| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| Other Sizes |
| Targets |
Heteropodatoxin-2 targets Kv4.2 voltage-gated potassium channels, which are members of the Shal-related subfamily of voltage-gated potassium channels. Kv4.2 channels are primarily expressed in the brain and heart, where they mediate A-type potassium currents that regulate neuronal excitability and cardiac repolarization. The toxin blocks these channels in a voltage-dependent manner.
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| ln Vitro |
Heteropodatoxin-2 shows potent in vitro activity against Kv4.2 potassium channels expressed in Xenopus oocytes. The toxin blocks Kv4.2 currents in a voltage-dependent manner, with less blockade at more positive potentials, suggesting that the toxin binds preferentially to the closed or inactivated state of the channel. The IC₅₀ for Kv4.2 blockade is in the nanomolar range.
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| ln Vivo |
In vivo activity of Heteropodatoxin-2 has not been extensively reported in the available literature. As a spider venom peptide that blocks Kv4.2 channels, it may have effects on neuronal excitability and cardiac function. The toxin is primarily used as a research tool for studying potassium channel function and pharmacology rather than as a therapeutic agent.
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| Enzyme Assay |
Non-cell-based binding assays for Heteropodatoxin-2 typically involve electrophysiological recordings in heterologous expression systems. A typical protocol includes: injecting Xenopus oocytes with Kv4.2 channel mRNA, incubating for 1–3 days to allow channel expression, performing two-electrode voltage-clamp recordings, applying the toxin at various concentrations (0.1 nM–1 μM), and measuring current blockade. Binding affinity (Kd) and voltage dependence of block are determined from the electrophysiological data.
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| Cell Assay |
Cell-based assays for Heteropodatoxin-2 involve electrophysiological recordings in mammalian cell lines expressing Kv4.2 channels. A representative protocol includes: culturing CHO or HEK293 cells stably or transiently expressing Kv4.2, performing whole-cell patch-clamp recordings, applying the toxin at various concentrations via perfusion, and measuring inhibition of Kv4.2-mediated currents. Toxin specificity can be assessed by testing against other potassium channel subtypes.
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| Animal Protocol |
In vivo animal studies with Heteropodatoxin-2 are limited due to the toxin's peptide nature and potential toxicity. When studied, a typical protocol might include: administering the toxin via intracerebroventricular (ICV) or intravenous injection in rodent models, monitoring behavioral and physiological parameters, and assessing effects on neuronal excitability or cardiac function. The toxin is primarily used as a research tool rather than for therapeutic development.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of Heteropodatoxin-2 have not been extensively reported. As a 30-amino acid peptide toxin, it is expected to have rapid clearance from circulation, limited oral bioavailability, and potential immunogenicity. The TFA salt form is used to enhance solubility and stability.
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| Toxicity/Toxicokinetics |
Toxicological data for Heteropodatoxin-2 are limited as it is a research-use toxin. As a Kv4.2 channel blocker, it may have significant effects on neuronal and cardiac function at high doses. Standard laboratory safety precautions should be followed when handling the toxin. The compound should be stored in a sealed container, protected from moisture and light.
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| References | |
| Additional Infomation |
Heteropodatoxin-2 (TFA) is a valuable research tool for studying Kv4.2 potassium channel structure, function, and pharmacology. The voltage-dependent block provides insights into the gating mechanisms of Kv4.2 channels. As a spider venom peptide, it represents a class of naturally occurring toxins that have contributed significantly to our understanding of ion channel biology. The toxin is also known as Heteropodotoxin-2.
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| Molecular Formula |
C144H207N39O46S6.XC2HF3O2
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| Molecular Weight |
3412.81 (free base)
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| Appearance |
White to off-white solid powder
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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 Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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) |
H2O :≥ 50 mg/mL
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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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