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| 1mg |
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| 5mg |
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| Targets |
µ-Conotoxin KIIIA TFA targets voltage-gated sodium channels (VGSCs), specifically the Nav1.2 subtype, in mammalian neurons. As a µ-conotoxin, it blocks these channels, inhibiting sodium ion influx and neuronal excitability. This mechanism underlies its analgesic properties. Voltage-gated sodium channels are critical for action potential generation and propagation in neurons, making them important targets for pain research.
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| ln Vitro |
In vitro studies demonstrate that µ-Conotoxin KIIIA TFA is an analgesic µ-conotoxin that blocks mammalian neuronal voltage-gated sodium channels (Nav1.2). The compound is isolated from the venom of Conus kinoshitai. By blocking Nav1.2 channels, it inhibits neuronal sodium influx and reduces neuronal excitability. Detailed in vitro activity data, including IC50 values for Nav1.2 inhibition, are not extensively documented in the available literature.
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| ln Vivo |
In vivo activity of µ-Conotoxin KIIIA TFA is related to its analgesic properties as a µ-conotoxin that blocks voltage-gated sodium channels. By inhibiting neuronal sodium channels, the compound may reduce pain signaling in vivo. Detailed in vivo efficacy data from animal models of pain are not extensively documented in the available literature. The compound is intended for research use only and is not for human therapeutic applications.
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| Enzyme Assay |
The in vitro receptor binding assay for µ-Conotoxin KIIIA TFA involves measuring its inhibitory activity against voltage-gated sodium channels, specifically Nav1.2. The assay typically uses patch-clamp electrophysiology on cells expressing Nav1.2 channels. Cells are treated with the peptide at varying concentrations, and sodium currents are measured. IC50 values are determined from dose-response curves. Standard protocols include appropriate positive controls such as tetrodotoxin and vehicle controls.
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| Cell Assay |
In vitro cell-based assays for µ-Conotoxin KIIIA TFA are conducted using neuronal cell lines or primary neurons expressing Nav1.2 channels. Cells are treated with the peptide at various concentrations, and sodium channel activity is assessed using patch-clamp electrophysiology or fluorescent membrane potential assays. Neuronal excitability and action potential firing may also be evaluated. Cytotoxicity is evaluated using standard cell viability assays. Standard protocols include appropriate positive controls and vehicle controls.
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| Animal Protocol |
In vivo animal studies for µ-Conotoxin KIIIA TFA would typically be conducted using mouse or rat models of pain. Animals would be administered the peptide via intrathecal or systemic routes, and analgesic efficacy would be evaluated using behavioral tests such as tail-flick, hot plate, or formalin tests. Detailed in vivo protocols and efficacy data are not available from the search results. The compound is intended for research use only.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of µ-Conotoxin KIIIA TFA include a molecular weight of 1884.16 (free base) and formula C70H106N28O22S6·2CHF3O2. As a peptide toxin, it is subject to proteolytic degradation and may have limited oral bioavailability. Storage recommendations include powder at -80°C for 2 years or -20°C for 1 year, and in solvent at -80°C for 6 months or -20°C for 1 month. Detailed pharmacokinetic parameters are not extensively documented.
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| Toxicity/Toxicokinetics |
Toxicity information for µ-Conotoxin KIIIA TFA is limited. As a peptide toxin derived from cone snail venom, it may have significant toxicity at higher concentrations due to its sodium channel blocking activity. Standard safety precautions for handling research chemicals should be followed. The compound is designated for research use only and is not for human therapeutic applications. No detailed toxicity data are available from the search results.
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| References | |
| Additional Infomation |
µ-Conotoxin KIIIA TFA is an analgesic µ-conotoxin from Conus kinoshitai that blocks mammalian neuronal voltage-gated sodium channels (Nav1.2). It has MW 1884.16 (free base) and formula C70H106N28O22S6·2CHF3O2. It is intended for research use only.
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| Molecular Formula |
C70H106N28O22S6.XC2HF3O2
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| Molecular Weight |
1884.16 (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, avoid exposure to moisture. |
| 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 :~100 mg/mL (with sonication)
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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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