| Size | Price | Stock | Qty |
|---|---|---|---|
| 500μg |
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| 1mg |
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| 5mg |
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| Other Sizes |
| Targets |
Nav1.7
The primary target of ProTxII is the voltage-gated sodium channel Nav1.7, which is predominantly expressed in peripheral sensory neurons and plays a critical role in pain signaling. ProTxII is a selective blocker of Nav1.7 with an IC50 of 0.3 nM and is at least 100-fold selective for Nav1.7 over other sodium channels. By binding to and blocking Nav1.7, ProTxII prevents the initiation and propagation of action potentials in pain-sensing neurons, thereby exerting analgesic effects. |
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| ln Vitro |
In vitro, ProTxII is a potent and selective inhibitor of Nav1.7 with an IC50 of 0.3 nM. It shows at least 100-fold selectivity for Nav1.7 over other sodium channels. The compound is a peptide toxin with a molecular weight of 3826.59 g/mol. It is typically used in electrophysiological studies to examine Nav1.7 function and to study the role of this channel in pain signaling. ProTxII is soluble in water to 1 mg/ml and is stored as a lyophilized solid at -20°C.
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| ln Vivo |
In vivo, ProTxII has potential applications in the study of pain and nociception by blocking Nav1.7 channels in peripheral sensory neurons. However, as a peptide toxin, its in vivo use is limited by its pharmacokinetic properties, including poor oral bioavailability and rapid clearance. It is primarily used as a research tool for in vitro studies rather than as a therapeutic agent. Further studies are needed to explore its potential in vivo applications.
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| Enzyme Assay |
In vitro assays for ProTxII typically involve measuring its inhibition of Nav1.7 channel activity using electrophysiological techniques such as patch-clamp recording in cell lines expressing recombinant Nav1.7 channels. The toxin is applied to the cells at varying concentrations (typically 0.01-10 nM), and the resulting inhibition of sodium current is measured. The IC50 of 0.3 nM is determined by fitting concentration-response curves. Selectivity assays against other sodium channel subtypes are also performed to assess the toxin's specificity.
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| Cell Assay |
Cellular assays for ProTxII typically use cell lines expressing recombinant Nav1.7 channels, such as HEK293 or CHO cells. The toxin is applied to the cells, and its effects on channel activity are assessed using electrophysiological techniques such as patch-clamp recording. Fluorescent-based membrane potential assays using voltage-sensitive dyes can also be used for higher-throughput screening of channel activity. Cells are treated with ProTxII at various concentrations (e.g., 0.01-10 nM), and the inhibition of sodium current or changes in membrane potential are measured. The IC50 for channel inhibition is determined from the concentration-response data.
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| Animal Protocol |
In vivo animal studies for ProTxII would typically involve the administration of the toxin to rodent models of pain to assess its analgesic effects. However, as a peptide toxin, ProTxII is primarily used as a research tool for in vitro studies rather than for in vivo applications. Its poor oral bioavailability and rapid clearance limit its utility in vivo. Studies involving ProTxII in vivo would likely require administration via intrathecal or local injection to achieve sufficient concentrations at the target site.
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| ADME/Pharmacokinetics |
As a peptide toxin, ProTxII has poor oral bioavailability and is rapidly cleared from circulation. It has a molecular weight of 3826.59 g/mol and is soluble in water. For research purposes, the toxin is typically stored as a lyophilized solid at -20°C. Detailed pharmacokinetic parameters such as half-life, volume of distribution, and bioavailability are not fully available in the public domain but are characteristic of peptide toxins.
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| Toxicity/Toxicokinetics |
There is no specific toxicity data reported for ProTxII in the available literature. As a research chemical and peptide toxin intended for laboratory use only, it should be handled with standard safety precautions for handling biological reagents. The compound is not approved for human therapeutic use. Researchers should consult the material safety data sheet (MSDS) for detailed safety and handling information. Any potential toxicity would need to be assessed through formal toxicological studies if the compound were to be developed further.
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| References |
[1]. Tanaka K, et al. Antihyperalgesic effects of ProTx-II, a Nav1.7 antagonist, and A803467, a Nav1.8 antagonist, in diabetic mice. J Exp Pharmacol. 2015 Jun 24;7:11-6.
[2]. Schmalhofer WA, et al. ProTx-II, a selective inhibitor of NaV1.7 sodium channels, blocks action potential propagation in nociceptors. Mol Pharmacol. 2008 Nov;74(5):1476-84. |
| Additional Infomation |
ProTxII is a peptide toxin that acts as a selective blocker of Nav1.7 with an IC50 of 0.3 nM. It has a molecular formula of C168H250N46O41S8 and a molecular weight of 3826.59 g/mol. ProTxII is at least 100-fold selective for Nav1.7 over other sodium channels. It is a 29-amino acid peptide toxin originally isolated from tarantula venom and is used as a research tool to study Nav1.7 in pain signaling. ProTxII is soluble in water and is stored at -20°C.
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| Molecular Formula |
C168H250N46O41S8
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|---|---|
| Exact Mass |
3824.669
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| CAS # |
484598-36-9
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| Related CAS # |
ProTx II TFA
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| PubChem CID |
90488904
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| Appearance |
Typically exists as solid at room temperature
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| LogP |
-11.9
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| Hydrogen Bond Donor Count |
53
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| Hydrogen Bond Acceptor Count |
57
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| Rotatable Bond Count |
77
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| Heavy Atom Count |
263
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| Complexity |
8680
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC(C)CC1C(=O)NC(C(=O)NC(CSSCC2C(=O)NC3CSSCC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(CSSCC(C(=O)NC(C(=O)N1)CCCNC(=N)N)NC(=O)C(NC(=O)C(NC(=O)CNC(=O)C(NC3=O)CCC(=O)O)CCSC)C(C)C)C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N2)CCCCN)CCCNC(=N)N)CCC(=O)O)CO)CC(=O)O)C(C)O)CC4=CNC5=CC=CC=C54)CCSC)CC6=CNC7=CC=CC=C76)CCCCN)CCC(=O)N)NC(=O)C(CC8=CC=C(C=C8)O)N)C(=O)NC(CCCCN)C(=O)NC(CCCCN)C(=O)NC(CCCCN)C(=O)NC(CC(C)C)C(=O)NC(CC9=CNC1=CC=CC=C19)C(=O)O)CC1=CNC2=CC=CC=C21
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| InChi Key |
XOAUGYVLRSCGBG-UHFFFAOYSA-N
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| InChi Code |
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)
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| Chemical Name |
2-[[2-[[6-amino-2-[[6-amino-2-[[6-amino-2-[[27,57-bis(4-aminobutyl)-21-[[2-amino-3-(4-hydroxyphenyl)propanoyl]amino]-24-(3-amino-3-oxopropyl)-54,74-bis(3-carbamimidamidopropyl)-13,51-bis(2-carboxyethyl)-45-(carboxymethyl)-39-(1-hydroxyethyl)-48-(hydroxymethyl)-30,36,68-tris(1H-indol-3-ylmethyl)-71-(2-methylpropyl)-7,33-bis(2-methylsulfanylethyl)-3,6,9,12,15,22,25,28,31,34,37,40,43,46,49,52,55,58,67,70,73,76,81-tricosaoxo-4-propan-2-yl-18,19,62,63,78,79-hexathia-2,5,8,11,14,23,26,29,32,35,38,41,44,47,50,53,56,59,66,69,72,75,82-tricosazatricyclo[40.34.4.216,60]dooctacontane-65-carbonyl]amino]hexanoyl]amino]hexanoyl]amino]hexanoyl]amino]-4-methylpentanoyl]amino]-3-(1H-indol-3-yl)propanoic acid
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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