| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 25mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg | |||
| Other Sizes |
| Targets |
Yunaconitine is a C19-diterpenoid alkaloid that acts on voltage-gated sodium channels. It binds to and activates tetrodotoxin-sensitive Na+ channels and prolongs the opening of the sodium-ion channel by suppressing conformational changes. This leads to neurotoxicity and cardiotoxicity. The compound also exhibits anti-inflammatory and analgesic properties. Yunaconitine has been shown to increase serum total complement as well as the phagocytic activity of the reticuloendothelial system in mice, effects that may contribute to its anti-inflammatory actions.
|
|---|---|
| ln Vitro |
In vitro, Yunaconitine exhibits cytotoxic activity in human leukemic cells. It has been shown to have anti-inflammatory and analgesic actions in various assays. The compound's effects on voltage-gated sodium channels can be studied in electrophysiological assays using neuronal cell lines. Its in vitro activity is characterized by its ability to modulate sodium channel function and induce cytotoxicity in cancer cell lines. Yunaconitine's anti-inflammatory effects can be assessed using standard in vitro inflammation assays.
|
| ln Vivo |
In vivo, Yunaconitine has been shown to have an anti-thermic effect in pyrexial rats when administered orally at a dose of 5 μg/kg. It has anti-inflammatory and analgesic actions in animal models. Research applications include in vivo studies showing it reduces fever, inhibits granuloma formation, and suppresses vascular permeability and leukocyte migration in rodent models. Yunaconitine also increases serum total complement and phagocytic activity of the reticuloendothelial system in mice. These findings demonstrate the compound's in vivo pharmacological activities.
|
| Enzyme Assay |
In vitro enzyme/receptor binding assays for Yunaconitine typically involve studying its interaction with voltage-gated sodium channels. The compound binds to and activates tetrodotoxin-sensitive Na+ channels. Binding assays can be performed using radiolabeled ligands and membrane preparations from neuronal tissues. These assays confirm the compound's mechanism of action as a sodium channel modulator. Its effects on sodium channel function can also be assessed using electrophysiological techniques.
|
| Cell Assay |
In vitro cellular assays for Yunaconitine typically involve treating cancer cell lines, such as human leukemic cells, with the compound and measuring cell viability and cytotoxicity. The compound exhibits cytotoxic activity in these assays. Its effects on sodium channel function can also be studied in neuronal cell lines using patch-clamp electrophysiology. These cell-based studies demonstrate the compound's cytotoxic and channel-modulating activities.
|
| Animal Protocol |
In vivo animal models for Yunaconitine include the pyrexial rat model to assess its anti-thermic effect. The compound is administered orally at a dose of 5 μg/kg. Other models include inflammation models to assess its anti-inflammatory and analgesic actions. In these models, Yunaconitine reduces fever, inhibits granuloma formation, and suppresses vascular permeability and leukocyte migration. Doses and administration routes are optimized based on the specific model and experimental endpoints.
|
| ADME/Pharmacokinetics |
Yunaconitine has a molecular formula of C35H49NO11 and a molecular weight of 659.76 g/mol. It is a C19-diterpenoid alkaloid isolated from Aconitum species. The compound is typically stored under appropriate conditions to maintain stability. Its physicochemical properties support its use in pharmacological and toxicological research. Yunaconitine's solubility and formulation for administration should be optimized based on specific experimental requirements. The compound is a known phytotoxin and should be handled with caution.
|
| Toxicity/Toxicokinetics |
Yunaconitine is a highly toxic compound due to its potent effects on voltage-gated sodium channels. It causes neurotoxicity and cardiotoxicity. The compound is a phytotoxin and a human urinary metabolite. Its toxicity is well-documented from its use in traditional medicine and from poisoning cases. Yunaconitine should be handled with extreme caution in laboratory settings. Appropriate safety measures, including the use of personal protective equipment, should be employed when handling this compound. Its toxicological profile is consistent with other Aconitum alkaloids.
|
| Additional Infomation |
Unaconine has been reported in aconite (Aconitum forrestii), bufotoxin (Aconitum volubile var. pubescens), and other organisms for which data is available. See also: Unaconine (note moved to).
Yunaconitine (CAS# 70578-24-4) is a C19-diterpenoid alkaloid isolated from Aconitum species. It has anti-inflammatory and analgesic actions and has been shown to have an anti-thermic effect in pyrexial rats when administered orally at a dose of 5 μg/kg. Yunaconitine is primarily studied in toxicological and pharmacological research due to its potent effects on voltage-gated sodium channels, leading to neurotoxicity and cardiotoxicity. It exhibits cytotoxic activity in human leukemic cells. The compound is for research use only and is not approved for human therapeutic use. It should be handled with extreme caution due to its high toxicity. |
| Molecular Formula |
C35H49NO11
|
|---|---|
| Molecular Weight |
659.773
|
| Exact Mass |
659.33
|
| CAS # |
70578-24-4
|
| PubChem CID |
155569
|
| Appearance |
White to off-white solid powder
|
| Density |
1.3±0.1 g/cm3
|
| Boiling Point |
722.8±60.0 °C at 760 mmHg
|
| Melting Point |
142-144ºC
|
| Flash Point |
390.9±32.9 °C
|
| Vapour Pressure |
0.0±2.5 mmHg at 25°C
|
| Index of Refraction |
1.599
|
| LogP |
0.61
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
12
|
| Rotatable Bond Count |
12
|
| Heavy Atom Count |
47
|
| Complexity |
1230
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
CCN1C[C@@]2([C@@H](C[C@@H]([C@@]34[C@@H]2[C@H]([C@@H](C31)[C@]5(C[C@@H]([C@]6(C[C@@H]4[C@@H]5[C@H]6OC(=O)C7=CC=C(C=C7)OC)O)OC)OC(=O)C)OC)OC)O)COC
|
| InChi Key |
LLEMSCWAKNQHHA-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C35H49NO11/c1-8-36-16-32(17-41-3)22(38)13-23(43-5)35-21-14-33(40)24(44-6)15-34(47-18(2)37,26(29(35)36)27(45-7)28(32)35)25(21)30(33)46-31(39)19-9-11-20(42-4)12-10-19/h9-12,21-30,38,40H,8,13-17H2,1-7H3
|
| Chemical Name |
[8-acetyloxy-11-ethyl-5,14-dihydroxy-6,16,18-trimethoxy-13-(methoxymethyl)-11-azahexacyclo[7.7.2.12,5.01,10.03,8.013,17]nonadecan-4-yl] 4-methoxybenzoate
|
| Synonyms |
Guayewuanine B Yunaconitine
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~151.57 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (3.15 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (3.15 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (3.15 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.5157 mL | 7.5784 mL | 15.1568 mL | |
| 5 mM | 0.3031 mL | 1.5157 mL | 3.0314 mL | |
| 10 mM | 0.1516 mL | 0.7578 mL | 1.5157 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
