Amiodarone

Cat. No.: HY-14187: FAQs
Data Sheet Handling Instructions

Molarity Calculator

Amiodarone is an antiarrhythmic agent for inhibition of ATP-sensitive potassium channel with an IC₅₀ of 19.1 μM.

At equivalent molar concentrations, both the salt and free forms of a compound exhibit comparable biological activity. Nevertheless, the salt form (Amiodarone hydrochloride) usually boasts enhanced water solubility and stability.

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

Amiodarone Chemical Structure

CAS No. : 1951-25-3

Size		Stock
MOQ		Minimum order quantity
50 mg		Get quote
100 mg		Get quote
250 mg		Get quote
Other size		Get quote

Synthetic products have potential research and development risk.

* Please select Quantity before adding items.

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

Other In-stock Forms of Amiodarone:

Amiodarone hydrochloride

Other Forms of Amiodarone:

9 Publications Citing Use of MCE Amiodarone

Featured Recommendations

•Related Small Molecules:

•Related Proteins:

Biological Activity
Purity & Documentation
References
Customer Review

Description

Amiodarone is an antiarrhythmic agent for inhibition of ATP-sensitive potassium channel with an IC₅₀ of 19.1 μM.

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]
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]
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]
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 Vivo

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 Mmodeling 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)

Opposite Product(s): /

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 Mmodeling 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)

Opposite Product(s): /

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

Clinical Trial

Molecular Weight

645.31

Formula

C₂₅H₂₉I₂NO₃

CAS No.

1951-25-3

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Singh, B.N. and E.M. Vaughan Williams, The effect of amiodarone, a new anti-anginal drug, on cardiac muscle. Br J Pharmacol, 1970. 39(4): p. 657-67. [Content Brief]

[2]. Rosenbaum, M.B., et al., Clinical efficacy of amiodarone as an antiarrhythmic agent. Am J Cardiol, 1976. 38(7): p. 934-44. [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]

Amiodarone Related Classifications

Molarity Calculator
Dilution Calculator

The molarity calculator equation

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

Mass		Concentration		Volume		Molecular Weight *
	=		×		×

The dilution calculator equation

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)	×	Volume _(start)	=	Concentration _(final)	×	Volume _(final)
	×		=		×
C1		V1		C2		V2

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.

Keywords:

Amiodarone1951-25-3Potassium ChannelAutophagyKcsAInhibitorinhibitorinhibit

Your Recently Viewed Products:

Product Name

Salutation

Applicant Name *

Email Address *

Phone Number *

Organization Name *

Department *

Requested quantity *

Country or Region *

Remarks