1. Induced Disease Models Products Membrane Transporter/Ion Channel Autophagy
  2. Respiratory System Disease Models Potassium Channel Autophagy
  3. Amiodarone

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.

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Amiodarone Chemical Structure

Amiodarone Chemical Structure

CAS No. : 1951-25-3

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Description

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

In Vivo

Cyproheptadine can be used in animal modeling to construct diabetes models.
Cyproheptadine (1 mg/kg; i.p.; daily, for 5 days; C57BL/6 mice) exerts thromboprotective properties in vivo[2].
Cyproheptadine is metabolized in rats through demethylation and oxidation to produce desmethylcyproheptadine (DMCPHepo), while cyproheptadine epoxide (CPHepo) is a minor metabolite. DMCPHepo accumulates in tissues and lasts longer than what the concentration curve in plasma would predict. DMCPHepo may be an active metabolite of CPH and could be associated with damage to pancreatic cells. Additionally, any remaining dose of CPH might be excreted through feces either in its original form or as metabolites[1].
Cyproheptadine can be used in animal modeling to construct models of diabetes[1].

1. 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): /



2. 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.
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
References
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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
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HY-14187
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