Art. -Nr.: HY-14188

Amiodarone hydrochloride

13 Cited Publications

Kundenbewertung

Based on 13 publication(s) in Google Scholar

Amiodarone hydrochloride, a benzofuran-based Class III antiarrhythmic agent, inhibits WT outward ionic current (IhERG) 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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Reinheit: 99.76%
CAS. Nr.: 19774-82-4
Formel: C₂₅H₃₀ClI₂NO₃
Molecular Weight:681.77

Speicherung:

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)

Amiodarone hydrochloride Chemical Structure

CAS. Nr.: 19774-82-4

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Biologische Aktivität
- Beschreibung
- In Vitro
- In Vivo
- Induced Disease Models
- Clinical Trial
Chemical Information
Publications (13)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Bioz

Biologische Aktivität

Beschreibung

Amiodarone hydrochloride, a benzofuran-based Class III antiarrhythmic agent, inhibits WT outward ionic current (IhERG) 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 hydrochloride 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) hydrochloride blocks inward IhERG by 68.8%, with concentration response data yielding IC₅₀ and h values of 765.5 nM and 0.9 for T623A hERG^[1].
Amiodarone (1 μM) hydrochloride blocks inward IhERG with an IC₅₀ and h values of 979.2 nM and 1.1 for S624A hERG^[1].
Amiodarone (1-6 μg/mL) hydrochloride induces human embryonic lung fibroblasts (HELFs) cell proliferation and PD98059 or SB203580 suppresses this effect^[2].
Amiodarone (1-6 μg/mL) hydrochloride does not induces HELFs cell apoptosis. Amiodarone (over 15 μg/mL) hydrochloride induces cell apoptosis^[2].
Amiodarone (1, 3 and 6 μg/mL;24 hours) hydrochloride 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

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.

Induced Disease Models

Note:
Please do not refer to only one article to determine the experimental conditions. It is recommended to determine the optimal experimental conditions (animal strain, age, dosage, frequency and cycle, detection time and indicators, etc.) through preliminary experiments before the formal experiment.

Amiodarone can be used to create pulmonary fibrosis models. Amiodarone has a large distribution volume and extensive tissue distribution, resulting in a terminal half-life in human plasma of up to 25 days. The major active metabolite of Amiodarone is deethylamiodarone. After oral administration, Amiodarone has low and variable bioavailability and exhibits high lipophilicity^[2].

Induction of lung fibrosis model^[1]

Background

Amiodarone induces pulmonary injury by direct toxicity to lung tissue, hypersensitivity reaction, enhanced oxidative stress, alteration of membrane properties and activation of alveolar macrophages and cytokine release. Amiodarone administration can result in interstitial and/or alveolar inflammation and release of inflammatory mediators.

Specific Modeling Methods

Rat: F344 rats • male • 200-225 g
Administration: 6.25 mg/kg • i.t. instillation • in 0.3 mL of water • on days 0 and 2

Note

The solution should brought to room temperature before instillation.

Modeling Indicators

Marker of lung fibrosis: Increased lung collagen content.
Higher levels of total protein in lung lavage fluid.
Increased LDH activity in bronchoalveolar lavage, and increased lung MPO activity.
Increased total cell counts, alveolar macrophages, neutrophils and eosinophils.

Opposite Product(s): Curcumin (HY-N0005)

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

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 19774-82-4
Appearance Solid
Molecular Weight 681.77
Formel C₂₅H₃₀ClI₂NO₃
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
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

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)

Publications (13)

All Cell Proliferation/Viability AssayBio/Physico-chemical AssayIn Vivo Efficacy Study

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Journal Impact Factor

Cell

Red blood cells undergo lytic programmed cell death involving NLRP3. [Abstract]

2025 May 29;188(11):3013-3029.e19. PMID: 40252640
Cell

Structural basis for human Cav1.2 inhibition by multiple drugs and the neurotoxin calciseptine. [Abstract]

2023 Nov 22;186(24):5363-5374.e16. PMID: 37972591
Cell

Structural basis for the severe adverse interaction of sofosbuvir and amiodarone on L-type Cav channels. [Abstract]

2022 Dec 8;185(25):4801-4810.e13. PMID: 36417914

Amiodarone hydrochloride purchased from MedChemExpress. Usage Cited in: Cell. 2022 Dec 8;185(25):4801-4810.e13. [Abstract]

Amiodarone hydrochloride (AMIO; 0-10 μM; 30 min) enhanced inhibition by co-applied MNI-1 and AMIO indicates a strong synergistic effect between these two drugs in HEK293 cells.

Amiodarone hydrochloride purchased from MedChemExpress. Usage Cited in: Cell. 2022 Dec 8;185(25):4801-4810.e13. [Abstract]

Modeling of pharmacodynamic effects of LTCC blockers on MNI-1. This figure was plotted from a batch of IC50 experiment measuring LTCC blockers supplemented with 3 μM MNI-1 (Amiodarone hydrochloride; AMIO), or 90 μM MNI-1 (nifedipine and verapamil). The concentrations of LTCC blockers decrease from left to right.
Sci Adv

Quantitative prediction of siRNA complexation by ionizable drugs enables their codelivery in nanoparticles. [Abstract]

2026 Jun 12;12(24):eaed2731. PMID: 42284421
Sci Adv

A worm-like nucleic acid nanostructure for gene delivery and endosomal escape via ClC3 ion exchanger. [Abstract]

2026 Mar 6;12(10):eadw0891. PMID: 41790895
Ecotoxicol Environ Saf

PPARγ-responsive luciferase reporter system for high-throughput screening of chemical toxins with potential pulmonary fibrosis effects. [Abstract]

2025 Nov 15:307:119433. PMID: 41273832

Amiodarone hydrochloride purchased from MedChemExpress. Usage Cited in: Ecotoxicol Environ Saf. 2025 Nov 15:307:119433. [Abstract]

Subcytotoxic concentrations of four chemicals (Amiodarone; 0-100 μM; 24 h) known to induce pulmonary fibrosis were assessed using the CCK-8 assay.
Ecotoxicol Environ Saf

Effect of bisphenol A on craniofacial cartilage development in zebrafish (Danio rerio) embryos: A morphological study. [Abstract]

2021 Apr 1:212:111991. PMID: 33548570

Amiodarone hydrochloride purchased from MedChemExpress. Usage Cited in: Ecotoxicol Environ Saf. 2021 Apr 1:212:111991. [Abstract]

Angle and length measured in 5- dpf zebrafish co-exposed from 0-5 dpf to 0.05 μM BPA+ 1.0 μM Amiodarone hydrochloride (AMO). (A-C) Data are presented as box-whisker plots (n = 7-8 fish per group), tick-down line indicates significant difference.(D) Representative images of whole-mounted alcian blue stained larval skull.
Front Bioeng Biotechnol

Application of 3D Hepatic Plate-Like Liver Model for Statin-Induced Hepatotoxicity Evaluation. [Abstract]

2022 Mar 17;10:826093. PMID: 35372314

Amiodarone hydrochloride purchased from MedChemExpress. Usage Cited in: Front Bioeng Biotechnol. 2022 Mar 17;10:826093. [Abstract]

Amiodarone hydrochloride (AMD; 0-300 μM; 24 h) decreased cell viability in L-02 cells in two-dimensional co-culture (2D), collagen sandwich co-culture (CS), 3D hybrid hydrogel fiber (3D-H)；3D hepatic plate-like Na-Alg hydrogel fiber co-culture model system (3D-P co-culture system）。
Biotechnol Bioeng

An integrated biomimetic array chip for establishment of collagen-based 3D primary human hepatocyte model for prediction of clinical drug-induced liver injury. [Abstract]

2021 Dec;118(12):4687-4698. PMID: 34478150
Viruses

Screening and Identification of Lujo Virus Inhibitors Using a Recombinant Reporter Virus Platform. [Abstract]

2021 Jun 28;13(7):1255. PMID: 34203149
Biochem Biophys Res Commun

Combinatorial screening of a panel of FDA-approved drugs identifies several candidates with anti-Ebola activities. [Abstract]

2020 Feb 19;522(4):862-868. PMID: 31806372
SSRN

2023 Nov 8.
Patent

US20180263995A1.

Lösungsmittel & Löslichkeit

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.4668 mL

7.3339 mL

14.6677 mL

5 mM

0.2934 mL

1.4668 mL

2.9335 mL

10 mM

0.1467 mL

0.7334 mL

1.4668 mL

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

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

Stock Solution Working Solution

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.

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (3.67 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

Working Solution

For the following dissolution methods, please prepare the working solution directly:

It is recommended to prepare fresh solutions and use them promptly within a short period of time.

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: 17% Solutol HS-15 in Saline

Solubility: 10 mg/mL (14.67 mM); Clear solution; Need ultrasonic

Protocol 2

Add each solvent one by one: 0.5% CMC-Na/1% Tween-80 in Saline water

Solubility: 3.3 mg/mL (4.84 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (288 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Yihong Zhang,et al. Interactions between amiodarone and the hERG potassium channel pore determined with mutagenesis and in silico docking. Biochem Pharmacol. 2016 Aug 1;113:24-35. [Content Brief]

[2]. Jie Weng, et al. Amiodarone induces cell proliferation and myofibroblast differentiation via ERK1/2 and p38 MAPK signaling in fibroblasts. Biomed Pharmacother. 2019 Jul;115:108889. [Content Brief]

[3]. Sabrina Le Bouter, et al. Long-term amiodarone administration remodels expression of ion channel transcripts in the mouse heart. Circulation. 2004 Nov 9;110(19):3028-35. [Content Brief]

[4]. Punithavathi D, et al. Protective effects of curcumin against amiodarone-induced pulmonary fibrosis in rats. Br J Pharmacol. 2003 Aug;139(7):1342-50. [Content Brief]

[5]. Shayeganpour A, et al. Pharmacokinetics of Amiodarone in hyperlipidemic and simulated high fat-meal rat models. Biopharm Drug Dispos. 2005 Sep;26(6):249-57. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

Amiodarone hydrochloride

13 Cited Publications

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Amiodarone hydrochloride

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Publications Citing Use of MedChemExpress (MCE) Amiodarone hydrochloride

Biologische Aktivität

Chemical Information

Publications (13)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Amiodarone hydrochloride Related Classifications

Art. -Nr.: HY-14188