| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| Other Sizes |
| Targets |
Lappaconitine targets voltage-gated sodium channels, specifically binding to the site-2 receptor and irreversibly blocking hH1 sodium channels. It is a selective blocker of tetrodotoxin (TTX)-sensitive Na⁺ channels without affecting the activation threshold. By blocking these channels, it reduces the excitability of neurons, which is the basis for its analgesic and antiarrhythmic effects. This mechanism is distinct from opioid analgesics, making it a non-opioid pain reliever. It also appears to influence pain pathways in the central nervous system, possibly through calcium antagonistic effects in the periaqueductal gray (PAG).
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| ln Vitro |
In vitro, Lappaconitine has been shown to block TTX-sensitive sodium channels and produce analgesic effects. It also exhibits activity in inducing differentiation and apoptosis in HL-60 cells, suggesting potential antitumor properties. Detailed IC₅₀ values for sodium channel inhibition are not extensively provided in the referenced sources. Its in vitro activity is well-established through electrophysiological studies on isolated neurons.
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| ln Vivo |
In vivo, Lappaconitine demonstrates analgesic effects. It increases the pain threshold and downregulates the expression of P2X3 receptors. Its antiarrhythmic effects have also been observed in animal models, though at higher concentrations (10⁻⁴ M) it can be arrhythmogenic. The compound is used clinically as an analgesic and antiarrhythmic agent in some countries.
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| Enzyme Assay |
Non-cell-based assays for Lappaconitine typically involve electrophysiological studies using voltage-gated sodium channels. The compound is applied to cells expressing sodium channels, and its effects on channel currents are measured using patch-clamp techniques. Binding studies can also be performed to determine its affinity for sodium channels.
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| Cell Assay |
Cellular assays for Lappaconitine are performed using neuronal cell lines or primary neurons. The cells are treated with the compound, and sodium channel activity is measured using electrophysiological or fluorescence-based techniques. The compound's ability to reduce neuronal excitability is assessed. Its effects on cell viability and apoptosis may also be evaluated in cancer cell lines.
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| Animal Protocol |
In vivo animal models for Lappaconitine include standard models of pain, such as the hot plate test, tail flick test, or formalin-induced pain model in rodents. The compound is administered orally or intraperitoneally, and its analgesic effects are measured. Its antiarrhythmic effects are assessed in models of cardiac arrhythmia, such as those induced by aconitine or other agents. Its antiepileptic effects are studied in seizure models.
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| ADME/Pharmacokinetics |
Lappaconitine has a molecular weight of 584.70 g/mol and a molecular formula of C₃₂H₄₄N₂O₈. Its CAS number is 32854-75-4. The compound is a solid. Purity is ≥96%. It is soluble in DMSO. Storage conditions: -20°C. The compound is supplied for research use only. Detailed pharmacokinetic parameters such as half-life and bioavailability are not extensively reported.
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| Toxicity/Toxicokinetics |
Lappaconitine has a well-established safety profile from its clinical use. It is considered to have low toxicity. However, at high concentrations (10⁻⁴ M), it can be arrhythmogenic. The compound is intended for research use only in the context of this request and is not for human consumption. Standard laboratory safety precautions should be followed.
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| Additional Infomation |
Lappaconitine is a diterpenoid compound.
Lappaconitine is also known as LA. It is a C19-diterpenoid alkaloid isolated from Aconitum sinomontanum Nakai. It is a centrally acting non-opioid analgesic and class-I antiarrhythmic agent. It binds to the site-2 receptor and irreversibly blocks hH1 sodium channels. It also exhibits anti-inflammatory, antiepileptic, and potential antitumor activities. Its CAS number is 32854-75-4. |
| Molecular Formula |
C32H44N2O8
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|---|---|
| Molecular Weight |
584.70
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| Exact Mass |
584.309
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| CAS # |
32854-75-4
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| PubChem CID |
441743
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
720.7±60.0 °C at 760 mmHg
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| Melting Point |
217-218ºC
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| Flash Point |
389.7±32.9 °C
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| Vapour Pressure |
0.0±2.4 mmHg at 25°C
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| Index of Refraction |
1.624
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| LogP |
2.13
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
42
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| Complexity |
1120
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| Defined Atom Stereocenter Count |
11
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| SMILES |
O([C@H]1CC[C@]2(CN([C@]3([H])[C@@]4([H])[C@]5(C[C@H](OC)[C@]6([H])[C@H](OC)[C@]5([C@@]([H])(C6)[C@@]13[C@]2([H])C4)O)O)CC)OC(C1C=CC=CC=1NC(=O)C)=O)C
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| InChi Key |
NWBWCXBPKTTZNQ-BAERZWJTSA-N
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| InChi Code |
InChI=1S/C32H44N2O8/c1-6-34-16-29(42-28(36)18-9-7-8-10-21(18)33-17(2)35)12-11-25(40-4)31-23(29)14-20(26(31)34)30(37)15-22(39-3)19-13-24(31)32(30,38)27(19)41-5/h7-10,19-20,22-27,37-38H,6,11-16H2,1-5H3,(H,33,35)/t19-,20+,22+,23-,24+,25+,26?,27+,29-,30+,31+,32+/m1/s1
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| Chemical Name |
[(1S,2S,3S,4S,5R,6S,8S,9S,13S,16S,17S)-11-ethyl-3,8-dihydroxy-4,6,16-trimethoxy-11-azahexacyclo[7.7.2.12,5.01,10.03,8.013,17]nonadecan-13-yl] 2-acetamidobenzoate
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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) |
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 | 1.7103 mL | 8.5514 mL | 17.1028 mL | |
| 5 mM | 0.3421 mL | 1.7103 mL | 3.4206 mL | |
| 10 mM | 0.1710 mL | 0.8551 mL | 1.7103 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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