Azimilide dihydrochloride
Based on 2 publication(s) in Google Scholar
Azimilide (NE-10064) dihydrochloride is a class III antiarrhythmic agent, which works by blocking potassium channels in the heart. Azimilide dihydrochloride is a dual blocker of IKs (IC50 = 2.6 μM (2mM [K⁺]ₑ)) and IKr (IC50 = 1 μM (4 mM [K⁺])). Azimilide dihydrochloride blocked HERG channel at 0.1 and 1 Hz with IC50s of 1.4 μM and 5.2 μM respectively. Azimilide dihydrochloride also inhibits L-type calcium current (ICa) (IC50 = 17.8 μM) and sodium current (INa) (IC50 = 19 μM). Azimilide dihydrochloride can be used for the study of atrial fibrillation and ventricular fibrillation.
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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: 98.17%
- CAS 番号: 149888-94-8
- 分子式: C23H30Cl3N5O3
- 分子量:530.88
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保管条件:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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MedChemExpress（MCE）の使用を引用している文献 Azimilide dihydrochloride
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生物活性
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IKr 2.6 μM (IC50) |
L-type calcium channel 17.8 μM (IC50) |
Azimilide dihydrochloride (0.1-100 μM) blocks IKr (reversibly dependent, affected by [K⁺]ₑ) and IKs channels (dependently on use, unaffected by [K⁺]ₑ) in mouse AT-1 cells and African clawed frog oocytes[1].
Azimilide dihydrochloride (0.3-5 μM) shortens the action potential duration (APD) of canine and guinea pig ventricular muscle cells[2][3].
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:VT model induced by PES established in male mongrel dogs weighing 14.5-21.5 kg[4]
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Dosage:10 mg/kg
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Administration:Intravenous injection (i.v.), single dose
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Result:Significantly reduced the incidence of VT induced by PES.
Prolonged the effective refractory period of the ventricle and the QTc interval, but does not affect the conduction parameters.
Provided significant protection against ischemia-induced ventricular fibrillation and improves survival rates.
化学情報
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CAS 番号 149888-94-8
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性状 Solid
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分子量 530.88
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分子式 C23H30Cl3N5O3
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Color Light yellow to yellow
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SMILES
O=C1N(CCCCN2CCN(C)CC2)C(CN1/N=C/C3=CC=C(C4=CC=C(Cl)C=C4)O3)=O.[H]Cl.[H]Cl
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別名
NE-10064 dihydrochloride
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (2)
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Journal Impact Factor
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Most Recent
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Biochem Biophys Res Commun
Inflammatory mediator bradykinin increases population of sensory neurons expressing functional T-type Ca(2+) channels. [Abstract]2016 Apr 29;473(2):396-402. PMID: 26944020 -
Exp Ther Med
Establishment and validation of a torsade de pointes prediction model based on human iPSC‑derived cardiomyocytes. [Abstract]2022 Dec 9;25(1):61. PMID: 36588805
溶剤 & 溶解度
H2O : 50 mg/mL (94.18 mM; Need ultrasonic)
DMSO : 2 mg/mL (3.77 mM; ultrasonic and warming and heat to 60°C; 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (275 KB)
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SDS (479 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Busch AE, et al. Blockade of HERG channels by the class III antiarrhythmic azimilide: mode of action. Br J Pharmacol. 1998 Jan;123(1):23-30. [Content Brief]
[2]. Yao JA, et al. Azimilide (NE-10064) can prolong or shorten the action potential duration in canine ventricular myocytes: dependence on blockade of K, Ca, and Na channels. J Cardiovasc Electrophysiol. 1997 Feb;8(2):184-98. [Content Brief]
[3]. Fermini B, et al. Use-dependent effects of the class III antiarrhythmic agent NE-10064 (azimilide) on cardiac repolarization: block of delayed rectifier potassium and L-type calcium currents. J Cardiovasc Pharmacol. 1995 Aug;26(2):259-71. [Content Brief]
[4]. Black SC, et al. Protection against programmed electrical stimulation-induced ventricular tachycardia and sudden cardiac death by NE-10064, a class III antiarrhythmic drug. J Cardiovasc Pharmacol. 1993 Dec;22(6):810-8. [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 (sealed storage, away from moisture). 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 |
|---|---|---|---|---|---|
| DMSO / H2O | 1 mM | 1.8837 mL | 9.4183 mL | 18.8366 mL | 47.0916 mL |
| H2O | 5 mM | 0.3767 mL | 1.8837 mL | 3.7673 mL | 9.4183 mL |
| 10 mM | 0.1884 mL | 0.9418 mL | 1.8837 mL | 4.7092 mL | |
| 15 mM | 0.1256 mL | 0.6279 mL | 1.2558 mL | 3.1394 mL | |
| 20 mM | 0.0942 mL | 0.4709 mL | 0.9418 mL | 2.3546 mL | |
| 25 mM | 0.0753 mL | 0.3767 mL | 0.7535 mL | 1.8837 mL | |
| 30 mM | 0.0628 mL | 0.3139 mL | 0.6279 mL | 1.5697 mL | |
| 40 mM | 0.0471 mL | 0.2355 mL | 0.4709 mL | 1.1773 mL | |
| 50 mM | 0.0377 mL | 0.1884 mL | 0.3767 mL | 0.9418 mL | |
| 60 mM | 0.0314 mL | 0.1570 mL | 0.3139 mL | 0.7849 mL | |
| 80 mM | 0.0235 mL | 0.1177 mL | 0.2355 mL | 0.5886 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Azimilide dihydrochloride 関連分類
HY-18600A 関連分類
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