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蚂蚁淘在线 / 品牌中心 / Smartox / Smartox/SK2 channel blocker/LED01-50010/5x.0.01mg

Smartox/SK2 channel blocker/LED01-50010/5x.0.01mg

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￥2433.60
货号：LED01-50010
浏览量：127
品牌：Smartox
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Leiuorotoxin-Dab7(Lei-Dab7)isamutatedversionofLeiurotoxin,apeptideidentifiedfromthevenomofthescorpionLeiurusquinquestriatushebraeus.TheDabaminoacidinposition7conferstothiscompoundahighselectivityforSK2channelsamongotherchannels.Lei-Dab7exhibits>200foldselectivityforSK2overSK1,SK3,IK,KvandKirchannels.TheIC50forSK2isabout3nM.


Description:

Productcode:N/A.Categories:KCachannels,Potassiumchannels.Tags:116235-63-3,leidab7,leiurotoxin,SK.

AAsequence:Ala-Phe-Cys3-Asn-Leu-Arg-Dab-Cys8-Gln-Leu-Ser-Cys12-Arg-Ser-Leu-Gly-Leu-Leu-Gly-Lys-Cys21-Ile-Gly-Asp-Lys-Cys26-Glu-Cys28-Val-Lys-His-NH2
Disulfidebondsbetween:Cys3-Cys21,Cys8-Cys26andCys12-Cys28
Length(aa):31
Formula: C141H236N46O39S6
MolecularWeight:3392.12Da
Appearance:Whitelyophilizedsolid
Solubility:waterandsalinebuffer
CASnumber:[1061556-49-7]Source:Synthetic
Purityrate:>95%

Reference:

Correspondencesbetweenthebindingcharacteristicsofanon-naturalpeptide,Lei-Dab7

Small-conductancecalcium-activatedpotassiumchannels(SK1-SK3channels)areresponsIBLeforlong-lastinghyperpolarizationfollowingactionpotentialandcontributetotheneuronalfiringandintegrationsignal.Twopeptidetoxins:apaminandLeiurotoxin1,blockthisSKchannelswithhighaffinities.WegeneratedamodifiedLeiurotoxin1(Lei-Dab7)thatinhibitsSK2channelswithahighselectivity.CompetitivebindingofrADIo-iodinatedapamintodifferentratbrainstructures,inthepresenceofnativeapaminandLei-Dab7,hasshownthatdissociationconstantsdifferbyafactorof1000andthusdemonstratedthatligandaffinityisasimportantasligandselectivityforaspecificreceptor.However,thelackofligandsdiscriminatingbetweenSKchannelsubunitsisimpedingtheunderstandingoftheroleofeachheteromericSKchanneltypeindifferenttissues.OurstudyaimstobetterunderstandthemolecularcombinationsofSKchannelsandtheirassociationwithspecificfunctionalimplications.Onthispurpose,aclusteringtechniqueallowsustoidentifyfivegroupsofbrainstructuresreflectingsingularprofilesofaffinityandselectivityofLei-Dab7incomparisonwithapamin.TheanalysisofcorrespondencesbetweenLei-Dab7bindinganddistributionofSKsubunitsinthesegroupsofbrainstructuressuggeststhatfunctionalheteromericSKchannelsareinvolvedinspecificinformationprocesses.

Aidi-KnaniS.,etal.(2015)Correspondencesbetweenthebindingcharacteristicsofanon-naturalpeptide,Lei-Dab7,andthedistributionofSKsubunitsintheratcentralnervoussystem.EurJPharmacol.PMID:25704615

 

Small-conductanceCa2+-activatedpotassiumtype2channelsregulatetheformationofcontextualfearmemory
Small-conductance,Ca2+activatedK+channels(SKchannels)areexpressedathighlevelsinbrainregionsresponsibleforlearningandmemory.InthecurrentstudywecharacterizedthecontributionofSK2channelstosynapticplasticityandtodifferentphasesofhippocampalmemoryformation.SelectiveSK2antisense-treatmentfacilitatedbasalsynaptictransmissionandtheta-burstinducedLTPinhippocampalbrainslices.UsingtheselectiveSK2antagoNISTLei-Dab7orSK2antisenseprobes,wefoundthathippocampalSK2channelsarecriticalduringtwodifferenttimewindows:1)blockadeofSK2channelsbeforethetrainingimpairedfearmemory,whereas,2)blockadeofSK2channelsimmediatelyafterthetrainingenhancedcontextualfearmemory.Weprovidedtheevidencethatthepost-trainingcleavageoftheSK2channelswasresponsiblefortheobservedbidirectionaleffectofSK2channelblockadeonmemoryconsolidation.Thus,Lei-Dab7-injectionbeforetrainingimpairedtheC-terminalcleavageofSK2channels,whileLei-Dab7givenimmediatelyaftertrainingfacilitatedtheC-terminalcleavage.Applicationofthesyntheticpeptidecomprisingaleucine-zipperdomainoftheC-terminalfragmenttoJurkatcellsimpairedSK2channel-mediatedcurrents,indicatingthattheendogenouslycleavedfragmentmightexertitseffectsonmemoryformationbyblockingSK2channel-mediatedcurrents.OurpresentfindingssuggestthatSK2channelproteinscontributetosynapticplasticityandmemorynotonlyasionchannelsbutalsobyadditionallygeneratingaSK2C-terminalfragment,involvedinbothprocesses.Themodulationoffearmemorybydown-regulatingSK2C-terminalcleavagemighthaveapplicABIlityinthetreatmentofanxietydisordersinwhichfearconditioningisenhanced.

MurthySR.,etal.(2015)Small-conductanceCa2+-activatedpotassiumtype2channelsregulatetheformationofcontextualfearmemory.PLoSOne.PMID:25938421

Smallconductancecalcium-activatedK+channels,SkCa,butnotvoltage-gatedK+(Kv)channels,areimplicatedintheantinociceptioninducedbyCGS21680,aA2Aadenosinereceptoragonist.

IthasbeenshownthatA2Aadenosinereceptorsareimplicatedinpainmodulation.TheprecisemechanismbywhichactivationofA2Areceptorsproducesanalgesiceffects,however,remainsunclear.Theaimofthisstudywastoinvestigatethepossibleinvolvementofapamin-sensitivecalcium-activatedpotassiumchannels(SKCa)andvoltage-gatedpotassium(Kv)channelsinA2Areceptoractivation-inducedanalgesiceffects.Usingmice,weevaluatedtheinfluenceofapamin,anonspecificblockerofSKCachannels,Lei-Dab7(ananalogofscorpionLeiurotoxin),aselectiveblockerofSKCa2channels,andkaliotoxin(KTX)aKvchannelblocker,ontheCGS21680(A2Aadenosinereceptoragonist)-inducedincreasesinhotplateandtailpinchlatencies.Alldrugswereinjectedinmiceviatheintracerebroventricularroute.WefoundthatapaminandLei-Dab7,butnotKTX,reducedantinociceptionproducedbyCGS21680onthehotplateandtailpinchtestsinadosedependentmanner.Lei-Dab7wasmorepotentthanapamininthisregard.WeconcludethatSKCabutnotKvchannelsareimplicatedinCGS21680-inducedantinociception.

RegayaI.,etal.(2004)Smallconductancecalcium-activatedK+channels,SkCa,butnotvoltage-gatedK+(Kv)channels,areimplicatedintheantinociceptioninducedbyCGS21680,aA2Aadenosinereceptoragonist.LifeSci.PMID:15530499

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。