| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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| 50mg |
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| Other Sizes |
| Targets |
Ranaconitine has been shown to exhibit cardiotoxicity. Its mechanism of action is complex and involves the modulation of ion channels, particularly sodium channels, which leads to its cardiotoxic effects. It also shows analgesic and local anesthetic activities in vivo, suggesting an effect on neuronal signaling pathways.
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| ln Vitro |
In vitro studies have demonstrated that the cytotoxicity of Ranaconitine is dose-dependent. This indicates that its toxic and potentially therapeutic effects are directly related to the concentration of the compound to which cells are exposed.
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| ln Vivo |
In vivo, Ranaconitine has been shown to possess analgesic and local anesthetic activities in mice. The effective doses for these activities are reported to have an ED50 of 6.99 µmol/kg for analgesic effect and 0.167 µmol/kg for local anesthetic effect.
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| Enzyme Assay |
To assess the binding of Ranaconitine to its targets, such as voltage-gated sodium channels, a radioligand binding assay can be employed. In this cell-free system, membrane preparations from cells expressing the channel are incubated with a radiolabeled toxin or ligand that binds to the channel. The displacement of this ligand by increasing concentrations of Ranaconitine is measured to determine its binding affinity.
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| Cell Assay |
Cellular assays to study the cytotoxicity and mechanism of action of Ranaconitine are performed in various cell lines. Cells are treated with the compound, and cell viability is assessed using standard assays like MTT or by measuring the release of lactate dehydrogenase (LDH). The dose-dependent nature of its cytotoxicity is a key finding from these experiments.
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| Animal Protocol |
In vivo experiments to evaluate the analgesic and local anesthetic effects of Ranaconitine are performed in mouse models. For analgesic activity, a model like the hot plate test or the acetic acid-induced writhing test is used. The compound is administered, and the latency to response or the number of writhes is measured.
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| ADME/Pharmacokinetics |
As a diterpenoid alkaloid, Ranaconitine has specific physicochemical properties. It is soluble in DMSO. Its high toxicity is a defining characteristic.
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| Toxicity/Toxicokinetics |
Ranaconitine is highly toxic. Its in vivo cardiotoxicity is a major concern. The toxic effects are likely related to its modulation of sodium channels in cardiac tissue.
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| Additional Infomation |
S-(2-Aminoethyl)isothiourea is an iminothiocarbamate. [(1S,2S,3S,4S,5R,6S,8S,9R,13S,16S,17S)-11-ethyl-3,8,9-trihydroxy-4,6,16-trimethoxy-11-azahexacyclo[7.7.2.12,5.01,10.03,8.013,17]nonadecan-13-yl] 2-acetaminobenzoate has been reported in Aconitum sinomontanum, Aconitum septentrionale, and other organisms with relevant data.
Ranaconitine is a research compound primarily used to study the pharmacological and toxicological effects of Aconitum alkaloids. It is not an approved drug. Its use in traditional Chinese medicine is noted, but its toxicity limits its therapeutic application. It is primarily a tool for understanding the mechanisms of cardiotoxicity and neurotoxicity. |
| Molecular Formula |
C32H44N2O9
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|---|---|
| Molecular Weight |
600.6998
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| Exact Mass |
600.305
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| Elemental Analysis |
C, 63.98; H, 7.38; N, 4.66; O, 23.97
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| CAS # |
1360-76-5
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| PubChem CID |
20056254
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| Appearance |
Solid powder
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| Density |
1.39g/cm3
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| Boiling Point |
758.9ºC at 760mmHg
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| Melting Point |
132-134℃
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| Flash Point |
412.8ºC
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| Vapour Pressure |
0mmHg at 25°C
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| Index of Refraction |
1.637
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| LogP |
1.923
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
43
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| Complexity |
1170
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| Defined Atom Stereocenter Count |
11
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| SMILES |
O([H])C12C([H])([H])[C@]3([H])[C@]4(C([H])([H])C([H])([H])C([H])(C3(C1([H])N(C([H])([H])C([H])([H])[H])C4([H])[H])[C@@]1([H])C([H])([H])[C@@]3([H])[C@]([H])(C([H])([H])[C@]2([C@]1([C@@]3([H])OC([H])([H])[H])O[H])O[H])OC([H])([H])[H])OC([H])([H])[H])OC(C1=C([H])C([H])=C([H])C([H])=C1N([H])C(C([H])([H])[H])=O)=O
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| InChi Key |
XTSVKUJYTUPYRJ-HMLOAIDSSA-N
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| InChi Code |
InChI=1S/C32H44N2O9/c1-6-34-16-28(43-26(36)18-9-7-8-10-20(18)33-17(2)35)12-11-24(41-4)31-22-13-19-21(40-3)14-30(38,32(22,39)25(19)42-5)29(37,27(31)34)15-23(28)31/h7-10,19,21-25,27,37-39H,6,11-16H2,1-5H3,(H,33,35)/t19-,21+,22+,23-,24+,25+,27?,28-,29-,30+,31-,32+/m1/s1
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| Chemical Name |
[(1S,2S,3S,4S,5R,6S,8S,9R,13S,16S,17S)-11-ethyl-3,8,9-trihydroxy-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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| Synonyms |
Ranaconitine
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| HS Tariff Code |
2934.99.03.00
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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 | 1.6647 mL | 8.3236 mL | 16.6472 mL | |
| 5 mM | 0.3329 mL | 1.6647 mL | 3.3294 mL | |
| 10 mM | 0.1665 mL | 0.8324 mL | 1.6647 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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