| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| Targets |
Voltage-dependent K⁺ channel (KV1.3) (IC50: 1.2 nM in cell-free assays) [1]
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|---|---|
| ln Vitro |
- KV1.3 channel inhibition: Agitoxin-2 potently blocks KV1.3 channels in cell-free assays with an IC50 of 1.2 nM. It shows high selectivity for KV1.3 over other K⁺ channel subtypes (e.g., KV1.1, KV1.2) [1].
- Recombinant expression and functional validation: In Pichia pastoris, Agitoxin-2 was recombinantly expressed and purified. Electrophysiological assays confirmed its ability to inhibit KV1.3 channels with similar potency to native toxin [2]. |
| Enzyme Assay |
KV1.3 channel activity assay: Xenopus oocytes expressing KV1.3 channels were voltage-clamped using the two-electrode voltage-clamp technique. Agitoxin-2 (0.1–100 nM) was applied to the bath solution, and K⁺ currents were recorded. IC50 was determined by fitting dose-response curves [1].
|
| Cell Assay |
KV1.3-mediated current inhibition: HEK293 cells transfected with KV1.3 cDNA were patch-clamped in the whole-cell configuration. Agitoxin-2 (0.1–100 nM) was perfused, and K⁺ currents were measured. Inhibition kinetics and potency were analyzed [1].
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| References |
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| Additional Infomation |
Mechanism of action: Agitoxin-2 acts as a pore-blocking inhibitor of KV1.3 channels, binding to the outer vestibule to prevent the outflow of K⁺ ions [1]. Production method: Recombinant Agitoxin-2 expressed in Pichia pastoris provides a scalable and cost-effective alternative for venom extraction [2].
|
| Molecular Formula |
C171H279F3N54O50S8
|
|---|---|
| Molecular Weight |
4090.877 (free acid)
|
| Related CAS # |
Agitoxin-2;168147-41-9
|
| SequenceShortening |
GVPINVSCTGSPQCIKPCKDAGMRFGKCMNRKCHCTPK (Disulfide bridge:Cys8-Cys28;Cys14-Cys33;Cys18-Cys35)
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| Appearance |
Typically exists as solid at room temperature
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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)
|
| 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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