| Size | Price | |
|---|---|---|
| 1mg | ||
| Other Sizes |
Purity: ≥98%
| Targets |
Citrate-buffered Tetrodotoxin targets voltage-gated sodium channels (Na+ channels) on excitable membranes. TTX binds with high affinity to the pore-forming α-subunit of the sodium channel, specifically to site 1 on the extracellular side of the channel. This binding physically blocks the flow of sodium ions through the channel, preventing the generation and propagation of action potentials in neurons and muscle cells. The compound is a reversible and selective blocker, with different sensitivity across sodium channel isoforms.
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|---|---|
| ln Vitro |
In vitro, Tetrodotoxin is used as a standard pharmacological tool to block sodium channels in various cell types including neurons, cardiomyocytes, and skeletal muscle cells. The compound's potency is characterized by its ability to inhibit sodium currents in voltage-clamp electrophysiology experiments, with nanomolar IC50 values depending on the sodium channel isoform. TTX is also used to study the role of sodium channels in neuronal excitability, synaptic transmission, and pain signaling. The citrate-buffered formulation ensures consistent activity and solubility for these applications.
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| ln Vivo |
In vivo, Tetrodotoxin produces potent neurotoxic effects through its blockade of sodium channels, leading to paralysis and respiratory failure at high doses. At sub-lethal doses, TTX is used in research to study pain mechanisms, as it can block nociceptive signaling. The compound has been investigated for its potential therapeutic applications in pain management, including neuropathic pain and cancer pain. However, its narrow therapeutic index limits its clinical utility. The citrate-buffered formulation is used for precise dosing in animal studies.
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| Enzyme Assay |
In vitro enzyme/receptor binding assays for Tetrodotoxin typically measure its binding affinity to sodium channels using radioligand binding techniques. Radiolabeled TTX (e.g., [³H]-TTX) is used in competition binding assays with membrane preparations from tissues or cells expressing sodium channels. The compound's binding affinity (Kd) and displacement by unlabeled TTX or other sodium channel blockers are determined. Electrophysiological assays using voltage-clamp or patch-clamp techniques measure the inhibition of sodium currents in isolated cells or heterologous expression systems. These assays are the gold standard for characterizing TTX potency and selectivity.
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| Cell Assay |
In vitro cellular assays for Tetrodotoxin are performed in primary neuronal cultures or cell lines expressing voltage-gated sodium channels. Cells are treated with TTX, and sodium channel activity is assessed by measuring changes in intracellular sodium levels using sodium-sensitive dyes, or by electrophysiological recording of action potentials and sodium currents. Neuronal excitability is evaluated by measuring spontaneous or evoked firing rates. Cytotoxicity is assessed to determine safe concentrations for experimental use. The compound's effects on synaptic transmission are studied in co-culture systems or brain slice preparations.
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| Animal Protocol |
In vivo animal studies with Tetrodotoxin are conducted in rodent models to study pain mechanisms and sodium channel pharmacology. TTX is administered via various routes including intrathecal, intraperitoneal, or subcutaneous injection depending on the experimental objective. Pain models such as formalin test, hot plate test, or nerve injury models are used to evaluate analgesic effects. Neurological assessments monitor motor function and respiratory status. Dosing is critical due to the compound's narrow therapeutic index. Pharmacodynamic studies measure sodium channel blockade through electrophysiological recordings or behavioral endpoints.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of Tetrodotoxin are characterized by rapid distribution and elimination. Following administration, TTX distributes to tissues with high sodium channel expression including nerve and muscle. The compound is primarily excreted unchanged in urine. The citrate-buffered formulation enhances solubility and stability for research use. The half-life of TTX in vivo is relatively short, typically on the order of hours depending on the species and route of administration. Its bioavailability varies depending on the route, with poor oral absorption limiting its utility for oral administration.
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| Toxicity/Toxicokinetics |
Tetrodotoxin is one of the most potent neurotoxins known, with an extremely low lethal dose in humans. Toxicity results from blockade of sodium channels in nerves and muscles, leading to paralysis, respiratory failure, and death. Symptoms include numbness, tingling, weakness, and respiratory distress. There is no specific antidote; treatment is supportive. The citrate-buffered formulation is for research use only and should be handled with extreme caution. Due to its high toxicity, TTX is a regulated substance. Safety protocols including appropriate personal protective equipment and handling procedures are mandatory.
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| Additional Infomation |
Citrate-buffered Tetrodotoxin is a formulation of the potent sodium channel blocker tetrodotoxin in a citrate buffer system. It is a reversible, selective blocker of voltage-gated sodium channels, used as a pharmacological tool to study neuronal excitability, pain mechanisms, and sodium channel function. The compound is soluble in water and stable at pH 4-5. It is not approved for human use and is available only for laboratory research. Due to its extreme toxicity, strict safety precautions are required.
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| Molecular Weight |
1629.9
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|---|---|
| Exact Mass |
319.102
|
| CAS # |
4368-28-9
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| Related CAS # |
Tetrodotoxin (TTX); 4368-28-9
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| PubChem CID |
11174599
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| Appearance |
Powder
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| Melting Point |
225 °C (decomposes)
; 225 °C
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| Hydrogen Bond Donor Count |
8
|
| Rotatable Bond Count |
1
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| Heavy Atom Count |
22
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| Complexity |
561
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| Defined Atom Stereocenter Count |
9
|
| SMILES |
C([C@@]1([C@H]2[C@@H]3[C@H](N=C(N[C@@]34[C@@H]([C@@H]1O[C@]([C@H]4O)(O2)O)O)N)O)O)O
|
| InChi Key |
CFMYXEVWODSLAX-QOZOJKKESA-N
|
| InChi Code |
InChI=1S/C11H17N3O8/c12-8-13-6(17)2-4-9(19,1-15)5-3(16)10(2,14-8)7(18)11(20,21-4)22-5/h2-7,15-20H,1H2,(H3,12,13,14)/t2-,3-,4-,5+,6-,7+,9+,10-,11+/m1/s1
|
| Chemical Name |
(1R,5R,6R,7R,9S,11S,12S,13S,14S)-3-amino-14-(hydroxymethyl)-8,10-dioxa-2,4-diazatetracyclo[7.3.1.17,11.01,6]tetradec-3-ene-5,9,12,13,14-pentol
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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) |
Soluble in Water
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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 | 0.6135 mL | 3.0677 mL | 6.1353 mL | |
| 5 mM | 0.1227 mL | 0.6135 mL | 1.2271 mL | |
| 10 mM | 0.0614 mL | 0.3068 mL | 0.6135 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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