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当前位置： 首页 > 产品中心 > acid_base_buffer_solution > Smartox/Waglerin-1块肌肉型nAChRs/12WAG001-01000/1mg
商品详细Smartox/Waglerin-1块肌肉型nAChRs/12WAG001-01000/1mg
Smartox/Waglerin-1块肌肉型nAChRs/12WAG001-01000/1mg
Smartox/Waglerin-1块肌肉型nAChRs/12WAG001-01000/1mg
商品编号： 12WAG001-01000
品牌： smartox-biotech
市场价： ¥1497.60
美元价： 1152.00
产地： 美国(厂家直采)
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产品分类： 酸碱缓冲液
公司分类： acid_base_buffer_solution
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商品介绍

Waglerin-1(Wtx-1) isapeptideoriginallyisolatedfromthevenomoftheWagler’spitviper(Trimeresuruswagleri).This22amino-acidpeptideisacompetitiveantagoNISTofmusclenicotinicacetylcholinereceptors. Waglerin-1competeswithα-bungarotoxin.

Waglerin-1 isaninterestingtooltodiscriminatebetweenfetalandadultmusclenAChRsasitbindstotheα-εsubunitinterfacewitha~2000foldhigheraffinitythantotheα-γorα-δsubunits.Waglerin-1isknowntobind100foldmorepotentlytonAChRfromadultmicethanthatfromratorhumans.ItblocksmusclenAChRfromadultmicewithanIC50valueof50nM.

Somestudieshavedemonstratedthat Waglerin-1 hasaneffectonionotropicGABAreceptors.ItmaypotentiateordepressI(GABA)dependingontheneurons.

Somederivativesof Waglerin-1 arecurrentlyusedincosmeticstoreducewrinkles.


Description:

Productcode:12WAG001.Category:NicotinicAcetylcholineReceptor.Tags:bungarotoxin,nachr,nicotinic.

AAsequence: Gly-Gly-Lys-Pro-Asp-Leu-Arg-Pro-Cys9-His-Pro-Pro-Cys13-His-Tyr-Ile-Pro-Arg-Pro-Lys-Pro-Arg-OH
Disulfidebonds: Cys9-Cys13
Length(aa): 22
Formula: C112H175N37O26S2
MolecularWeight: 2520Da
Appearance: Whitelyophilizedsolid
Solubility: waterorsalinebuffer
CASnumber: NA
Source: Synthetic

Reference:

Peptide-toxintoolsforprobingtheexpressionandfunctionoffetalandadultsubtypesofthenicotinicacetylcholinereceptor

Althoughtheneuromuscularnicotinicacetylcholinereceptor(nAChR)isoneofthemostintensivelystudiedionchannelsinthenervoussystem,thedifferentialrolesoffetalandadultsubtypesofthenAChRundernormalandpathologicalconditionsarestillincompletelydefined.Untilrecently,nopharmacologicaltoolsdistinguishedbetweenfetalandadultsubtypes.Waglerintoxins(fromsnakevenom)&alphaA(S)-conotoxins(fromcone-snailvenom)haveprovidedsuchtools.Becausethesepeptideswerecharacterizedbydifferentresearchgroupsusingdifferentmethods,wehave:1)moreextensivelytestedtheirsubtypeselectivity,and2)beguntoexplorehowthesepeptidesmaybeusedinconcerttoelucidateexpressionpatternsandfunctionsoffetalandadultnAChRs.Inheterologousexpressionsystemsandnativetissues,Waglerin-1&analphaA(S)-conotoxinanalog,alphaA-OIVA[K15N],arehigh-affinity,highlyselectiveinhibitorsoftheadultandfetalmusclenAChRs,respectively.WehaveusedthepeptidesandtheirfluorescentderivativestoexploretheexpressionandfunctionofthefetalandadultnAChRsubtypes.WhilefluorescentderivativesofthesepeptidesindicatedagradualtransitionfromfetaltoadultmusclenAChRsinmiceduringthefirst2weekspostnatal,weunexpectedlyobservedasteepertransitioninfunctionalexpressioninthemousediaphragmmuscleusingelectrophysiology.Asatoolkitofpharmacologicalagentswithcomplementaryspecificity,alphaA-OIVA[K15N]&Waglerin-1shouldhavefurtherutilityindeterminingtherolesoffetal&adultnAChRsubtypesindevelopment,inmaturetissues,andunderpathologicalconditions.

TeichertRW. etal. Peptide-toxintoolsforprobingtheexpressionandfunctionoffetalandadultsubtypesofthenicotinicacetylcholinereceptor. AnnNYAcadSci. PMID: 18567854

ConformationalanalysisofatoxicpeptidefromTrimeresuruswagleriwhichblocksthenicotinicacetylcholinereceptor
The22-residuetoxicpeptide(WTX1)fromthevenomoftheSoutheastAsiansnakeTrimeresuruswaglerihasmultiplesitesofaction,butitslethaleffecthasbeenattributedtoblockingthepostsynapticacetylcholinereceptorattheneuromuscularjunction.The3-dimensionalstructureofWTX1wasstudiedusing2-dimensionalnuclearmagneticresonancespectroscopy,circulardichroism,andcomputersimulations.Inaqueoussolution,WTX1wasshowntohaveextendedandflexIBLe“tails”definedbyashort,rigiddisulfide-bondedloop.Theflexibleregionscanundergostructuralrearrangementwhenmovedfromanaqueoustoalesspolarenvironmentandmaycontributetoitseffectivenessatdifferentreceptorsites.BysubstitutingGlyorPheforHisatposition10,significanteffectsonthedisulfidebondformationand,thereby,theactivityofthepeptidewereobserved.Theseresultssuggestthatevensubtledifferencesinsingleresiduescanhaveprofoundeffectsonthedynamicsoffolding,disulfidebondformation,&activityofthistoxicpeptide.

SellinLC. etal. ConformationalanalysisofatoxicpeptidefromTrimeresuruswagleriwhichblocksthenicotinicacetylcholinereceptor. BiophysJ. 1996. PMID: 8770182

IdentificationofresiduesatthealphaandepsilonsubunitinterfacesmediatingspeciesselectivityofWaglerin-1fornicotinicacetylcholinereceptors
Waglerin-1(Wtx-1)isa22-aminoacidpeptidethatisacompetitiveantagonistofthemusclenicotinicreceptor(nAChR).WefindthatWtx-1binds2100-foldmoretightlytothealpha-epsilonthantothealpha-deltabindingsiteinterfaceofthemousenAChR.Moreover,Wtx-1binds100-foldmoretightlytothealpha-epsiloninterfacefrommousenAChRthanthatfromratorhumansources.Site-directedmutagenesisofresiduesdifferingintheextracellulardomainsofratandmouseepsilonsubunitsindicatesthatresidues59and115mediatethespeciesdifferenceinWtx-1affinity.Mutationofresidues59(Aspinmouse,Gluinratepsilon)and115(Tyrinmouse,Serinratepsilon)convertsWtx-1affinityforthealpha-epsiloninterfaceofonespeciestothatoftheotherspecies.Studiesofdifferentmutationsatposition59indicatebothstericandelectrostaticcontributionstoWtx-1affinity,whereasatposition115,botharomaticandpolargroupscontributetoaffinity.ThehumannAChRalsohasloweraffinityforWtx-1thanmousenAChR,butunlikeratnAChR,residuesinbothalphaandepsilonsubunitsmediatetheaffinitydifference.InhumannAChR,polarresidues(Ser-187andThr-189)conferlowaffinity,whereasinmousenAChRaromaticresidues(Trp-187andPhe-189)conferhighaffinity.Theoverallresultsshowthatnon-conservedresiduesatthenAChRbindingsite,althoughnotcrucialforactivationbyACh,governthepotencyofneuromusculartoxins.

MollesBE. etal. IdentificationofresiduesatthealphaandepsilonsubunitinterfacesmediatingspeciesselectivityofWaglerin-1fornicotinicacetylcholinereceptors. JBiolChem.2002. PMID: 11724791

Waglerin-1selectivelyblockstheepsilonformofthemusclenicotinicacetylcholinereceptor
NeonatalmiceresistthelethaleffectofWaglerin-1.BecauseWaglerin-1blocksthenicotinicacetylcholinereceptorofmatureend-plates,theappearanceoflethalitymayresultfromtheepsilon-forgamma-subunitsubstitution.Insupportofthishypothesis,adultknockout(KO)micelackingthegenecodingfortheepsilon-subunitresistthelethaleffectofWaglerin-1.Incontrast,heterozygouslittermatesrespondtoWaglerin-1likeadultwild-typemice.Invitroapplicationof1microMWaglerin-1inhibitedspontaneousminiatureend-platepotentialsandevokedend-platepotentialsofadultwild-typeandheterozygousKOmice.Bothminiatureend-platepotentialsandend-platepotentialsofneonatalwild-typeandadulthomozygousKOmiceresistedWaglerin-1.Waglerin-1decreasedtheend-plateresponseofadultwild-typemicetoiontophoreticallyappliedacetylcholine(ACh)withanIC50valueof50nM;1microMWaglerin-1decreasedtheAChresponseto4+/-1%ofcontrolforadultheterozygousKOmice.Incontrast,1microMWaglerin-1decreasedtheAChresponseto73+/-2%ofcontrolforwild-typemicelessthan11daysoldandhadnoeffectontheAChresponseofadulthomozygousKOmice.Between11and12daysafterbirth,thesuppressanteffectofWaglerin-1onwild-typeend-plateresponsestoAChdramaticallyincreased.Waglerin-1reducedbindingofalpha-bungarotoxintoend-platesofadultbutnotneonatalwild-typemice.ThesedatademonstratethatWaglerin-1selectivelyblocksthemousemusclenicotinicacetylcholinereceptorcontainingtheepsilon-subunit.

McArdleJJ. etal.Waglerin-1selectivelyblockstheepsilonformofthemusclenicotinicacetylcholinereceptor. JPharmacolExpTher. PMID: 10087048

Waglerin-1inhibitsGABA(A)currentofneuronsinthenucleusaccumbensofneonatalrats.BrainRes

TheeffectofWaglerin-1,a22-aminoacidpeptidepurifiedfromthevenomofWagler’spitviperonthewholecellcurrentresponse(I(GABA))togamma-aminobutyricacid(GABA)wasexaminedforneuronsfreshlyisolatedfromthenucleusaccumbensof3-to7-day-oldrats.Waglerin-1depressedI(GABA)inducedbysubsaturatingconcentrationsofGABA;theIC(50)forI(GABA)inducedby10microMGABAwas2.5microMWaglerin-1.ThisconcentrationofWaglerin-1shiftedtheGABAconcentration-responsecurvetotherightinaparallelmanner,increasingtheGABAEC(50)from12+/-3to27+/-5microM.ThedepressanteffectofWaglerin-1wasgreateratnegativeholdingpotentials.Zn(2+)alsoinhibitedI(GABA)withanIC(50)of0.3microM.PhosphorylationstateappearedtomodulateGABA(A)receptorsensitivitytotheinhibitoryeffectofWaglerin-1sincedialysisofneuronswithN-[2-((p-bromocinnamyl)amino)ethyl]-5-isoquinolinesulfonamideHCl(H-89),aninhibitorofproteinkinaseA,preventedinhibition.ThedataarediscussedintermsofdevelopmentalinfluencesonthesubunitcompositionofGABA(A)receptorsinneuronsofthenucleusaccumbens.

YeJH. etal. Waglerin-1inhibitsGABA(A)currentofneuronsinthenucleusaccumbensofneonatalrats. BrainRes. 1999. PMID: 10433985

Waglerin-1modulatesgamma-aminobutyricacidactivatedcurrentofmurinehypothalamicneurons
WeexaminedtheeffectofWaglerin-1,apeptideof22aminoacidresiduespurifiedfromthevenomofWagler’spitviper(Trimeresuruswagleri),onthewholecellcurrentresponse(I(GABA))offreshlyisolatedmurinehypothalamicneuronstogamma-aminobutyricacid(GABA).Althoughtheapplicationof32microMWaglerin-1alonehadnoeffectonmembraneconductance,coapplicationwithGABAincreasedI(GABA)for78andsuppressedI(GABA)for44ofthe141neuronsexamined.ThepotentiatingeffectofWaglerin-1wasassociatedwithaleftwardshiftoftheconcentration-responserelationofGABAwithoutincreasingpeakI(GABA).ThispotentiatingeffectofWaglerin-1onI(GABA)mimicsdiazepam.FurThermore,thebenzodiazepineantagonistflumazenilantagonizedWaglerin-1potentiationofI(GABA),TheseobservationssuggestthatWaglerin-1actsonthebenzodiazepinesiteofonetypeofGABA(A)receptor/channelcomplextoincreaseitsaffinityforagonist.Incontrast,thedepressanteffectofWaglerin-1wasassociatedwitharightwardshiftoftheconcentration-responserelationofGABAwithoutdepressingthemaximalI(GABA);thissuggestsacompetitiveinhibitionofasecondclassofGABAR.TheABIlityofWaglerin-1tosuppressI(GABA)showedapositivecorrelationwithasimilaractionofZn++.AswithZn++,thedepressanteffectofWaglerin-1onI(GABA)wasmorepronouncedatnegativeholdingpotentials.TheseobservationsarediscussedintermsofvariationinthesubunitcompositionofGABAreceptorsthatmurinecentralnervoussystemneuronsexpress.

YeJH. etal.Waglerin-1modulatesgamma-aminobutyricacidactivatedcurrentofmurinehypothalamicneurons. JPharmacolExpTher. PMID: 9223541

品牌介绍
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) ”。 
公司介绍
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, Smart
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其他 Kv1.3通道 GPCR 机械敏感通道 嘌呤受体 hERG/Kv11.1型 内整流钾通道 NMDA受体 高压门控Ca2 +通道
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