Azimilide dihydrochloride (Synonyms: NE-10064 dihydrochloride)

Name: Azimilide dihydrochloride
Brand: MedChemExpress
SKU: HY-18600A
Rating: 5.0 (2 reviews)

Cat. No.: HY-18600A Purity: 98.17%: Data Sheet
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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 I_Ks (IC₅₀ = 2.6 μM (2mM [K⁺]ₑ)) and I_Kr (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 (I_Ca) (IC₅₀ = 17.8 μM) and sodium current (I_Na) (IC₅₀ = 19 μM). Azimilide dihydrochloride can be used for the study of atrial fibrillation and ventricular fibrillation.

For research use only. We do not sell to patients.

Azimilide dihydrochloride Chemical Structure

CAS No. : 149888-94-8

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in Water ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in Water	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	Get quote
100 mg	Get quote

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Customer Review

Based on 2 publication(s) in Google Scholar

Other Forms of Azimilide dihydrochloride:

2 Publications Citing Use of MCE Azimilide dihydrochloride

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View All Calcium Channel Isoform Specific Products:

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N-type calcium channel L-type calcium channel P/Q-type calcium channel T-type calcium channel Calcium Channel

View All Sodium Channel Isoform Specific Products:

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Na_v1.1 Na_v1.2 Na_v1.3 Na_v1.4 Na_v1.5 Na_v1.6 Na_v1.7 Na_v1.8 Na_v1.9

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]^[3]

IKr

2.6 μM (IC₅₀)

L-type calcium channel

17.8 μM (IC₅₀)

In Vitro

Azimilide dihydrochloride (0.1-100 μM) blocks I_Kr (reversibly dependent, affected by [K⁺]ₑ) and I_Ks 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.

In Vivo

Azimilide dihydrochloride (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

530.88

Formula

C₂₃H₃₀Cl₃N₅O₃

CAS No.

149888-94-8

Appearance

Solid

Color

Light yellow to yellow

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.8837 mL	9.4183 mL	18.8366 mL
5 mM	0.3767 mL	1.8837 mL	3.7673 mL
10 mM	0.1884 mL	0.9418 mL	1.8837 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 (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.

Molarity Calculator
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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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Concentration _(final)

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In Vivo Dissolution Calculator

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.

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Working solution concentration: mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).

Purity & Documentation

Purity: 98.17%

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Data Sheet (275 KB) SDS (479 KB)

COA (248 KB) HNMR (272 KB) LCMS (93 KB)

Handling Instructions (2659 KB)

References

[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

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 Related Classifications

Cardiovascular Disease

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.

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Azimilide dihydrochloride (Synonyms: NE-10064 dihydrochloride)

Customer Review

Other Forms of Azimilide dihydrochloride:

Azimilide dihydrochloride Related Antibodies

2 Publications Citing Use of MCE Azimilide dihydrochloride

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Calcium Channel Isoform Specific Products:

View All Sodium Channel Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

Azimilide dihydrochloride Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Azimilide dihydrochloride Related Classifications

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Customer Review

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