ProTx-II, an effective and selective NaV1.7 channel blocker, shifts activation gating positively and decreases current magnitude. It blocks action potential propagation in nociceptors.
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M.F/Formula | C168H250N46O41S8 |
M.W/Mr. | 3826.59 |
Sequence | YCQKWMWTCDSERKCCEGMVCRLWCKKKLW(Disulfide bridge: Cys2-Cys16, Cys9-Cys21, Cys15-Cys25) |
Labeling Target | NaV1.7 channel |
Purity | >98% |
Activity | Blocker |
Long-term Storage Conditions | Soluble in water |
Solubility | -20 °C |
InChI | InChI=1S/C168H250N46O41S8/c1-86(2)66-117-151(239)203-120(70-92-75-183-102-35-15-11-31-97(92)102)154(242)209-126(159(247)193-106(39-19-24-58-170)141(229)188-105(38-18-23-57-169)140(228)189-107(40-20-25-59-171)143(231)200-118(67-87(3)4)152(240)205-123(166(254)255)72-94-77-185-104-37-17-13-33-99(94)104)81-259-261-83-128-163(251)210-127-82-260-258-80-125(207-138(226)100(174)68-90-45-47-95(217)48-46-90)158(246)197-113(49-52-131(175)218)147(235)191-108(41-21-26-60-172)144(232)201-119(69-91-74-182-101-34-14-10-30-96(91)101)153(241)198-116(56-65-257-9)149(237)202-121(71-93-76-184-103-36-16-12-32-98(93)103)156(244)214-137(89(7)216)165(253)212-130(162(250)204-122(73-135(224)225)155(243)206-124(79-215)157(245)196-114(51-54-134(222)223)148(236)192-110(43-28-62-180-167(176)177)142(230)190-109(146(234)208-128)42-22-27-61-173)85-263-262-84-129(161(249)194-111(145(233)199-117)44-29-63-181-168(178)179)211-164(252)136(88(5)6)213-150(238)115(55-64-256-8)187-132(219)78-186-139(227)112(195-160(127)248)50-53-133(220)221/h10-17,30-37,45-48,74-77,86-89,100,105-130,136-137,182-185,215-217H,18-29,38-44,49-73,78-85,169-174H2,1-9H3,(H2,175,218)(H,186,227)(H,187,219)(H,188,229)(H,189,228)(H,190,230)(H,191,235)(H,192,236)(H,193,247)(H,194,249)(H,195,248)(H,196,245)(H,197,246)(H,198,241)(H,199,233)(H,200,231)(H,201,232)(H,202,237)(H,203,239)(H,204,250)(H,205,240)(H,206,243)(H,207,226)(H,208,234)(H,209,242)(H,210,251)(H,211,252)(H,212,253)(H,213,238)(H,214,244)(H,220,221)(H,222,223)(H,224,225)(H,254,255)(H4,176,177,180)(H4,178,179,181) |
InChI Key | XOAUGYVLRSCGBG-UHFFFAOYSA-N |
References | The tarantula venom peptides ProTx-I and ProTx-II inhibit voltage-gated sodium channels by shifting their voltage dependence of activation to a more positive potential, thus acting by a mechanism similar to that of potassium channel gating modifiers such as hanatoxin and VSTX1. ProTx-I and ProTx-II inhibit all sodium channel (Nav1) subtypes tested with similar potency and represent the first potent peptidyl inhibitors of TTX-resistant sodium channels. Like gating modifiers of potassium channels, ProTx-I and ProTx-II conform to the inhibitory cystine knot motif, and ProTx-II was demonstrated to bind to sodium channels in the closed state. ProTx-I and ProTx-II: Gating modifiers of voltage-gated sodium channels |
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