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Amiodarone hydrochloride, a benzofuran-based Class III antiarrhythmic agent, inhibits WT outwardIhERG tails with an IC50 of ∼45 nM. Amiodarone hydrochloride induces cell proliferation and myofibroblast differentiation via ERK1/2 and p38 MAPK signaling in fibroblasts. Amiodarone hydrochloride can be used in the research of both supraventricular and ventricular arrhythmias.

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Amiodarone hydrochloride Chemical Structure

Amiodarone hydrochloride Chemical Structure

CAS No. : 19774-82-4

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10 mM * 1 mL in DMSO
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Based on 9 publication(s) in Google Scholar

Other Forms of Amiodarone hydrochloride:

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Description

Amiodarone hydrochloride, a benzofuran-based Class III antiarrhythmic agent, inhibits WT outwardIhERG tails with an IC50 of ∼45 nM[1]. Amiodarone hydrochloride induces cell proliferation and myofibroblast differentiation via ERK1/2 and p38 MAPK signaling in fibroblasts[2]. Amiodarone hydrochloride can be used in the research of both supraventricular and ventricular arrhythmias[1].

In Vitro

Amiodarone blocks inward IhERG tails in a high K+ external solution ([K+]e) of 94 mM with an IC50 of 117.8 nM[1].
Amiodarone (1 μM) blocks inwardIhERG by 68.8±6.1%, with concentration response data yielding IC50 and h values of 765.5±287.8 nM and 0.9±0.4 for T623A hERG[1].
Amiodarone (1 μM) blocks inward IhERG with an IC50 and h values of 979.2±84.3 nM and 1.1±0.1 for S624A hERG[1].
Amiodarone (1-6 μg/mL) induces human embryonic lung fibroblasts (HELFs) cell proliferation and PD98059 or SB203580 suppresses this effect[2].
Amiodarone (1-6 ug/mL) does not induces HELFs cell apoptosis. Amiodarone (over 15 ug/mL) induces cell apoptosis[2].
Amiodarone (1, 3 and 6 μg/mL;24 hours) induces α-SMA and vimentin mRNA and protein expression accompanied by increased phosphorylation of ERK1/2 and p38 MAPK[2].

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

Cell Proliferation Assay[2]

Cell Line: HELFs
Concentration: 1, 3 and 6 μg/mL
Incubation Time: 24 hours
Result: Increased HELFs proliferation compared with the control group.

Western Blot Analysis[2]

Cell Line: HELFs
Concentration: 1, 3 and 6 μg/mL
Incubation Time: 24 hours
Result: α-SMA and vimentin were increased significantly in a dose-dependent manner.

RT-PCR[2]

Cell Line: HELFs
Concentration: 1, 3 and 6 μg/mL
Incubation Time: 24 hours
Result: Induced an increase of α-SMA and vimentin mRNA expression.
In Vivo

Amiodarone hydrochloride can be used in animal modeling to construct animal models of pulmonary fibrosis.

Long-term Amiodarone (90, and 180 mg/kg/day) treatment induces a dose-dependent remodeling of ion-channel expression that is correlated with the cardiac electrophysiologic effects of Amiodarone[3].

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

Animal Model: Ten-week-old male C57BL/6 mice[3]
Dosage: 30, 90, and 180 mg/kg/day
Administration: Treated orally; for 6 weeks
Result: Mice treated with 90 and 180 mg/kg/day had decreased body and heart weights, although their heart weight-to-body weight ratios were not significantly different from sham.
6-week treatment induced a decrease in plasma triiodothyronine and an increase in reverse triiodothyronine. This effect reached significance for the 90 and 180 but not for the 30 mg/kg/day dose groups.
Clinical Trial
Molecular Weight

681.77

Formula

C25H30ClI2NO3

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CCCCC1=C(C(C2=CC(I)=C(OCCN(CC)CC)C(I)=C2)=O)C3=C(O1)C=CC=C3.Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture and light

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

Solvent & Solubility
In Vitro: 

DMSO : 24.5 mg/mL (35.94 mM; Need ultrasonic and warming; 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 1.4668 mL 7.3339 mL 14.6677 mL
5 mM 0.2934 mL 1.4668 mL 2.9335 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 and light). 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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  • Dilution Calculator

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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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 (3.67 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 (3.67 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:

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(per animal)

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
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%
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 and light)

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: 99.96%

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 and light). 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 1.4668 mL 7.3339 mL 14.6677 mL 36.6693 mL
5 mM 0.2934 mL 1.4668 mL 2.9335 mL 7.3339 mL
10 mM 0.1467 mL 0.7334 mL 1.4668 mL 3.6669 mL
15 mM 0.0978 mL 0.4889 mL 0.9778 mL 2.4446 mL
20 mM 0.0733 mL 0.3667 mL 0.7334 mL 1.8335 mL
25 mM 0.0587 mL 0.2934 mL 0.5867 mL 1.4668 mL
30 mM 0.0489 mL 0.2445 mL 0.4889 mL 1.2223 mL
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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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Amiodarone hydrochloride
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