1. Membrane Transporter/Ion Channel
  2. Potassium Channel
  3. Azimilide dihydrochloride

Azimilide dihydrochloride  (Synonyms: NE-10064 dihydrochloride)

Cat. No.: HY-18600A Purity: 98.91%
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Azimilide (NE-10064) dihydrochloride is a class III antiarrhythmic compound, inhibits I(Ks) and I(Kr) in guinea-pig cardiac myocytes and I(Ks) (minK) channels expressed in Xenopus oocytes.

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Azimilide dihydrochloride Chemical Structure

Azimilide dihydrochloride Chemical Structure

CAS No. : 149888-94-8

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Solid + Solvent
10 mM * 1 mL in Water
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Solid
5 mg USD 55 In-stock
10 mg USD 77 In-stock
50 mg USD 352 In-stock
100 mg USD 671 In-stock
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Customer Review

Based on 2 publication(s) in Google Scholar

Other Forms of Azimilide dihydrochloride:

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Description

Azimilide (NE-10064) dihydrochloride is a class III antiarrhythmic compound, inhibits I(Ks) and I(Kr) in guinea-pig cardiac myocytes and I(Ks) (minK) channels expressed in Xenopus oocytes. IC50 value: Target: in vitro: Azimilide dihydrochloride blocked HERG channels at 0.1 and 1 Hz with IC50s of 1.4 microM and 5.2 microM respectively. Azimilide dihydrochloride blockade of HERG channels expressed in Xenopus oocytes and I(Kr) in mouse AT-1 cells was decreased under conditions of high [K+]e, whereas block of slowly activating I(Ks) channels was not affected by changes in [K+]e [1]. Azimilide dihydrochloride suppressed the following currents (Kd in parenthesis): IKr (< 1 microM at -20 mV), IKs (1.8 microM at +30 mV), L-type Ca current (17.8 microM at +10 mV), and Na current (19 microM at -40 mV). Azimilide dihydrochloride was a weak blocker of the transient outward and inward rectifier currents (Kd > or = 50 microM at +50 and -140 mV, respectively). Azimilide dihydrochloride blocked IKr, IKs, and INa in a use-dependent manner. Furthermore, azimilide reduced a slowly inactivating component of Na current that might be important for maintaining the action potential plateau in canine ventricular myocytes [2]. In guinea pig ventricular myocytes, Azimilide (0.3-3 microM) dihydrochloride significantly prolonged action potential duration (APD) at 1 Hz. At 3 Hz, Azimilide (0.3-1 microM) dihydrochloride increased APD only slightly, and at 10 microM decreased APD and the plateau potential. Azimilide dihydrochloride potently blocked the rapidly activating component of the delayed rectifier, IKr (IC50 0.4 microM), and inhibited IKs (IC50 3 microM) with nearly 10-fold less potency [3]. in vivo: Azimilide (10 mg/kg intravenously, i.v.) dihydrochloride reduced (p < 0.05) the incidence (8 of 12) of PES-induced ventricular tachycardia (VT). The cycle length of induced VT was not prolonged by Azimilide (0.245 +/- 0.046 s predrug vs. 0.301 +/- 0.060 s postdrug) dihydrochloride. Azimilide dihydrochloride increased ventricular effective refractory period (VERP 166 +/- 5 ms predrug vs. 194 +/- 13 ms postdrug, p = 0.013), prolonged QTc interval (310 +/- 12 ms predrug vs. 350 +/- 16 ms postdrug, p = 0.004) and prolonged the effective refractory period (ERP) of noninfarcted myocardium (p = 0.045) [4].

Clinical Trial
Molecular Weight

530.88

Formula

C23H30Cl3N5O3

CAS No.
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
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.

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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
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 (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.

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Azimilide dihydrochloride Related Classifications

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    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
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