| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
Sodium Channel (NaV)
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|---|---|
| ln Vitro |
Taplucainium chloride is a sodium channel blocker. It exhibits 70-95% inhibition at 10 uM in vitro. It is a quaternary ammonium compound (azepinium derivative) that likely acts as a state-dependent blocker of sodium channels. Its primary applications are in analgesia and neurophysiology research to study peripheral nerve conduction, local anesthetic mechanisms, and ion channel pharmacology. No specific IC50 is reported.
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| ln Vivo |
Taplucainium chloride is reported to have applications as an analgesic (pain reliever). Based on its in vitro activity as a sodium channel blocker, it would be expected to have in vivo analgesic efficacy in animal models of pain, such as the formalin test, CFA-induced hyperalgesia, or nerve injury models. The compound is classified as an analgesic.
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| Enzyme Assay |
Recombinant human sodium channel isoforms (e.g., NaV1.7, NaV1.8) are expressed in HEK293 cells. Whole-cell patch-clamp recordings are performed to measure sodium currents. Cells are held at a depolarized potential (e.g., -60 mV) to mimic inactivated channel states. Taplucainium chloride is applied at varying concentrations (0.1-100 uM), and current inhibition is measured. The % inhibition at 10 uM (70-95%) is reported; IC50 values can be calculated from the dose-response data. For radioligand binding, [3H]saxitoxin is used.
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| Cell Assay |
HEK293 cells expressing human NaV1.7 channels are cultured in DMEM with 10% FBS and antibiotics. Cells are plated on coverslips and whole-cell patch-clamp electrophysiology is performed at room temperature. The internal pipette solution contains CsF, CsCl, and EGTA. The external solution contains NaCl, KCl, CaCl2, MgCl2, HEPES, and glucose. Currents are elicited by depolarizing pulses from a holding potential of -120 mV to a test potential of -10 mV, with a 500 ms prepulse to -60 mV to induce inactivation. Taplucainium chloride is applied (0.1-100 uM) and the inhibition is measured.
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| Animal Protocol |
No published in vivo animal study data available. A typical protocol for assessing analgesic efficacy would involve administering Taplucainium chloride (e.g., 1-30 mg/kg) via intraperitoneal injection or oral gavage to male Sprague-Dawley rats or ICR mice. Pain models would include the formalin-induced paw licking test (50 uL of 2% formalin injected into the hind paw; time spent licking/injured paw is scored for 60 min), or the CFA-induced thermal hyperalgesia model (Hargreaves test). Behavioral responses are measured for 60-180 min post-administration.
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| ADME/Pharmacokinetics |
No specific PK data for Taplucainium chloride. As a quaternary ammonium compound, it is charged and likely has poor oral bioavailability due to low gastrointestinal absorption. It may not cross the blood-brain barrier, making it a peripherally restricted sodium channel blocker (which could be advantageous for peripheral pain with minimal CNS side effects). It is likely administered intravenously or locally for research applications.
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| Toxicity/Toxicokinetics |
No specific toxicity data for Taplucainium chloride. As a sodium channel blocker, potential on-target toxicities include CNS effects (if it crosses BBB) such as dizziness, sedation, and ataxia, as well as cardiovascular effects (QT prolongation, arrhythmias) due to cardiac NaV channel block. The compound is reported to display 70-95% inhibition at 10 uM, so a therapeutic window exists. For research use, handle with standard precautions.
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| References |
[1]. WHO Drug Informat ion - World Health Organization (WHO).
[2]. Cole BM, et al. Preparation of ammonium salts as charged ion channel blockers and methods for use: World Intellectual Property Organization, WO2020185830. 2020-09-17. [3]. WHO Drug Information-World Health Organization (WHO). |
| Additional Infomation |
Taplucainium chloride (INN name: Taplucainium chloride) is a sodium channel blocker in development for analgesic indications. The compound is a quaternary azepinium derivative. It is listed as a small-molecule drug in clinical or preclinical research. As an INN (International Nonproprietary Name) listed compound, it has been assigned a unique ingredient identifier (UNII: E69A9Y8Z4L). Molecular formula: C23H31ClN2O, MW 386.96. Not approved for clinical use. Reference: WHO INN List.
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| Molecular Formula |
C23H31CLN2O
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|---|---|
| Molecular Weight |
386.958045244217
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| Exact Mass |
386.212
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| CAS # |
2489565-37-7
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| PubChem CID |
166642641
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| Appearance |
Off-white to light yellow solid powder
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
27
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| Complexity |
426
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| Defined Atom Stereocenter Count |
0
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| SMILES |
[Cl-].O=C(C[N+]1(CC2C=CC=CC=2)CCCCCC1)NC1C(C)=CC=CC=1C
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| InChi Key |
LKGJDWZDLANXSQ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C23H30N2O.ClH/c1-19-11-10-12-20(2)23(19)24-22(26)18-25(15-8-3-4-9-16-25)17-21-13-6-5-7-14-21;/h5-7,10-14H,3-4,8-9,15-18H2,1-2H3;1H
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| Chemical Name |
2-(1-benzylazepan-1-ium-1-yl)-N-(2,6-dimethylphenyl)acetamide;chloride
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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) |
DMSO: 10 mg/mL (25.84 mM)
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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 | 2.5842 mL | 12.9212 mL | 25.8425 mL | |
| 5 mM | 0.5168 mL | 2.5842 mL | 5.1685 mL | |
| 10 mM | 0.2584 mL | 1.2921 mL | 2.5842 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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