Mesaconitine是一种生物碱,主要存在于某些毒性较强的植物如乌头(Aconitum)中,通过与钠通道结合,来增强神经信号传递,进而提高神经元的兴奋性。
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| Type | HazMat fee for 500 gram (Estimated) |
| Excepted Quantity | USD 0.00 |
| Limited Quantity | USD 15-60 |
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| Inaccessible (Haz class 6.1), International | USD 150+ |
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| 靶点 |
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| 描述 | Mesaconitine is the main active component of genus aconitum plants. |
| Concentration | Treated Time | Description | References | |
| guinea pig ventricular myocytes | 0.1, 0.3 μM | MACO depolarized the resting membrane potential (RMP) and reduced the action potential amplitude (APA) and durations (APDs) in a concentration-dependent manner, and induced DAD, EAD, and TA | Acta Pharmacol Sin. 2021 Feb;42(2):218-229 | |
| H9c2 cells | 250 µM | 24 hours | To evaluate the effect of Mesaconitine on H9c2 cell viability. The results showed that 250 µM MA significantly decreased the survival rate of H9c2 cells to 61.88±0.78%. | Evid Based Complement Alternat Med. 2022 Apr 13;2022:5731372 |
| HT22 cells | 400, 800, 1600 μM | 72 hours | To evaluate the neurotoxic effects of Mesaconitine on HT22 cells. Results showed that Mesaconitine significantly reduced cell viability, increased lactate dehydrogenase (LDH) release, induced oxidative stress, and activated autophagy pathways. | Front Pharmacol. 2024 Jun 13;15:1393717 |
| H9c2 cardiomyocytes | 300 μmol/L | 24 hours | MA significantly reduced H9c2 cell viability, resulting in diminished mitochondrial membrane potential and nuclear pyknosis and damage. | Front Pharmacol. 2024 Mar 4;15:1367682 |
| recombinant human CYP3A4 | 5, 10, 20, 40 μM | 90 minutes | To determine the kinetic parameters of Mesaconitine, results showed KM of 131.3±99.75 μM, Vmax of 0.73±0.44 nmol·mg protein−1·min−1, and in vitro intrinsic clearance rate of 0.0056 mL·nmol CYP−1·min−1. | Evid Based Complement Alternat Med. 2019 Mar 21;2019:3508658 |
| human liver microsomes (HLMs) | 20 μM | 60 minutes | To evaluate the inhibitory effect of CYP3A-specific inhibitor ketoconazole on Mesaconitine metabolism, results showed the hepatic metabolism rate of mesaconitine decreased to 21.67±19.64%. | Evid Based Complement Alternat Med. 2019 Mar 21;2019:3508658 |
| rat chondrocytes | 5, 10, 20 μg/ml | 24 hours | To evaluate the cytotoxic effects of Mesaconitine on rat chondrocytes. Results showed that Mesaconitine at concentrations of 5, 10, 20 μg/ml significantly inhibited chondrocyte viability, indicating its cytotoxicity against chondrocytes. | Front Pharmacol. 2020 Jul 24;11:1053 |
| Administration | Dosage | Frequency | Description | References | ||
| Guinea pigs | Not specified | Intravenous injection | 25 μg/kg | Single injection, recorded for 120 minutes | MACO induced various types of arrhythmias, including ventricular premature beats, atrioventricular blockade, ventricular tachycardia, and ventricular fibrillation, and was more potent than ACO | Acta Pharmacol Sin. 2021 Feb;42(2):218-229 |
| SD rats | Hepatotoxicity model | Oral | 0.8 mg/kg/day and 1.2 mg/kg/day | 6 consecutive days | To evaluate the effects of MA on the liver and its hepatotoxicity mechanism | Toxins (Basel). 2022 Jul 14;14(7):486 |
| Rats | SD rats | Oral and intravenous | 5 mg/kg orally and 0.1 mg/kg intravenously | Single dose | To study the pharmacokinetics of 10-hydroxy mesaconitine in rats, showing bioavailability of 17.6% and half-lives of 3.1±0.4h and 1.3±0.6h for oral and intravenous administration, respectively | J Anal Methods Chem. 2021 Apr 19;2021:6640184 |
| Zebrafish | Zebrafish embryos | Water bath exposure | 0 µM, 2.5 µM, 5 µM, 7.5 µM | 48 hours | Study the toxic effects of Mesaconitine on liver development and function in zebrafish embryos | Toxics. 2025 Feb 23;13(3):155 |
| Zebra fish | Zebra fish embryos | 30, 60 μM | Treatment at 1 dpf for 2 days | To evaluate the neurotoxic effects of Mesaconitine on zebra fish embryos. Results showed that Mesaconitine significantly reduced survival and hatching rates, inhibited the expression of neurodevelopment-related genes, and caused abnormal locomotor behavior. | Front Pharmacol. 2024 Jun 13;15:1393717 |
| 计算器 | ||||
| 存储液制备 | ![]() |
1mg | 5mg | 10mg |
|
1 mM 5 mM 10 mM |
1.58mL 0.32mL 0.16mL |
7.92mL 1.58mL 0.79mL |
15.83mL 3.17mL 1.58mL |
|
| CAS号 | 2752-64-9 |
| 分子式 | C33H45NO11 |
| 分子量 | 631.71 |
| SMILES Code | O(C)[C@@H]1[C@@]23[C@]4([C@](COC)(CN(C)[C@@]2([C@]([C@@H]4OC)([C@]5(OC(C)=O)[C@@]6([C@]3(C[C@@](O)([C@@H]6OC(=O)C7=CC=CC=C7)[C@@H](OC)[C@@H]5O)[H])[H])[H])[H])[C@H](O)C1)[H] |
| MDL No. | MFCD00210528 |
| 别名 | 新乌头碱;新乌碱;美沙乌头碱 |
| 运输 | 蓝冰 |
| 存储条件 |
In solvent -20°C: 3-6个月 -80°C: 12个月 Pure form Keep in dark place, sealed in dry, 2-8°C |
| 溶解方案 |
无水乙醇: 4 mg/mL(6.33 mM),配合低频超声助溶,注意:无水乙醇开封后,易挥发,也会吸收空气中的水分,导致溶解能力下降,请避免使用开封较久的乙醇 |
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