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Smartox/Huwentoxin-XVI is a selective blocker of N-type Ca2+ channels/HWT016-00100/0.1mg

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¥2246.40
货号:HWT016-00100
浏览量:127
品牌:Smartox
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商品描述

Huwentoxin-XVIisa39aminoacidspeptidethatwasdiscoveredfromthevenomoftheChinesetarantulaOrnithoctonushuwena.Huwentoxin-XVIwasshowntobeapotentblockerofHVAN-typecalciumchannelswithanIC50valueof60nMinratDRG.Theblockingeffectappearstobesimilartothatofω-conotoxin-GVIAandω-conotoxin-MVIIA.Neverthelss,Huwentoxin-XVIdiffersfromGVIAandMVIIAthankstoitsgreaterreversibilityanditshigherselectivityforN-typeoverP/QtypethanMVIIA.


Description:

Productcode:N/A.Category:Highvoltage-gatedCa2+channels.Tags:Cav2.2,N-type.

AAsequence: Cys1-Ile-Gly-Glu-Gly-Val-Pro-Cys8-Asp-Glu-Asn-Asp-Pro-Arg-Cys15-Cys16-Ser-Gly-Leu-Val-Cys21-Leu-Lys-Pro-Thr-Leu-His-Gly-Ile-Trp-Tyr-Lys-Ser-Tyr-Tyr-Cys36-Tyr-Lys-Lys-OH
Disulfidebonds:    Cys1-Cys16,Cys8-Cys21andCys15-Cys36
Length(aa):39
Formula:  C196H292N50O56S6
Appearance:Whitelyophilizedsolid
MolecularWeight:4437.2Da
CASnumber:Notavailable
Source:Synthetic
Purityrate:>98%

Forresearchuseonly

Reference:

Huwentoxin-XVI,ananalgesic,highlyreversIBLemammalianN-typecalciumchannelantagoNISTfromChinesetarantulaOrnithoctonushuwena
N-typecalciumchannelsplayimportantrolesinthecontrolofneurotransmissionreleaseandtransmissionofpainsignalstothecentralnervoussystem.Theirselectiveinhibitorsarebelievedtobepotentialdrugsfortreatingchronicpain.Inthisstudy,anovelneurotoxinnamedHuwentoxin-XVI(HWTX-XVI)specificforN-typecalciumchannelswaspurifiedandcharacterizedfromthevenomofChinesetarantulaOrnithoctonushuwena.HWTX-XVIiscomposedof39aminoacidresiduesincludingsixcysteinesthatconstitutethreedisulfidebridges.HWTX-XVIcouldalmostcompletelyblockthetwitchresponseofratvasdeferenstolow-frequencyelectricalstimulation.ElectrophysiologicalassayindicatedthatHWTX-XVIspecificallyinhibitedN-typecalciumchannelsinratdorsalrootganglioncells(IC50∼60 nM).TheinhibitoryeffectofHWTX-XVIonN-typecalciumchannelcurrentswasdose-dependentandsimilartothatofCTx-GVIAandCTx-MVIIA.However,thethreepeptidesexhibitedmarkedlydifferentdegreesofreversibilityafterblock.Thetoxinhadnoeffectonvoltage-gatedT-typecalciumchannels,potassiumchannelsorsodiumchannels.IntraperitonealinjectionofthetoxinHWTX-XVItoratselicitedsignificantanalgesicresponsestoformalin-inducedinflammationpain.Toxintreatmentalsochangedwithdrawallatencyinhotplatetests.Intriguingly,wefoundthatintramuscularinjectionofthetoxinreducedmechanicalallodyniainducedbyincisionalinjuryinVonFreytest.Thus,ourfindingssuggestthattheanalgesicpotencyofHWTX-XVIanditsgreaterreversibilitycouldcontributetothedesignofanovelpotentialanalgesicagentwithhighpotencyandlowsideeffects

DengM.,etal.(2014)Huwentoxin-XVI,ananalgesic,highlyreversiblemammalianN-typecalciumchannelantagonistfromChinesetarantulaOrnithoctonushuwena.Neuropharmacol. 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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