Aprindine
Based on 1 Customer Validation
Aprindine is an Ib-class anti-arrhythmic agent. Aprindine mainly exerts its effect by blocking sodium channels (INa), thereby reducing the excitability and conduction velocity of cardiac muscle cells. Aprindine significantly inhibits delayed potassium currents, which helps to prolong the atrial effective refractory period (AERP) and inhibit the occurrence of atrial fibrillation. Aprindine can also regulate intracellular calcium ion concentration by inhibiting Na+/Ca2+ exchange current (INCX), thereby further stabilizing cardiac electrical activity. Aprindine can be used for the study of atrial fibrillation (AF) and ventricular arrhythmias.
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- Pureté: 98.43%
- CAS No.: 37640-71-4
- Formule: C22H30N2
- Masse moléculaire:322.49
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Stockage:Pure form -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
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Cell Line
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Type | Value | Description | References |
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| HeLa | IC50 |
7.69 μM
Compound: Aprindine
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Inhibition of Ebolavirus glycoprotein/matrix protein VP40 entry in human HeLa cells after 4.5 hrs beta-lactamase reporter assay
Inhibition of Ebolavirus glycoprotein/matrix protein VP40 entry in human HeLa cells after 4.5 hrs beta-lactamase reporter assay
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[PMID: 29624387] |
Aprindine (0-128 μg/mL, 1 h-7 d) inhibits the proliferation of bone marrow cells and human lymphocytes with ED50s of 15.5 μg/mL and 8 μg/mL, and also inhibits the colony formation of normal human bone marrow CFU-C cells[1].
Aprindine (0-1000 μM) exhibits concentration-dependent inhibition on Na+/Ca2+ exchange current (INCX), and the inhibitory effects on both inward (IC50 = 51.8 μM, -100mV) and outward (IC50 = 48.8 μM, 50 mV) currents are similar, suggesting no significant voltage dependence in CCL39 cells[2].
Aprindine (0-40 μM) competes with KB-R7943 (HY-138947) and inhibits extracellular Ca2+ in CCL39 cells[2].
Aprindine (3 μM) significantly inhibits voltage-dependently rectifier K+ current (Ik), and has a slight effect on Ica and inward rectifier K+ current (Ik1) in guinea pig atrial muscle cells[3].
Aprindine (0-100 μM) inhibits the acetylcholine receptor-operated K+ current (Ik.Ach) induced by Carbachol (HY-B1208) and GTPγS (HY-137677B) with the IC50 values of 0.4 and 2.5 mM, respectively in guinea pig atrial muscle cells[3].
Aprindine (3 μM) inhibits the induction of atrial fibrillation (AF) by prolonging monophasic action potential (MAP) and effective refractory period (ERP) in isolated guinea pig heart[3].
Aprindine (0-500 μM) inhibits the calcium-binding protein-activated phosphodiesterase and Ca-ATPase activities in both isolated bovine brain tissue and human red blood cells with the IC50 values of 18 and 84 μM, respectively[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Warfarin-induced arrhythmia model in Hartley strain guinea pigs (male, 450-550 g)[5]
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Dosage:5 mg/kg
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Administration:Intravenous injection (i.v.), single dose
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Result:Increased the threshold for arrhythmia by 90% and the threshold for ventricular fibrillation by 70%.
Chemical Information
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CAS No. 37640-71-4
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Appearance Solid-Liquid Mixture
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Masse moléculaire 322.49
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Formule C22H30N2
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Color Colorless to light yellow
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SMILES
CCN(CC)CCCN(C1CC2=C(C=CC=C2)C1)C3=CC=CC=C3
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Pure form -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
DMSO : 100 mg/mL (310.09 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 7.5 mg/mL (23.26 mM); Clear solution
This protocol yields a clear solution of ≥ 7.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (75.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 7.5 mg/mL (23.26 mM); Clear solution
This protocol yields a clear solution of ≥ 7.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (75.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureté et documentation
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Fiche technique (276 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instruction de manipulation (2659 KB)
Références
[2]. Watanabe Y, et al. Inhibitory effect of aprindine on Na+/Ca2+ exchange current in guinea-pig cardiac ventricular myocytes. Br J Pharmacol. 2002 Jun;136(3):361-6. [Content Brief]
[3]. Y Ohmoto-Sekine, et al. Inhibitory effects of aprindine on the delayed rectifier K+ current and the muscarinic acetylcholine receptor-operated K+ current in guinea-pig atrial cells. Br J Pharmacol. 1999 Feb;126(3):751-61. [Content Brief]
[4]. Levine SN, Hollier B. Aprindine inhibits calmodulin-stimulated phosphodiesterase and Ca-ATPase activities. J Cardiovasc Pharmacol. 1983 Jan-Feb;5(1):151-6. [Content Brief]
[5]. Brooks RR, et al. Broad sensitivity of rodent arrhythmia models to class I, II, III, and IV antiarrhythmic agents. Proc Soc Exp Biol Med. 1989 Jun;191(2):201-9. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 3.1009 mL | 15.5044 mL | 31.0087 mL | 77.5218 mL |
| 5 mM | 0.6202 mL | 3.1009 mL | 6.2017 mL | 15.5044 mL | |
| 10 mM | 0.3101 mL | 1.5504 mL | 3.1009 mL | 7.7522 mL | |
| 15 mM | 0.2067 mL | 1.0336 mL | 2.0672 mL | 5.1681 mL | |
| 20 mM | 0.1550 mL | 0.7752 mL | 1.5504 mL | 3.8761 mL | |
| 25 mM | 0.1240 mL | 0.6202 mL | 1.2403 mL | 3.1009 mL | |
| 30 mM | 0.1034 mL | 0.5168 mL | 1.0336 mL | 2.5841 mL | |
| 40 mM | 0.0775 mL | 0.3876 mL | 0.7752 mL | 1.9380 mL | |
| 50 mM | 0.0620 mL | 0.3101 mL | 0.6202 mL | 1.5504 mL | |
| 60 mM | 0.0517 mL | 0.2584 mL | 0.5168 mL | 1.2920 mL | |
| 80 mM | 0.0388 mL | 0.1938 mL | 0.3876 mL | 0.9690 mL | |
| 100 mM | 0.0310 mL | 0.1550 mL | 0.3101 mL | 0.7752 mL |
Aprindine Related Classifications
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