| 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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| Other Sizes |
| ln Vitro |
Fugilin can greatly restore the beating rhythm and boost cell viability in myocardial cells that have been damaged by sodium pentobarbital [1]. It also possesses the ability to combat this damage.
In primary cultured neonatal rat cardiomyocytes, fuziline (at concentrations of 10 μM, 1 μM and 0.1 μM) significantly increased cell viability after pentobarbital sodium‑induced damage, as measured by the MTT method. The percentage increases in cell viability were 65.44% at 10 μM, 64.14% at 1 μM, and 63.09% at 0.1 μM. Additionally, fuziline recovered the beating rhythm of the cardiomyocytes when examined under a microscope. [1] |
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| ln Vivo |
Oral fuzilin doses of 14 mg/kg, 2·4 mg/kg, and 4 mg/kg to rats resulted in average half-lives of 5.93 hours, 6.13 hours, and 5.12 hours, respectively [2].
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| Cell Assay |
Neonatal rat cardiomyocytes were cultured in 96‑well plates with DMEM medium supplemented with 15% FBS. Cultures were maintained in a 37 °C humidified incubator with 5% CO₂. On the fifth day, when the cardiomyocytes were growing with rhythmical beating, they were exposed to a medium containing pentobarbital sodium at a concentration of 8 mg/mL for 8 min. Then the medium was replaced with serum‑free medium containing fuziline at concentrations of 10 μM, 1 μM, and 0.1 μM, respectively, and incubated for 24 h. After that, 10 μL of MTT solution (5 mg/mL) was added and incubated for 4 h. Absorbance was measured at both 570 nm and 655 nm, and cell viability was evaluated from the deviations between the two measurements. [1]
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| Animal Protocol |
For the pharmacokinetic study, male Sprague‑Dawley rats (weight 250±20 g) were randomly divided into three dosage groups (n=6 per group). The animals were fasted overnight with free access to water before dosing. Fuziline was dissolved in saline and administered intragastrically at doses of 4, 2 and 1 mg/kg. Serial blood samples (0.25 mL) were collected into heparinized tubes at 0, 10, 20, 40 min and 1, 2, 3, 4, 6, 8, 10, 12, 24 h after dosing. Plasma samples were obtained by centrifugation at 1500 g for 10 min and stored at ‑80 °C until analysis. The pharmacokinetic analysis was performed using a noncompartmental approach with WinNonlin software (version 6.1). [2]
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| ADME/Pharmacokinetics |
After intragastric administration of fuziline to rats at doses of 1, 2 and 4 mg/kg, the following pharmacokinetic parameters were obtained:
- Mean half‑life (t₁/₂): 5.93±2.04 h (1 mg/kg), 6.13±2.47 h (2 mg/kg), 5.12±1.83 h (4 mg/kg). - Mean residence time (MRT): 10.73±3.28 h (1 mg/kg), 11.06±3.75 h (2 mg/kg), 9.48±2.93 h (4 mg/kg). - Maximum plasma concentration (Cₘₐₓ): 15.81±4.18 ng/mL (1 mg/kg), 42.63±10.62 ng/mL (2 mg/kg), 69.37±17.72 ng/mL (4 mg/kg). - AUC₀→₂₄ₕ: 142.74±34.95 ng·h/mL (1 mg/kg), 257.27±69.15 ng·h/mL (2 mg/kg), 442.35±163.42 ng·h/mL (4 mg/kg). - AUC₀→∞: 183.83±39.12 ng·h/mL (1 mg/kg), 320.82±58.26 ng·h/mL (2 mg/kg), 594.93±198.73 ng·h/mL (4 mg/kg). - Volume of distribution (V/F): 13920±4281.52 mL/kg (1 mg/kg), 12038±3828.72 mL/kg (2 mg/kg), 13790±4021.53 mL/kg (4 mg/kg). - Clearance (CL/F): 1529.63±782.67 mL/h/kg (1 mg/kg), 1629.26±628.28 mL/h/kg (2 mg/kg), 1538.15±892.39 mL/h/kg (4 mg/kg). The maximum plasma concentration was reached at 3–4 h after oral administration. The pharmacokinetics of fuziline in rats followed first‑order kinetics within the examined dose range (1–4 mg/kg). [2] |
| References |
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| Additional Infomation |
Fuziline is a diterpenoid alkaloid present in the lateral roots of Aconitum carmichaelii (Fuzi). Fuzi is widely used in traditional Chinese medicine for the treatment of arthralgia and heart failure. Modern pharmacological studies have revealed that Fuzi plays an important role in cardiotonic, anti‑arrhythmia, anti‑thrombosis, anti‑hypoxia, anti‑shock effects and in inhibiting thrombosis, with diterpenoid alkaloids including fuziline being among the active components. [2]
In the study by Xiong et al. (2012), fuziline (at 10, 1 and 0.1 μM) was shown to protect against pentobarbital sodium‑induced cardiomyocyte damage by recovering beating rhythm and increasing cell viability. [2] |
| Molecular Formula |
C24H39NO7
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|---|---|
| Molecular Weight |
453.5690
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| Exact Mass |
453.272
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| Elemental Analysis |
C, 63.55; H, 8.67; N, 3.09; O, 24.69
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| CAS # |
80665-72-1
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| PubChem CID |
102004854
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| Appearance |
White to off-white solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
596.9±50.0 °C at 760 mmHg
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| Melting Point |
206-207ºC
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| Flash Point |
314.8±30.1 °C
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| Vapour Pressure |
0.0±3.8 mmHg at 25°C
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| Index of Refraction |
1.617
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| LogP |
-1.32
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
32
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| Complexity |
783
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| Defined Atom Stereocenter Count |
13
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| SMILES |
O[C@H]1CC[C@]2(CN([C@H]3[C@]41[C@@H]1C[C@@H]5[C@H]([C@@H]([C@]([C@H]1[C@H]5O)(O)[C@H]3[C@@H]([C@@H]42)OC)O)OC)CC)COC
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| InChi Key |
FPECZWKKKKZPPP-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C24H39NO7/c1-5-25-9-22(10-30-2)7-6-13(26)23-12-8-11-16(27)14(12)24(29,21(28)17(11)31-3)15(20(23)25)18(32-4)19(22)23/h11-21,26-29H,5-10H2,1-4H3
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| Chemical Name |
11-ethyl-6,18-dimethoxy-13-(methoxymethyl)-11-azahexacyclo[7.7.2.12,5.01,10.03,8.013,17]nonadecane-4,7,8,16-tetrol
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| Synonyms |
Senbusine C; Fuziline
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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 Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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) |
DMSO : ~100 mg/mL (~220.47 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.51 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 25.0 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: ≥ 2.5 mg/mL (5.51 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 25.0 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: ≥ 2.5 mg/mL (5.51 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 | 2.2047 mL | 11.0237 mL | 22.0473 mL | |
| 5 mM | 0.4409 mL | 2.2047 mL | 4.4095 mL | |
| 10 mM | 0.2205 mL | 1.1024 mL | 2.2047 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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