2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. Potassium Channel Calcium Channel Sodium Channel
  4. Azimilide

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.

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Azimilide

Azimilide Chemical Structure

CAS No. : 149908-53-2

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Based on 2 publication(s) in Google Scholar

Other Forms of Azimilide:

Azimilide Related Antibodies

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  • Purity & Documentation

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  • Customer Review

Description

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[1][2][3][4].

IC50 & Target[1][3]

IKr

2.6 μM (IC50)

L-type calcium channel

17.8 μM (IC50)

In Vitro

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.

Azimilide Related Antibodies
In Vivo

Azimilide (10 mg/kg, i.v., single dose) significantly reduces the occurrence of ventricular tachycardia (VT) induced by electrical stimulation (PES) in dogs[4].

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.
Clinical Trial
Molecular Weight

457.95

Formula

C23H28ClN5O3
CAS No.
Appearance

Solid

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1836 mL 10.9182 mL 21.8364 mL
5 mM 0.4367 mL 2.1836 mL 4.3673 mL
View the 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.

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This equation is commonly abbreviated as: C1V1 = C2V2

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Working solution concentration: mg/mL
Purity & Documentation
References

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
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Azimilide Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Azimilide149908-53-2NE-10064NE10064NE 10064Potassium ChannelCalcium ChannelSodium ChannelKcsACa2+ channelsCa channelsNa channelsNa+ channelsElectrophysiologyIonWorks HTIhHyperpolarization-activatedPatch-clampZD7288Inhibitorinhibitorinhibit

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