请使用支持JavaScript的浏览器!
主营:动物毒液多肽毒素
℡ 4000-520-616
℡ 4000-520-616
Smartox/Maurotoxin Kv and SK channels blocker/08MAR001-00500/0.5mg
产品编号:08MAR001-00500
市  场 价:¥8736.00
场      地:美国(厂家直采)
联系QQ:1570468124
电话号码:4000-520-616
邮      箱: info@ebiomall.com
美  元  价:$840.00
品      牌: Smartox
公      司:Smartox
公司分类:
Smartox/Maurotoxin Kv and SK channels blocker/08MAR001-00500/0.5mg
商品介绍

Maurotoxin isacomponentofthevenomofScorpiomauruspalmatus. Maurotoxin isamemberoftheα-KTx6.2scorpiontoxinfamily.Itblocksvoltage-gatedpotassiumchannels(KV1.1/KCNA1,KV1.2/KCNA2,andKV1.3/KCNA3)andinhibitsapamin-sensitivesmallconductancecalcium-activatedchannels(SKchannels),particularlyKCa3.1(IKca1,SK4).TheblockageofKv1.2occurswithhighaffinity.


Description:

Productcode:N/A.Categories:Kvchannels,Potassiumchannels.Tags:kv,SK.

AAsequence: Val-Ser-Cys3-Thr-Gly-Ser-Lys-Asp-Cys9-Tyr-Ala-Pro-Cys13-Arg-Lys-Gln-Thr-Gly-Cys19-Pro-Asn-Ala-Lys-Cys24-Ile-Asn-Lys-Ser-Cys29-Lys-Cys31-Tyr-Gly-Cys34-NH2
Disulfidebonds: Cys3-Cys24,Cys9-Cys29,Cys13-Cys19 andCys31 -Cys34
Length(aa): 34
Formula: C145H231N45O47S8
MolecularWeight: 3612.55Da
Appearance:Whitelyophilizedsolid
Solubility: waterorsalinebuffer
CASnumber: notavailable
Source: Synthetic
Purityrate: >95%

Reference:

Analysisoftheinteractingsurfaceofmaurotoxinwiththevoltage-gatedShakerBK(+)channel
Maurotoxin(MTX)isa34-residuetoxinthatwasisolatedinitiallyfromthevenomofthescorpionScorpiomauruspalmatus.Unliketheothertoxinsoftheα-KTx6family(Pi1,Pi4,Pi7,andHsTx1),MTXexhibitsauniquedisulfidebridgeorganizationofthetypeC(1)C(5),C(2)C(6),C(3)C(4),andC(7)C(8)(insteadoftheconventionalC(1)C(5),C(2)C(6),C(3)C(7),andC(4)C(8),hereinreferredtoasPi1-like)thatdoesnotpreventitsfoldingalongtheclassicα/βscaffoldofscorpiontoxins.MTX(Pi1)isanMTXvariantwithaconventionalpatternofdisulfidebridgingwithoutanyprimarystructurealterationofthetoxin.Here,usingMTXand/orMTX(Pi1)asmodels,weinvestigatedhowthetypeoffoldinginfluencestoxinrecognitionoftheShakerBpotassiumchannel.AminoacidresiduesofMTXthatwerestudiedforShakerBrecognitionwereselectedonthebasisoftheirhomologouspositionincharyBDotoxin,athreedisulfide-bridgedscorpiontoxinalsoactiveonthischanneltype.TheseresiduesfavoredeitheranMTX-orMTX(Pi1)-likefolding.OurdataindicateclearlythatLys(23)andTyr(32)(twooutoftenaminoacidresiduesstudied)arethemostimportantresiduesforShakerBchannelblockagebyMTX.ForactivityonSKCachannels,thesameaminoacidresiduesalsoaffect,directlyorindirectly,therecognitionofSKchannels.ThemolecularmodelingtechniqueandcomputeddockingindicatetheexistenceofacorrelationbetweenthehalfcystinepairingsofthemutatedanalogsandtheiractivityontheShakerBK(+)channel.Overall,mutationsinMTXcould,orcouldnot,changethereorganizationofdisulfidebridgesofthismoleculewithoutaffectingitsα/βscaffold.However,changingofthepeptidebackbone(crosslinkingdisulfidebridgesfromMTX-liketypevsMTX(Pi1)-liketype)appearstohavelessimpactonthemoleculeactivitythanmutationofcertainkeyaminoacidssuchasLys(23)andTyr(32)inthistoxin.FajlounZ, etal.,(2011)Analysisoftheinteractingsurfaceofmaurotoxinwiththevoltage-gatedShakerBK(+)channel. JPeptSci. PMID: 21308876
Effectofmaurotoxin,afourdisulfide-bridgedtoxinfromthechactoidscorpionScorpiomaurus,onShakerK+channels
Maurotoxinisa34-residuetoxinisolatedfromthevenomoftheTunisianchactoidscorpionScorpiomauruspalmatusandcontainsfourdisulfidebridgesthatarenormallyfoundinlong-chaintoxinsof60-70aminoacidresidues,whichaffectvoltage-gatedsodiumchannels.However,despitetheunconventionaldisulfide-bridgepatternofmaurotoxin,theconformationofthistoxinremainssimilartothatofothertoxinsactingonpotassiumchannels.Here,weanalyzedtheeffectsofsyntheticmaurotoxinonvoltage-gatedShakerpotassiumchannels(ShB)expressedinXenopusoocytes.Maurotoxinproducesastrong,butreversIBLe,inhibitionoftheShBK+currentwithanIC50of2nM.Increasingconcentrationsofthetoxininduceaprogressivelyhigherblockatsaturatingconcentrations.Atnonsaturatingconcentrationsofthetoxin(5-20nM),thechannelblockappearsslightlymorepronouncedatthresholdpotentialssuggestingthatthetoxinmayhaveahigheraffinityfortheclosedstateofthechannel.Atthesinglechannellevel,thetoxindoesnotmodifytheunitarycurrentamplitude,butdecreasesensemblecurrentsbyincreasingthenumberofdepolarizingepochsthatfailedtoelicitanyopening.ApointmutationofLys23toalanineinmaurotoxinproducesa1000-foldreductionintheIC50ofblockbythetoxinsuggestingtheimportanceofthischargedresiduefortheinteractionwiththechannel.MaurotoxindoesnotaffectK+currentscarriedbyKir2.3channelsinoocytesorNa+currentscarriedbythealphaIIachannelexpressedinCHOcells.Carlier,E.,etal.(2000)Effectofmaurotoxin,afourdisulfide-bridgedtoxinfromthechactoidscorpionScorpiomaurus,onShakerK+channels, JPept. PMID: 10888198
Maurotoxin,afourdisulfidebridgesscorpiontoxinactingonK+channels
Maurotoxin,a toxin fromthevenomoftheTunisianchactoid scorpion Scorpiomaurus,hasbeenpurifiedtohomogeneitybygelfiltration/reversed-phaseHPLC,andcharacterized.ItisabasicandC-terminalamidated34-residuepolypeptidecross-linkedby four disulfide bridges.FromEdmansequencingresults,onlysixdifferentpairingsbetweenthefirstsixhalf-cystineswereretainedwhereasa disulfide bridgewaspredictedbetweenthetwohalf-cystinesinpositions31and34.Modellingbasedonthestructureofcharybdotoxinfavoredtwodifferentpairings,oneofwhichpossessedtwodisulfidesincommonwiththegeneralmotifof scorpion toxins.Thesolid-phasetechniquewasusedtoobtainsynthetic maurotoxin,sMTX.Thehalf-cystinepairingsofsMTXweredeterminedbyenzymaticcleavageandwerefoundtobeCys3Cys24,Cys9-Cys29,Cys13-Cys19,andCys31-34,inagreementwithexperimentaldataobtainedwithnatural maurotoxin.Bothnaturalandsyntheticmaurotoxinswerelethaltomicefollowingintracerebroventricularinjection(LD50,80ng/mouse).TheyblockedtheKv1.1,Kv1.2,andKv1.3 channels expressedinXenopusoocyteswithalmostidenticalhalf-effects(IC50)intherangeof40,0.8and150nM,respectively.Theyalsocompetedwith125I-apamin(SKcachannelblocker)and125I-kaliotoxin(Kvchannelblocker)forbindingtoratbrainsynaptosomeswithIC50ofabout5and0.03nM.Asthenaturalandsyntheticmaurotoxinsexhibitindistinguishablephysicochemicalandpharmacologicalproperties,theyarelikelytoadoptthesamehalf-cystinepairingpatternwhichisuniqueamongknown scorpion toxins.However,this disulfide organizationisdifferentfromthosereportedforPandinusimperatorandHeterometrusspinnifertoxins1(Pi1andHsTx1),twonovel four-disulfide bridged K+channel-acting scorpion toxin sharingabout50-70%sequenceidentitywith maurotoxin.

Rochat,H., etal.(1998)Maurotoxin,afourdisulfidebridgesscorpiontoxinactingonK+channels, Toxicon.PMID: 9792177

Solutionstructureofmaurotoxin,ascorpiontoxinfromScorpiomaurus,withhighaffinityforvoltage-gatedpotassiumchannels

Maurotoxin (MTX),purifiedfromthescorpionid Scorpio maurus isapotentligandfor potassium channels.ItshowsabroadspecificityasbeingactiveonKv1.1(Kd=37nM),Kv1.2(Kd=0.8nM),Kv1.3(Kd=150nM) voltage-gated potassium channels,aswellasonsmall-conductancecalcium-activated potassium channels.Ithasauniquedisulfidepairingamongthe scorpion toxinsfamily.The solution structure ofMTXhasbeendeterminedby2D-NMRtechniques,whichledtothefulldescriptionofits3Dconformation:abendedhelixfromresidues6to16connectedbyalooptoatwo-strandedantiparallelbetasheet(residues23to26and28to31).TheinteractionofMTXwiththeporeregionoftheKv1.2 potassium channelhasbeenmodeledaccordingtotheirchargeanisotropy.The structure ofMTXissimilartoothershort scorpion toxinsdespiteitspeculiardisulfidepairing.ItsinteractionwiththeKv1.2channelinvolvesadipolemoment,whichguidesandorientsthe toxin ontothepore,towardthebindingsite,andwhichthusisresponsibleforthespecificity.

Blanc,E., etal.(1997)Solutionstructureofmaurotoxin,ascorpiontoxinfromScorpiomaurus,withhighaffinityforvoltage-gatedpotassiumchannels, Proteins. PMID: 9365987

品牌介绍

Smartox Biotechnolgy的多肽毒素产品如下:

 

1. 作用于钠离子通道(Sodium channel)的毒素

 

Toxin name

Catalog #

Target

Phrixotoxin-3

13PHX003

Selective blocker of Nav1.2

µ-conotoxin GIIIB

CON020

Selective blocker of Nav1.4

µ-conotoxin CnIIIC

CON021

Selective blocker of Nav1.4

μ-conotoxin PIIIA

08CON006

Selective blocker of Nav1.4

Jingzhaotoxin-III

12JZH003

Selective blocker of Nav1.5

ProTx-II

07PTX002

Selective blocker of Nav1.7

ProTx-II Biotin

12PTB002

Selective blocker of Nav1.7

ProTx-I

12PTX001

Blocker of Nav1.8, Nav1.2, Nav1.5, Nav1.7

Huwentoxin-I

07HWT001

Blocker of TTX-S

Huwentoxin-IV

08HWT002

Blocker of TTX-S

Hainantoxin-III

13HTX003

Blocker of TTX-S

Hainantoxin-IV

12HTX001

Blocker of TTX-S

GsAF-I

12GSF001

Blocker of TTX-S

GsAF-II

12GSF002

Blocker of TTX-S

 

2. 作用于钾离子通道(Potassium channel)的毒素

 

Toxin name

Catalog #

Target

KCa channels

Apamin 蜜蜂神经毒素

08APA001

SK1, SK2, SK3

Charybdotoxin 蝎毒素

11CHA001

KCa1.1, KCa3.1 - Kv1.2, Kv1.3, Kv1.6

Iberiotoxin

12IBX001

KCa1.1

Leiurotoxin 1 (Scyllatoxin)

10LEI001

SK1, SK2, SK3

Tamapin

10TAM001

SK1, SK2, SK3

Kaliotoxin-1

08KTX002

BK, Kv1.1, Kv1.2, Kv1.3

Kv channels

ShK

08SHK001

Kv1.3, Kv1.1, Kv1.4, Kv1.6

TMR-ShK

SAT001

Kv1.3, Kv1.1

Margatoxin

08MAG001

Kv1.3

(Dap22)-ShK

13SHD001

Kv1.3

ADWX-1

13ADW001

Kv1.3

HsTx1

08NEU001

Kv1.3, Kv1.2

Agitoxin-2

13AGI002

Kv1.3, Kv1.1

Maurotoxin

08MAR001

Kv1.2, KCa3.1

Guangxitoxin 1E

11GUA002

Kv2.1, Kv2.2

Stromatoxin 1 NEW

SCT01

Kv2.1, Kv2.2

Kaliotoxin-1

08KTX002

BK, Kv1.1, Kv1.2, Kv1.3

Charybdotoxin

11CHA001

KCa1.1, KCa3.1 - Kv1.2, Kv1.3, Kv1.6

Phrixotoxin-2

PHX002

Kv4.2, Kv4.3

AmmTx3 NEW

AMX001

A-type potassium channels

Inwardly rectifying potassium channels

TertiapinQ

08TER001

Kir1.1, Kir3.1/3.4, Kir3.1/3.2-KCa1.1

hERG/Kv11.1

BeKm-1

13BEK001

ERG1

 

3. 作用于钙离子通道(Calcium channel)的毒素

 

Toxin name

Catalog #

Target

High voltage-gated Ca2+ channels

ω-agatoxin IVA

11AGA001

P/Qtype

ω-Conotoxin MVIIC

08CON002

P/Qtype, N-type

ω-Conotoxin MVIIA

08CON001

N-type

ω-Conotoxin GVIA

08CON003

N-type

ω-Conotoxin SO3

08CON013

N-type

Huwentoxin I

07HWT001

N-type

ProTx-II

07PTX002

T-type, L-type

Intermediate voltage-gated Ca2+ channels

SNX482

08SNX002

R-type

Low voltage-gated Ca2+ channels

ProTx-I

12PTX001

T-type

ProTx-II

07PTX002

T-type, L-type

Ryanodine receptors

Maurocalcine

07PAU001

Ryr1

 

4. 作用于氯离子通道(Chloride channel)的毒素

 

Toxin name

Catalog #

Target

Chlorotoxin

08CHL001

Blocker of small conductance Cl- channels

GaTx1

13GTX001

Selective blocker of CFTR channel

GaTx2

10GTX002

Selective blocker of ClC-2 channel

 

5. 作用于乙酰胆碱受体(Acetylcholine receptor)的毒素

 

Toxin name

Catalog #

Target

α-conotoxin PeIA

13CON017

α9α10, α3β2 subunits

α-Conotoxin PrXA

13CON016

α1/β1/ε/δ, α1/β1/γ/δ subunits

Waglerin-1

12WAG001

MusclenAChR

α-conotoxin MI

08CON012

α1/δsubunits

α-conotoxin GI

08CON005

α/δsite

α-conotoxin IMI

08CON011

α7 homomeric nAChR

α-conotoxin GID

CON019

Blocker of α3β2, α7 and α4β2 nAChRs

 

6. 含N-甲基-D-天冬氨酸NR2B

(NMDA, NR2B containing N-methyl-D-aspartate)

Conantokin-G

选择性、特异性抑制含NR2B的NMDAR。Conantokin-G能剂量依赖性抑制Ca2+内流,抑制NMDA诱导的兴奋性中毒效应。研究表明,在小鼠皮层神经元,Conantokin-G阻滞NMDA引发的电流信号的IC50值为480 nM。

 

7. 作用于酸敏感离子通道(ASIC channel, Acid-Sensing Ion Channel)的毒素

 

Toxin name

Catalog #

Target

APETx2

07APE002

Selective blocker of ASIC3

Psalmotoxin1/PcTx1

13PCT001

Selective blocker of ASIC1a

Ugr9-1

13UGR001

Blocker of ASIC3

 

8. 作用于瞬时受体电位(TRP channel, transient receptor potential)的毒素

 

Toxin name

Catalog #

Target

GsMTx4

08GSM001

TRPC, TRPA

Vanillotoxin3

10VAN003

Activator of TRPV1

ProTx-I

12PTX001

Antagonist of TRPA1

 

9. 作用于嘌呤能通道(Purinergic channel)的毒素

Purotoxin-1

选择性抑制P2X3受体。100 nM Purotoxin-1 (PT-1)选择性抑制P2X3受体通道,在大鼠DRG神经元上,使用膜片钳实验表明:PT-1对电压门控通道和TRPV1均无抑制效应。10 µM ATP和100 µM α,β Methylene-ATP浓度下Purotoxin-1对P2X3受体有选择性作用,在该ATP浓度下Purotoxin-1对P2X2和杂化二聚体P2X2/3并无激动作用。Purotoxin-1对疼痛的潜在治疗作用。

 

10. 作用于其它膜受体通道(Others)的毒素

Smartox Biotechnology还提供其他类型的膜受体抑制剂:

 

Toxin name

Catalog #

Target

Morphiceptin

011CAS001

Agonist of µ-opoid receptors

Lys-conopressin G

11CON14

Vasopressin-like peptide

GsMTx4

08GSM001

Mechano sensitive ion channels

Obtustatin

10OBT001

Blocks the binding of α1β1  integrin to collagen IV

Rho-Conotoxin TIA

CON022

Blocks α1-adrenergic receptor

 

 

公司简介

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)”。

总之,Smartox Biotechnolgy提供一系列高质量、具开创价值的多肽毒素。这些化合物在离子通道 研究中具有高的亲和性和选择性,是相应领域科学研究理想的生物毒素提供商和贴心的合作伙伴。


自营商城图标
厂家直采
全球直采 正品优价
正品保障图标
正品保障
厂家直发 有线跟踪
解放采购图标
正规清关
CIF100%正规报关,提供发票
及时交付图标
及时交付
限时必达 不达必赔