| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| Other Sizes |
| Targets |
Lappaconine targets voltage-gated sodium channels (VGSCs). By interacting with these channels, it stabilizes their inactive state, reducing the excitability of neurons and thereby inhibiting the propagation of pain signals. This mechanism is similar to that of other local anesthetics and antiarrhythmic agents. Lappaconine has also been noted for its weak hypotensive, ganglioblocking, and antiarrhythmic actions. Its primary therapeutic application has been in the field of pain management.
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| ln Vitro |
In vitro, Lappaconine has been shown to interact with voltage-gated sodium channels and produce antinociceptive effects. It is used as a research tool to study sodium channel function and pain pathways. Its activity is confirmed through electrophysiological studies on isolated neurons, where it reduces sodium currents and neuronal excitability. Detailed IC₅₀ values for sodium channel inhibition are not extensively provided in the referenced sources.
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| ln Vivo |
Detailed in vivo activity data for Lappaconine are not extensively provided in the referenced sources. However, its pharmacological properties, including analgesic and anti-inflammatory effects, have been observed in animal models. The compound has an LD₅₀ of 142–195 mg/kg (i/v, mice), indicating moderate toxicity. It also exhibits weak hypotensive and antiarrhythmic actions. Further studies are needed to fully characterize its in vivo efficacy.
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| Enzyme Assay |
Non-cell-based assays for Lappaconine 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, though these are less common.
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| Cell Assay |
Cellular assays for Lappaconine 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 are also evaluated to determine cytotoxicity.
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| Animal Protocol |
In vivo animal models for Lappaconine 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 intravenously or intraperitoneally, and its analgesic effects are measured. Its effects on cardiovascular parameters, such as blood pressure and heart rate, may also be assessed to characterize its antiarrhythmic and hypotensive actions.
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| ADME/Pharmacokinetics |
Lappaconine has a molecular weight of 423.55 g/mol and a molecular formula of C₂₃H₃₇NO₆. Its CAS number is 23943-93-3. The compound is a solid, soluble in DMSO. Purity is typically ≥98%. 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 |
Lappaconine has a relatively low toxicity profile compared to other Aconitum alkaloids, with an LD₅₀ value greater than 50 mg/kg. It has an LD₅₀ of 142–195 mg/kg (i/v, mice). As a research compound, its full safety profile would need to be established through standard preclinical toxicity assessments. The compound is intended for research use only and is not for human consumption. Standard laboratory safety precautions should be followed.
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| References | |
| Additional Infomation |
Reports indicate that (1R,2S,3S,4S,5R,6S,8S,9R,10R,13S,16S,17S)-11-ethyl-4,6,16-trimethoxy-11-azahexacyclo[7.7.2.12,5.01,10.03,8.013,17]nonadecan-3,8,13-triol has been discovered in Delphinium cashmerianum, and related data are available.
Lappaconine is a diterpenoid alkaloid and an analog of norditerpenoid alkaloids. It exhibits analgesic, anti-inflammatory, and antinociceptive effects. Its analgesic action is mediated through interaction with voltage-gated sodium channels. It also exhibits weak hypotensive, ganglioblocking, and antiarrhythmic actions. Lappaconine is used in research to study pain mechanisms and sodium channel function. Its CAS number is 23943-93-3. |
| Molecular Formula |
C23H37NO6
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|---|---|
| Molecular Weight |
423.54298
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| Exact Mass |
423.262
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| CAS # |
23943-93-3
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| PubChem CID |
44566468
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.33g/cm3
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| Boiling Point |
572.4ºC at 760 mmHg
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| Flash Point |
300ºC
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| Vapour Pressure |
1.74E-15mmHg at 25°C
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| Index of Refraction |
1.608
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| LogP |
0.192
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| Hydrogen Bond Donor Count |
3
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
30
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| Complexity |
751
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| Defined Atom Stereocenter Count |
12
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| SMILES |
O([C@H]1CC[C@@]2(O)CN(CC)C3C4[C@]5(C[C@H](OC)[C@@H]6C([H])(OC)[C@@]5(O)[C@@]([H])(C6)C13[C@]2([H])C4)O)C
|
| InChi Key |
ZBSZKFYYJKXUHF-QWRRKDOKSA-N
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| InChi Code |
InChI=1S/C23H37NO6/c1-5-24-11-20(25)7-6-17(29-3)22-15(20)9-13(18(22)24)21(26)10-14(28-2)12-8-16(22)23(21,27)19(12)30-4/h12-19,25-27H,5-11H2,1-4H3/t12-,13-,14+,15-,16+,17+,18-,19+,20-,21+,22+,23+/m1/s1
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| Chemical Name |
(1R,2S,3S,4S,5R,6S,8S,9R,10R,13S,16S,17S)-11-ethyl-4,6,16-trimethoxy-11-azahexacyclo[7.7.2.12,5.01,10.03,8.013,17]nonadecane-3,8,13-triol
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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 | 2.3611 mL | 11.8053 mL | 23.6105 mL | |
| 5 mM | 0.4722 mL | 2.3611 mL | 4.7221 mL | |
| 10 mM | 0.2361 mL | 1.1805 mL | 2.3611 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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