ジソピラミド
Based on 2 publication(s) in Google Scholar
Disopyramide (Dicorantil) is a class IA antiarrhythmic agent with efficacy in ventricular and atrial arrhythmias. Disopyramide blocks the fast inward sodium current of cardiac muscle and prolongs the duration of cardiac action potentials. Disopyramide inhibits HERG encoded potassium channels. Disopyramide also exhibits complex protein binding, and has a potent negative inotropic action.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.75%
- CAS 番号: 3737-09-5
- 分子式: C21H29N3O
- 分子量:339.47
-
保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
生物活性
-
化学情報
-
溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
-
Help & FAQs
-
Membrane Transporter/Ion Channel Compound Library
HY-L011
-
FDA-Approved Drug Library
HY-L022
-
Drug Repurposing Compound Library
HY-L035
-
Anti-Cardiovascular Disease Compound Library
HY-L046
-
NMPA-Approved Drug Library
HY-L053
-
FDA Approved & Pharmacopeial Drug Library
HY-L066
-
Anti-Alzheimer's Disease Compound Library
HY-L069
-
Neuroprotective Compound Library
HY-L070
-
Neurodegenerative Disease-related Compound Library
HY-L086
-
Sodium Channel Blocker Library
HY-L118
-
Potassium Channel Compound Library
HY-L119
-
Human Metabolite Library
HY-L123
-
Heterocyclic Compound Library
HY-L138
-
Off-patent Drug Library
HY-L141
-
Membrane Protein-targeted Compound Library
HY-L149
-
Membrane Receptor-targeted Compound Library
HY-L150
-
Mitochondrial Toxicity Compound Library
HY-L155
-
Ion Channel Compound Library
HY-L166
-
Multi-Target Compound Library
HY-L176
-
Bioactive Compound Library Max
HY-L181
-
MCE Bioactive Compound Library
HY-L001V
-
Drug Repurposing Compound Library Plus
HY-L035P
-
FDA-Approved Drug Library Plus
HY-L022P
-
FDA-Approved Drug Library Mini
HY-L022M
-
Bioactive Compound Library
HY-L001
-
High-Throughput Bioactive Compound Library
HY-L205
-
Mass Spectrometry Human Metabolite Library
HY-L215
-
Cardiotoxic Compound Library
HY-L225
-
Nephrotoxicity Compound Library
HY-L229
MedChemExpress（MCE）の使用を引用している文献 Disopyramide
More
生物活性
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| CHO | IC50 |
1036.7 μM
Compound: disopyramide
|
Inhibition of Cav1.2 current measured using QPatch automatic path clamp system in CHO cells expressing Cav1.2, beta-2 and alpha-2/delta-1 subunits
Inhibition of Cav1.2 current measured using QPatch automatic path clamp system in CHO cells expressing Cav1.2, beta-2 and alpha-2/delta-1 subunits
|
[PMID: 23812503] |
| HEK293 | IC50 |
81.7 μM
Compound: disopyramide
|
Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells by confocal microscopy
Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells by confocal microscopy
|
[PMID: 18788725] |
HERG tail currents recorded at -40 mV following test pulses to +30 mV are inhibited in a dose-dependent fashion by Disopyramide concentrations within the clinical range (IC50=7.23 μM)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
-
CAS 番号 3737-09-5
-
性状 Solid
-
分子量 339.47
-
分子式 C21H29N3O
-
Color White to off-white
-
SMILES
NC(C(C1=CC=CC=C1)(C2=CC=CC=N2)CCN(C(C)C)C(C)C)=O
-
別名
Disopyramide; Dicorantil; Dicorantil
-
輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (2)
-
Journal Impact Factor
-
Most Recent
-
J Med Chem
Development of an In Silico Prediction Model for P-glycoprotein Efflux Potential in Brain Capillary Endothelial Cells toward the Prediction of Brain Penetration. [Abstract]2021 Mar 11;64(5):2725-2738. PMID: 33619967 -
Biochem Biophys Res Commun
Dual-cardiotoxicity evaluation of torsadogenic risk drugs using human iPSC-derived cardiomyocytes. [Abstract]2025 Oct 30:786:152756. PMID: 41043280
溶剤 & 溶解度
DMSO : 200 mg/mL (589.15 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
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: ≥ 5 mg/mL (14.73 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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: ≥ 5 mg/mL (14.73 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%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.
純度とドキュメンテーション
-
データシート (279 KB)
-
SDS (557 KB)
- English - EN (557 KB)
- Français - FR (557 KB)
- Deutsch - DE (557 KB)
- Norwegian - NO (557 KB)
- Español - ES (557 KB)
- Swedish - SV (557 KB)
- Italian - IT (557 KB)
- Korean - KR (557 KB)
- Portuguese - PT (557 KB)
-
取扱説明書 (2659 KB)
参考文献
[1]. S V Jones, et al. Non-competitive Effects of Disopyramide at the Neuromuscular Junction: Evidence for Endplate Ion Channel Block. Br J Anaesth. 1987 Jun;59(6):776-83. [Content Brief]
[2]. L A Siddoway, et al. Clinical Pharmacokinetics of Disopyramide. Clin Pharmacokinet. May-Jun 1986;11(3):214-22. [Content Brief]
[3]. A A Paul, et al. Inhibition of HERG Potassium Channel Current by the Class 1a Antiarrhythmic Agent Disopyramide. Biochem Biophys Res Commun. 2001 Feb 9;280(5):1243-50. [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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.9458 mL | 14.7288 mL | 29.4577 mL | 73.6442 mL |
| 5 mM | 0.5892 mL | 2.9458 mL | 5.8915 mL | 14.7288 mL | |
| 10 mM | 0.2946 mL | 1.4729 mL | 2.9458 mL | 7.3644 mL | |
| 15 mM | 0.1964 mL | 0.9819 mL | 1.9638 mL | 4.9096 mL | |
| 20 mM | 0.1473 mL | 0.7364 mL | 1.4729 mL | 3.6822 mL | |
| 25 mM | 0.1178 mL | 0.5892 mL | 1.1783 mL | 2.9458 mL | |
| 30 mM | 0.0982 mL | 0.4910 mL | 0.9819 mL | 2.4548 mL | |
| 40 mM | 0.0736 mL | 0.3682 mL | 0.7364 mL | 1.8411 mL | |
| 50 mM | 0.0589 mL | 0.2946 mL | 0.5892 mL | 1.4729 mL | |
| 60 mM | 0.0491 mL | 0.2455 mL | 0.4910 mL | 1.2274 mL | |
| 80 mM | 0.0368 mL | 0.1841 mL | 0.3682 mL | 0.9206 mL | |
| 100 mM | 0.0295 mL | 0.1473 mL | 0.2946 mL | 0.7364 mL |
Disopyramide 関連分類
HY-12533 関連分類
Powered by Bioz