| Size | Price | Stock | Qty |
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| 1mg |
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| Other Sizes |
| Targets |
Charybdotoxin TFA targets potassium channels, specifically calcium-activated potassium channels (KCa1.1/BK and KCa3.1/IK). It is a highly specific blocker of these channels, with little effect on voltage-gated potassium channels. The peptide binds to the channel pore and physically occludes ion conductance.
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| ln Vitro |
Charybdotoxin is an excellent resource for learning about K+ channels [1].
In vitro, Charybdotoxin is an excellent resource for studying K+ channels. It is used to block BK and IK channels in electrophysiology experiments. At concentrations of 10-100 nM, it completely inhibits BK channel currents in patch-clamp recordings. It has no effect on voltage-gated K+ channels (e.g., Kv1.x) at these concentrations. |
| ln Vivo |
In vivo, Charybdotoxin is used to study the physiological role of BK and IK channels in animal models. It is injected (e.g., intracerebroventricularly or intrathecally) to assess the contribution of these channels to pain, neuronal excitability, and smooth muscle tone. Detailed in vivo efficacy data for the TFA salt form is limited.
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| Enzyme Assay |
For in vitro binding assays, the affinity of Charybdotoxin TFA for BK channels is determined using radiolabeled iberiotoxin (a BK-specific toxin) competition. Membrane preparations from smooth muscle or brain are incubated with 125I-iberiotoxin and varying concentrations of Charybdotoxin TFA (0-1000 nM). Bound radioactivity is measured by filtration.
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| Cell Assay |
For cell-based assays, CHO or HEK293 cells stably expressing BK or IK channels are used. Whole-cell or inside-out patch-clamp recordings are performed. Charybdotoxin TFA (1-100 nM) is applied to the extracellular solution via a perfusion system. The reduction in K+ current amplitude is measured as a percentage of control.
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| Animal Protocol |
For animal studies, rodents (mice or rats) are used. Charybdotoxin TFA is typically dissolved in saline (with 0.1% BSA to prevent adsorption) and administered via intrathecal injection (e.g., 10-100 pmol/mouse) or intracerebroventricular injection. Behavioral endpoints such as pain sensitivity (e.g., tail-flick or hot plate test) are measured.
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| ADME/Pharmacokinetics |
Charybdotoxin TFA has a molecular weight of 4409.91 Da (for the TFA salt). The TFA salt enhances water solubility. As a peptide, it is susceptible to proteolytic degradation in vivo, which limits its half-life. It is stored as a powder at -20degC, protected from light and moisture. The free base CAS is 95751-30-7.
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| Toxicity/Toxicokinetics |
Charybdotoxin TFA is a research-grade peptide not for human use. At standard research doses (e.g., pmol amounts in the CNS), it is considered non-toxic. However, as a potent K+ channel blocker, it can be lethal if administered systemically at high doses due to effects on smooth muscle and neuronal excitability.
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| References | |
| Additional Infomation |
Charybdotoxin TFA is a 37-amino acid peptide with the sequence: ZFTNVSCTTSKECWSVCQRLHNTSRGKCMNKKCRCYS (where Z is pyroglutamic acid). It has three disulfide bridges. The TFA salt is typically supplied with a purity of >97% as a solid. Store at -20degC, protected from light.
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| Molecular Formula |
C176H277N57O55S7.C2HF3O2
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|---|---|
| Molecular Weight |
4409.91
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| Related CAS # |
Charybdotoxin;95751-30-7
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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) |
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.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.2268 mL | 1.1338 mL | 2.2676 mL | |
| 5 mM | 0.0454 mL | 0.2268 mL | 0.4535 mL | |
| 10 mM | 0.0227 mL | 0.1134 mL | 0.2268 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
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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