Azimilide
Based on 2 publication(s) in Google Scholar
Azimilide (NE-10064) is a class III antiarrhythmic agent, which works by blocking potassium channels in the heart. Azimilide is a dual blocker of IKs (IC50 = 2.6 μM (2mM [K⁺]ₑ)) and IKr (IC50 = 1 μM (4 mM [K⁺])). Azimilide blocked HERG channel at 0.1 and 1 Hz with IC50s of 1.4 μM and 5.2 μM respectively. Azimilide also inhibits L-type calcium current (ICa) (IC50 = 17.8 μM) and sodium current (INa) (IC50 = 19 μM). Azimilide can be used for the study of atrial fibrillation and ventricular fibrillation.
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: 99.01%
- CAS 番号: 149908-53-2
- 分子式: C23H28ClN5O3
- 分子量:457.95
-
保管条件:Powder -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]
-
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
MedChemExpress（MCE）の使用を引用している文献 Azimilide
MoreCalcium Channel アイソフォーム固有の製品をすべて表示
More
生物活性
製品説明
|
IKr 2.6 μM (IC50) |
L-type calcium channel 17.8 μM (IC50) |
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| Ventricular myocyte | IC50 |
0.18 μM
Compound: 2
|
Inhibition of ERG in guinea pig ventricular myocytes assessed as blockade of rapid delayed rectifier potassium current by whole cell patch-clamp technique
Inhibition of ERG in guinea pig ventricular myocytes assessed as blockade of rapid delayed rectifier potassium current by whole cell patch-clamp technique
|
[PMID: 19185489] |
| Ventricular myocyte | IC50 |
0.24 μM
Compound: 2
|
Inhibition of KVLQT1/minK in guinea pig ventricular myocytes assessed as blockade of slow delayed rectifier potassium current by whole cell patch-clamp technique
Inhibition of KVLQT1/minK in guinea pig ventricular myocytes assessed as blockade of slow delayed rectifier potassium current by whole cell patch-clamp technique
|
[PMID: 19185489] |
体外実験
Azimilide (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 (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.
体内実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:VT model induced by PES established in male mongrel dogs weighing 14.5-21.5 kg[4]
-
Dosage:10 mg/kg
-
Administration:Intravenous injection (i.v.), single dose
-
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.
臨床実験
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
-
CAS 番号 149908-53-2
-
性状 Solid
-
分子量 457.95
-
分子式 C23H28ClN5O3
-
Color Off-white to light brown
-
SMILES
O=C1N(CCCCN2CCN(C)CC2)C(CN1/N=C/C3=CC=C(C4=CC=C(Cl)C=C4)O3)=O
-
別名
NE-10064
-
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 6 months -20°C 1 month
Publications (2)
-
Journal Impact Factor
-
Most Recent
-
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
体外:
DMSO : 125 mg/mL (272.96 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.
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
-
データシート (274 KB)
-
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
-
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. 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 | 1 mM | 2.1836 mL | 10.9182 mL | 21.8364 mL | 54.5911 mL |
| 5 mM | 0.4367 mL | 2.1836 mL | 4.3673 mL | 10.9182 mL | |
| 10 mM | 0.2184 mL | 1.0918 mL | 2.1836 mL | 5.4591 mL | |
| 15 mM | 0.1456 mL | 0.7279 mL | 1.4558 mL | 3.6394 mL | |
| 20 mM | 0.1092 mL | 0.5459 mL | 1.0918 mL | 2.7296 mL | |
| 25 mM | 0.0873 mL | 0.4367 mL | 0.8735 mL | 2.1836 mL | |
| 30 mM | 0.0728 mL | 0.3639 mL | 0.7279 mL | 1.8197 mL | |
| 40 mM | 0.0546 mL | 0.2730 mL | 0.5459 mL | 1.3648 mL | |
| 50 mM | 0.0437 mL | 0.2184 mL | 0.4367 mL | 1.0918 mL | |
| 60 mM | 0.0364 mL | 0.1820 mL | 0.3639 mL | 0.9099 mL | |
| 80 mM | 0.0273 mL | 0.1365 mL | 0.2730 mL | 0.6824 mL | |
| 100 mM | 0.0218 mL | 0.1092 mL | 0.2184 mL | 0.5459 mL |
Azimilide 関連分類
HY-18600 関連分類
Powered by Bioz