ProTx II

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.

Designed for biological research and industrial applications, not intended for individual clinical or medical purposes.
ProTx II(CAS 484598-36-9)

CAT No: R0894

CAS No:484598-36-9

Synonyms/Alias:ProTx II;484598-36-9;ProTx-II;PTX-3995-PI;JUA59836;AKOS024457935;PD079626;

Custom Peptide Synthesis
cGMP Peptide
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  • CMC information required for an IND
  • IND and NDA support
  • Drug master files (DMF) filing
M.F/Formula
C168H250N46O41S8
M.W/Mr.
3827
Sequence
One Letter Code:YCQKWMWXCDSERKCCEGMVCRLWCKKKLW
Three Letter Code:H-DL-Tyr-DL-Cys(1)-DL-Gln-DL-Lys-DL-Trp-DL-Met-DL-Trp-DL-xiThr-DL-Cys(2)-DL-Asp-DL-Ser-DL-Glu-DL-Arg-DL-Lys-DL-Cys(3)-DL-Cys(1)-DL-Glu-Gly-DL-Met-DL-Val-DL-Cys(2)-DL-Arg-DL-Leu-DL-Trp-DL-Cys(3)-DL-Lys-DL-Lys-DL-Lys-DL-Leu-DL-Trp-OH
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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