1. Membrane Transporter/Ion Channel
  2. Sodium Channel Potassium Channel
  3. Eleclazine hydrochloride

Eleclazine hydrochloride  (Synonyms: GS 6615 hydrochloride)

Cat. No.: HY-16738A Purity: 99.62%
COA Handling Instructions

Eleclazine (GS 6615) hydrochloride is a selective cardiac late sodium current inhibitor and a weak inhibitor of potassium current with IC50 value of <1 μM and approximately 14.2 μM, respectively. Eleclazine hydrochloride shows concurrent protection against autonomically induced atrial premature beats, repolarization alternans and heterogeneity, and atrial fibrillation in porcine model. Eleclazine hydrochloride can be used to research cardiac arrhythmias.

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

Eleclazine hydrochloride Chemical Structure

Eleclazine hydrochloride Chemical Structure

CAS No. : 1448754-43-5

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 330 In-stock
Solution
10 mM * 1 mL in DMSO USD 330 In-stock
Solid
1 mg USD 142 In-stock
5 mg USD 300 In-stock
10 mg USD 450 In-stock
50 mg USD 1350 In-stock
100 mg USD 2150 In-stock
200 mg   Get quote  
500 mg   Get quote  

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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Eleclazine hydrochloride

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Eleclazine (GS 6615) hydrochloride is a selective cardiac late sodium current inhibitor and a weak inhibitor of potassium current with IC50 value of <1 μM and approximately 14.2 μM, respectively. Eleclazine hydrochloride shows concurrent protection against autonomically induced atrial premature beats, repolarization alternans and heterogeneity, and atrial fibrillation in porcine model. Eleclazine hydrochloride can be used to research cardiac arrhythmias[1][2][3].

IC50 & Target

Sodium current, Potassium current[1][2]

In Vitro

Eleclazine inhibits sodium current in hiPSC-derived cardiomyocytes with an IC50 of 2.5 μM[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Eleclazine (0.3 and 0.9 mg/kg; IV; infused over 15 minutes) reduces the incidence of epinephrine-induced ventricular premature beats and couplets, and shortens ventricular QT and atrial PTa intervals[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male Yorkshire pigs (35.20 ± 0.46 kg; injected with epinephrine via a jugular vein)[1]
Dosage: 0.3 and 0.9 mg/kg
Administration: IV; infused over 15 minutes
Result: Reduced the incidence of epinephrine-induced ventricular premature beats and couplets by 51% (from 31.3 ± 1.91 to 15.2 ± 5.08 episodes; P = 0.038) and the incidence of 3- to 7-beat ventricular tachycardia (VT) by 56% (from 10.8 ± 3.45 to 4.7 ± 3.12 episodes; P = 0.004).
Shortened ventricular QT and atrial PTa intervals by 7%, and reduced atrial repolarization alternans and heterogeneity without attenuation of the inotropic response to catecholamine.
Clinical Trial
Molecular Weight

451.83

Formula

C21H17ClF3N3O3

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C1N(CC2=NC=CC=N2)CCOC3=CC=C(C4=CC=C(OC(F)(F)F)C=C4)C=C13.[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: 

DMSO : 50 mg/mL (110.66 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2132 mL 11.0661 mL 22.1322 mL
5 mM 0.4426 mL 2.2132 mL 4.4264 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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (5.53 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (5.53 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

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

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).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.62%

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 1 mM 2.2132 mL 11.0661 mL 22.1322 mL 55.3305 mL
5 mM 0.4426 mL 2.2132 mL 4.4264 mL 11.0661 mL
10 mM 0.2213 mL 1.1066 mL 2.2132 mL 5.5331 mL
15 mM 0.1475 mL 0.7377 mL 1.4755 mL 3.6887 mL
20 mM 0.1107 mL 0.5533 mL 1.1066 mL 2.7665 mL
25 mM 0.0885 mL 0.4426 mL 0.8853 mL 2.2132 mL
30 mM 0.0738 mL 0.3689 mL 0.7377 mL 1.8444 mL
40 mM 0.0553 mL 0.2767 mL 0.5533 mL 1.3833 mL
50 mM 0.0443 mL 0.2213 mL 0.4426 mL 1.1066 mL
60 mM 0.0369 mL 0.1844 mL 0.3689 mL 0.9222 mL
80 mM 0.0277 mL 0.1383 mL 0.2767 mL 0.6916 mL
100 mM 0.0221 mL 0.1107 mL 0.2213 mL 0.5533 mL
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Eleclazine hydrochloride 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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Eleclazine hydrochloride
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