Referencia número: HY-14187

Amiodarone

13 Cited Publications

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Based on 13 publication(s) in Google Scholar

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

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Pureza: 98.32%
No. CAS: 1951-25-3
Fòrmula: C₂₅H₂₉I₂NO₃
Peso molecular:645.31

Almacenamiento:

-20°C, sealed storage, away from moisture

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

Amiodarone Chemical Structure

No. CAS: 1951-25-3

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Actividad biológica
- Descripciòn
- Cellular Effect
- In Vitro
- Induced Disease Models
Chemical Information
Publications (13)
Solvente y solubilidad
- In Vitro
- In Vivo
Pureza y Documentación
Referencias
Help & FAQs
Classifications
Bioz

Actividad biológica

Descripciòn

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

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	IC₅₀	1.9 μM Compound: amiodarone	Inhibition of Cav1.2 current measured using QPatch automatic path clamp system in CHO cells expressing Cav1.2, beta-2 and alpha-2/delta-1 subunits Inhibition of Cav1.2 current measured using QPatch automatic path clamp system in CHO cells expressing Cav1.2, beta-2 and alpha-2/delta-1 subunits	[PMID: 23812503]
CHO-K1	IC₅₀	>10 μM Compound: Amiodarone	Antagonism of compound towards thyroid response element (TRAF alpha) in CHO-K1 cells Antagonism of compound towards thyroid response element (TRAF alpha) in CHO-K1 cells	[PMID: 11806713]
CHO-K1	IC₅₀	>10 μM Compound: Amiodarone	Antagonism of compound towards thyroid response element (TRAF beta) in CHO-K1 cells Antagonism of compound towards thyroid response element (TRAF beta) in CHO-K1 cells	[PMID: 11806713]
CHO-K1	IC₅₀	0.6 μM Compound: Amiodarone	Concentration required to inhibit 50% of binding of [125I]T3 to human Thyroid hormone receptor beta 1 in CHO-K1 cells Concentration required to inhibit 50% of binding of [125I]T3 to human Thyroid hormone receptor beta 1 in CHO-K1 cells	[PMID: 11806713]
CHO-K1	IC₅₀	0.65 μM Compound: Amiodarone	Concentration required to inhibit 50% of binding of [125I]-T3 to human Thyroid hormone receptor alpha-1 in CHO-K1 cells Concentration required to inhibit 50% of binding of [125I]-T3 to human Thyroid hormone receptor alpha-1 in CHO-K1 cells	[PMID: 11806713]
CHRC5 cell line	EC₅₀	2300 nM Compound: amiodarone	Reversal of sensitivity of multidrug resistant chinese hamster ovary cell line CHRC/5 expressed as concentration that restores 50% of cytotoxic activity of 5 ug/mL toward doxorubicin Reversal of sensitivity of multidrug resistant chinese hamster ovary cell line CHRC/5 expressed as concentration that restores 50% of cytotoxic activity of 5 ug/mL toward doxorubicin	[PMID: 7608906]
HEK293	IC₅₀	30 nM Compound: Amiodarone	Inhibition of potassium current (Ikr) measured using whole-cell patch clamp experiments in HEK-293 cells stable transfected with hERG cDNA Inhibition of potassium current (Ikr) measured using whole-cell patch clamp experiments in HEK-293 cells stable transfected with hERG cDNA	[PMID: 21300721]
HL-60	IC₅₀	5.27 μM Compound: 17; ZINC03830212	Antiproliferative activity against human HL-60 cells measured after 24 hrs by MTT assay Antiproliferative activity against human HL-60 cells measured after 24 hrs by MTT assay	[PMID: 34605238]
KB	IC₅₀	16.6 μM Compound: 45	Cytotoxicity in human KB cells Cytotoxicity in human KB cells	[PMID: 21504156]
LLC-PK1	IC₅₀	22.5 μM Compound: Amiodarone	TP_TRANSPORTER: inhibition of Daunorubicin transepithelial transport (basal to apical) (Daunorubicin: 0.035 uM) in MDR1-expressing LLC-PK1 cells TP_TRANSPORTER: inhibition of Daunorubicin transepithelial transport (basal to apical) (Daunorubicin: 0.035 uM) in MDR1-expressing LLC-PK1 cells	[PMID: 11231118]
LLC-PK1	IC₅₀	45.6 μM Compound: Amiodarone	TP_TRANSPORTER: inhibition of Digoxin transepithelial transport (basal to apical) (Digoxin: 0.025 uM) in MDR1-expressing LLC-PK1 cells TP_TRANSPORTER: inhibition of Digoxin transepithelial transport (basal to apical) (Digoxin: 0.025 uM) in MDR1-expressing LLC-PK1 cells	[PMID: 11231118]
MCF7	IC₅₀	>50 μM Compound: 17; ZINC03830212	Antiproliferative activity against human MCF7 cells measured after 24 hrs by MTT assay Antiproliferative activity against human MCF7 cells measured after 24 hrs by MTT assay	[PMID: 34605238]
MDA-MB-231	IC₅₀	33.43 μM Compound: 17; ZINC03830212	Antiproliferative activity against human MDA-MB-231 cells measured after 24 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells measured after 24 hrs by MTT assay	[PMID: 34605238]
MDA-MB-231	IC₅₀	33.43 μM Compound: 16; ZINC03830212	Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay	[PMID: 38261767]
RAW264.7	IC₅₀	3.5 μM Compound: Amiodarone	Protection against Bacillus anthracis lethal toxin-mediated cytotoxicity in mouse RAW264.7 cells assessed as change in viability after 24 hrs by WST1 dye reduction assay Protection against Bacillus anthracis lethal toxin-mediated cytotoxicity in mouse RAW264.7 cells assessed as change in viability after 24 hrs by WST1 dye reduction assay	[PMID: 17485504]
U-937	IC₅₀	9.31 μM Compound: 17; ZINC03830212	Antiproliferative activity against human U-937 cells measured after 24 hrs by MTT assay Antiproliferative activity against human U-937 cells measured after 24 hrs by MTT assay	[PMID: 34605238]

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 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) 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) induces human embryonic lung fibroblasts (HELFs) cell proliferation and PD98059 or SB203580 suppresses this effect^[2].
Amiodarone (1-6 μg/mL) does not induces HELFs cell apoptosis. Amiodarone (over 15 μg/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.

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 in animal modeling to create pulmonary toxicity and liver injury models. After a single oral dose of Amiodarone in rats, the pharmacokinetic characteristics detectable include an absorption half-life of approximately 1.83 hours and a clearance half-life ranging from 15 hours (at a 100 mg/kg dose) to 105 hours (at a 200 mg/kg dose), with an average oral bioavailability of 39%. Amiodarone is primarily distributed in the lungs, liver, thyroid, and adipose tissue, with drug concentrations in the lungs and adipose tissue being significantly higher than in other tissues. Following long-term oral administration, the accumulation of Amiodarone in adipose tissue is notably increased^[3]^[4]^[5].

Induction of pulmonary toxicity^[4]

Background

Amiodarone promotes the release of cytokines such as TNF, TGF-β, IL-4, and IL-8 by activating NF-κB, while also enhancing the involvement of natural killer cells in immune regulation. This leads to the release of reactive oxygen species, leukocyte aggregation, and intracellular lipid accumulation, thereby inducing pulmonary damage ^[4].

Specific Modeling Methods

Rat: Fischer • male • 9 to 10 weeks old
Administration: 175 mg/kg • po • once daily, 5 days a week for 12 weeks

Note

(1) Amiodarone is suspended in a 0.5% methylcellulose solution (HY-125861).
(2) The rats are weighed weekly and the drug dose is adjusted if necessary, higher doses of amiodarone could be fatal.

Modeling Indicators

Histological Changes: The number of macrophages, neutrophils, and lymphocytes in the bronchi and alveoli of rats is significantly increased.
Phenotypic Observations: Lung sections of rats show interstitial thickening with accumulation of mononuclear cells, alveoli filled with numerous foamy macrophages, and mild fibrosis.

Correlated Product(s): Methyl cellulose (HY-125861)

Induction of liver injury^[5]

Background

Amiodarone is metabolized in the liver by the cytochrome P450 3A4 enzyme to produce metabolites such as desethylamiodarone (DEA), leading to mitochondrial dysfunction, increased intracellular oxidative stress, and lipid metabolism disorders, which in turn activate macrophages (Kupffer cells) in the liver, thereby inducing liver injury in mice^[5].

Specific Modeling Methods

Mice: Balb/cCrSlc • male • 8-week-old
Administration: 1000 mg/kg • po • single dose

Note

1. Amiodarone is dissolved in corn oil.
2. Prior to oral administration of Amiodarone, pre-treatment with Dexamethasone (HY-14648) was conducted to induce cytochrome P450 3A4 enzyme expression. Dexamethasone was dissolved in corn oil and administered at a dose of 60 mg/kg via intraperitoneal injection once daily for 3 days. Amiodarone was administered orally 24 hours after the final dose of Dexamethasone.

Modeling Indicators

Molecular Changes: The levels of alanine aminotransferase (ALT) and triglycerides in the plasma of mice are significantly elevated. The release of cytochrome c into the cytosol of liver cells is increased. The ratio of reduced glutathione to oxidized glutathione disulfide in the liver is significantly decreased, indicating increased oxidative stress and reduced cellular antioxidant capacity in the liver.

Correlated Product(s): Dexamethasone (HY-14648)

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

Chemical Information

No. CAS 1951-25-3
Appearance <54°C Solid, >55°C Liquid
Peso molecular 645.31
Fòrmula C₂₅H₂₉I₂NO₃
Color Off-white to light yellow
SMILES

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

Room temperature in continental US; may vary elsewhere.
Almacenamiento

-20°C, sealed storage, away from moisture

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

Publications (13)

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

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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 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 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 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 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 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.

Solvente y solubilidad

In Vitro:

DMSO : ≥ 175 mg/mL (271.19 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

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Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.5496 mL

7.7482 mL

15.4964 mL

5 mM

0.3099 mL

1.5496 mL

3.0993 mL

10 mM

0.1550 mL

0.7748 mL

1.5496 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). 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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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

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Molecular Weight Molecular Weight

Calculadora de dilución

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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 90% (20% SBE-β-CD in Saline)

Solubility: 2.5 mg/mL (3.87 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

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 2

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

Solubility: ≥ 2.5 mg/mL (3.87 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.

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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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

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

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Referencias

[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]. Plomp TA, et al. Pharmacokinetics and body distribution of amiodarone and desethylamiodarone in rats after oral administration. In Vivo. 1987 Sep-Oct;1(5):265-79. [Content Brief]

[4]. Wilson BD, et al. Amiodarone-induced pulmonary toxicity in the rat. Lung. 1989;167(5):301-11. [Content Brief]

[5]. Takai S, et al. Establishment of a mouse model for amiodarone-induced liver injury and analyses of its hepatotoxic mechanism. J Appl Toxicol. 2016 Jan;36(1):35-47. [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	1.5496 mL	7.7482 mL	15.4964 mL	38.7411 mL
	5 mM	0.3099 mL	1.5496 mL	3.0993 mL	7.7482 mL
	10 mM	0.1550 mL	0.7748 mL	1.5496 mL	3.8741 mL
	15 mM	0.1033 mL	0.5165 mL	1.0331 mL	2.5827 mL
	20 mM	0.0775 mL	0.3874 mL	0.7748 mL	1.9371 mL
	25 mM	0.0620 mL	0.3099 mL	0.6199 mL	1.5496 mL
	30 mM	0.0517 mL	0.2583 mL	0.5165 mL	1.2914 mL
	40 mM	0.0387 mL	0.1937 mL	0.3874 mL	0.9685 mL
	50 mM	0.0310 mL	0.1550 mL	0.3099 mL	0.7748 mL
	60 mM	0.0258 mL	0.1291 mL	0.2583 mL	0.6457 mL
	80 mM	0.0194 mL	0.0969 mL	0.1937 mL	0.4843 mL
	100 mM	0.0155 mL	0.0775 mL	0.1550 mL	0.3874 mL

Keywords

Amiodarone

13 Cited Publications

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Amiodarone

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Publications Citing Use of MedChemExpress (MCE) Amiodarone

Actividad biológica

Chemical Information

Publications (13)

Solvente y solubilidad

Pureza y Documentación

Referencias

Help & FAQs

Complete Stock Solution Preparation Table

Amiodarone Related Classifications

HY-14187 Related Classifications