonChannelsAttenuatestheAugmentedExercisePressorReflexinRatswithChronicFemoralArteryOcclusion. JPhysiol. PubMedlink

HumanASIC3channeldynamicallyadaptsitsactivitytosensetheextracellularpHinbothacidicandalkalinedirections.

Inrodentsensoryneurons,acid-sensingionchannel3(ASIC3)hasrecentlyemergedasaparticularlyimportantsensorofnonadaptivepainassociatedwithtissueacidosis.However,littleisknownaboutthehumanASIC3channel,whichincludesthreesplicevariantsdifferingintheirC-terminaldomain(hASIC3a,hASIC3b,andhASIC3c).hASIC3atranscriptsrepresentthemainmRNAsexpressedinbothperipheralandcentralneuronaltissues(dorsalrootganglia[DRG],spinalcord,andbrain),whereasmallproportionofhASIC3ctranscriptsisalsodetected.WeshowthathASIC3channels(hASIC3a,hASIC3b,orhASIC3c)areabletodirectlysenseextracellularpHchangesnotonlyduringacidification(uptopH5.0),butalsoduringalkalization(uptopH8.0),anoriginalandinduciblepropertyyetunknown.WhentheexternalpHdecreases,hASIC3displayatransientacidmodewithbriefactivationthatisrelevanttotheclassicalASICcurrents,aspreviouslydescribed.Ontheotherhand,anexternalpHincreaseactivatesasustainedalkalinemodeleADIngtoaconstitutiveactivityatrestingpH.BothmodesareinhibitedbytheAPETx2toxin,anASIC3-typechannelinhibitor.ThealkalinesensitivityofhASIC3isanintrinsicpropertyofthechannel,whichissupportedbytheextracellularloopandinvolvestwoarginines(R68andR83)onlypresentinthehumanclone.hASIC3isthusabletosensetheextracellularpHinbothdirectionsandthereforetodynamicallyadaptitsactivitybetweenpH5.0and8.0,apropertylikelytoparticipateinthefinetuningofneuronalmembranepotentialandtoneuronsensitizationinvariouspHenvironments.

DelaunayA.,etal.(2012)HumanASIC3channeldynamicallyadaptsitsactivitytosensetheextracellularpHinbothacidicandalkalinedirections.PNAS.PMID:22829666

SolutionstructureofAPETx2,aspecificpeptideinhibitorofASIC3proton-gatedchannels.

Acid-sensingionchannels(ASIC)areproton-gatedsodiumchannelsthathavebeenimplicatedinpaintransductionassociatedwithacidosisininflamedorischemictissues.APETx2,apeptidetoxineffectorofASIC3,hasbeenpurifiedfromanextractoftheseaanemoneAnthopleuraelegantissima.APETx2isa42-amino-acidpeptidecross-linkedbythreedisulfidebridges.Itsthree-dimensionalstructure,asdeterminedbyconventionaltwo-dimensional1H-NMR,consistsofacompactdisulfide-bondedcorecomposedofafour-strandedbeta-sheet.Itbelongstothedisulfide-richall-betastructuralfamilyencompassingpeptidetoxinscommonlyfoundinanimalvenoms.ThestructuralcharacteristicsofAPETx2arecomparedwiththatofPcTx1,anothereffectorofASICchannelsbutspecifictotheASIC1asubtypeandtoAPETx1,atoxinstructurallyrelatedtoAPETx2,whichtargetstheHERGpotassiumchannel.Structuralcomparisons,coupledwiththeanalysisoftheelectrostaticcharacteristicsofthesevariousionchanneleffectors,ledustosuggestaputativechannelinteractionsurfaceforAPETx2,encompassingitsNterminustogetherwiththetypeI-betaturnconnectingbeta-strandsIIIandIV.Thisbasicsurface(R31andR17)isalsorichinaromaticresidues(Y16,F15,Y32,andF33).AnadditionalregionmadeofthetypeII’-betaturnconnectingbeta-strandsIandIIcouldalsoplayaroleinthespecificityobservedforthesedifferentioneffectors.

ChagotB.,etal.(2005)SolutionstructureofAPETx2,aspecificpeptideinhibitorofASIC3proton-gatedchannels,ProteinSci.PMID:15987885

Anewseaanemonepeptide,APETx2,inhibitsASIC3,amajoracid-sensitivechannelinsensoryneurons.

Fromasystematicscreeningofanimalvenoms,weisolatedanewtoxin(APETx2)fromtheseaanemoneAnthopleuraelegantissima,whichinhibitsASIC3homomericchannelsandASIC3-containingheteromericchannelsbothinheterologousexpressionsystemsandinprimaryculturesofratsensoryneurons.APETx2isa42amino-acidpeptidecrosslinkedbythreedisulfidebridges,withastructuralorganizationsimilartothatofotherseaanemonetoxinsthatinhibitvoltage-sensitiveNa+andK+channels.APETx2reversiblyinhibitsratASIC3(IC50=63nM),withoutanyeffectonASIC1a,ASIC1b,andASIC2a.APETx2directlyinhibitstheASIC3channelbyactingatitsexternalside,anditdoesnotmodifythechannelunitaryconductance.APETx2alsoinhibitsheteromericASIC2b+3current(IC50=117nM),whileithaslessaffinityforASIC1b+3(IC50=0.9microM),ASIC1a+3(IC50=2microM),andnoeffectontheASIC2a+3current.TheASIC3-likecurrentinprimaryculturedsensoryneuronsispartlyandreversiblyinhibitedbyAPETx2withanIC50of216nM,probablyduetothemixedinhibitionsofvariousco-expressedASIC3-containingchannels.

DiochotS.,etal.(2004)Anewseaanemonepeptide,APETx2,inhibitsASIC3,amajoracid-sensitivechannelinsensoryneurons.EMBOJ.PMID:15044953

Smartox生物素ProTx-I电压门控钠通道和T型Cav的阻断剂毒素I（ProTx-1；β-theraphotoxin-Tp1a）是一种毒素，最初是从Prixopelma pruriens（秘鲁绿色天鹅绒狼蛛）的毒液中分离出来的。此毒素可逆地抑制抗河豚毒素（TTX）的通道 Na v 1.8（IC 50 = 27 nM）和 Na v 1.2，Na v 1.5和Na v 1.7 ，IC 50 值为50至100 nM。此外， ProTx-I 改变了T型Ca v 3.1通道的电压依赖性活动（IC 50 = 50 nM），而不会影响灭活的电压依赖性。生物素ProTx-I是ProTx-I的生物素标签版本。

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