| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg | |||
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| Targets |
Calcium Channel
Mesaconitine targets voltage-gated sodium channels. It binds to the neurotoxin site 2 on the α-subunit of the sodium channel and prevents channel inactivation, leading to persistent activation of the channel. This results in increased sodium influx, depolarization, and repetitive firing of neurons and cardiac myocytes. It also affects other ion channels and receptors. |
|---|---|
| ln Vitro |
In vitro, mesaconitine has been shown to activate voltage-gated sodium channels in neuronal and cardiac cell lines. It increases sodium current and causes cell depolarization. It can also induce apoptosis and cell death at higher concentrations. It has analgesic effects in some in vitro models.
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| ln Vivo |
In vivo, mesaconitine is highly toxic. It causes cardiovascular effects including arrhythmias, hypotension, and cardiac arrest. It also causes neurological effects including paresthesia, muscle weakness, and respiratory paralysis. It has been used in traditional medicine for its analgesic and anti-inflammatory effects, but its use is risky.
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| Enzyme Assay |
For non-cellular enzyme/receptor binding assays, mesaconitine can be tested for binding to voltage-gated sodium channels using radioligand binding assays. The effect on sodium channel function can be assessed using electrophysiological techniques in isolated membranes or oocytes expressing sodium channels.
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| Cell Assay |
For in vitro cell-based assays, neuronal and cardiac cell lines are cultured and treated with mesaconitine. Sodium current is measured using patch-clamp electrophysiology. Cell viability, apoptosis, and signaling pathway activation can be assessed.
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| Animal Protocol |
For in vivo animal studies, mesaconitine can be administered to animal models. Cardiovascular and neurological effects are monitored. Analgesic effects can be assessed using pain models. Toxicity and lethal dose are determined.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties include solubility in DMSO and ethanol. It is a lipophilic alkaloid and is absorbed after oral administration. It is metabolized in the liver and excreted. It has a narrow therapeutic window. Storage is typically at -20°C. It is a solid and should be handled with extreme caution due to its high toxicity.
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| Toxicity/Toxicokinetics |
Toxicological data for mesaconitine is well-established. It is highly toxic, with a lethal dose of a few milligrams in humans. Symptoms include nausea, vomiting, paresthesia, muscle weakness, cardiac arrhythmias, and respiratory paralysis. It is not for human use. Extreme caution should be exercised when handling.
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| References |
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| Additional Infomation |
Mesoaconitine is a diterpenoid compound. It has been reported to exist in Aconitum carmichaelii, Aconitum floribunda, and other organisms with relevant data. See also: Mesoaconitine (note moved to).
Mesaconitine is a highly toxic diterpenoid alkaloid from Aconitum plants. It targets voltage-gated sodium channels and prevents channel inactivation. It causes cardiovascular and neurological toxicity. It has been used in traditional medicine for its analgesic effects, but its use is limited by its high toxicity. |
| Molecular Formula |
C33H45NO11
|
|---|---|
| Molecular Weight |
631.7105
|
| Exact Mass |
631.299
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| Elemental Analysis |
C, 62.74; H, 7.18; N, 2.22; O, 27.86
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| CAS # |
2752-64-9
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| Related CAS # |
2752-64-9
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| PubChem CID |
441747
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| Appearance |
White to off-white solid powder
|
| Density |
1.4±0.1 g/cm3
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| Boiling Point |
695.0±55.0 °C at 760 mmHg
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| Flash Point |
374.1±31.5 °C
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| Vapour Pressure |
0.0±2.3 mmHg at 25°C
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| Index of Refraction |
1.618
|
| LogP |
0.27
|
| Hydrogen Bond Donor Count |
3
|
| Hydrogen Bond Acceptor Count |
12
|
| Rotatable Bond Count |
10
|
| Heavy Atom Count |
45
|
| Complexity |
1200
|
| Defined Atom Stereocenter Count |
14
|
| SMILES |
O(C(C([H])([H])[H])=O)[C@]12[C@]([H])([C@@]([H])([C@@]3([C@@]([H])([C@@]1([H])[C@@]([H])(C3([H])[H])[C@@]13[C@]([H])(C([H])([H])[C@]([H])([C@]4(C([H])([H])OC([H])([H])[H])C([H])([H])N(C([H])([H])[H])C1([H])[C@]2([H])[C@@]([H])([C@@]34[H])OC([H])([H])[H])O[H])OC([H])([H])[H])OC(C1C([H])=C([H])C([H])=C([H])C=1[H])=O)O[H])OC([H])([H])[H])O[H]
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| InChi Key |
XUHJBXVYNBQQBD-TUWOXVOMSA-N
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| InChi Code |
InChI=1S/C33H45NO11/c1-16(35)45-33-21-18(13-31(39,28(43-6)26(33)37)27(21)44-29(38)17-10-8-7-9-11-17)32-20(41-4)12-19(36)30(15-40-3)14-34(2)25(32)22(33)23(42-5)24(30)32/h7-11,18-28,36-37,39H,12-15H2,1-6H3/t18-,19-,20+,21-,22+,23+,24-,25?,26+,27-,28+,30+,31-,32+,33-/m1/s1
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| Chemical Name |
[(1S,2R,3R,4R,5R,6S,7S,8R,9R,13R,14R,16S,17S,18R)-8-acetyloxy-5,7,14-trihydroxy-6,16,18-trimethoxy-13-(methoxymethyl)-11-methyl-11-azahexacyclo[7.7.2.12,5.01,10.03,8.013,17]nonadecan-4-yl] benzoate
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| Synonyms |
NSC 77210; NSC-77210;NSC77210; Mesaconitine
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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) |
Ethanol: ~4.6 mg/mL (~7.3 mM)
H2O: <0.1 mg/mL DMSO: <1 mg/mL |
|---|---|
| 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 | 1.5830 mL | 7.9150 mL | 15.8300 mL | |
| 5 mM | 0.3166 mL | 1.5830 mL | 3.1660 mL | |
| 10 mM | 0.1583 mL | 0.7915 mL | 1.5830 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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