Amiodarone hydrochloride

Name: Amiodarone hydrochloride
Brand: MedChemExpress
SKU: HY-14188
Rating: 5.0 (9 reviews)

Cat. No.: HY-14188 Purity: 99.86%: FAQs
Data Sheet SDS COA Handling Instructions

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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.

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

Amiodarone hydrochloride Chemical Structure

CAS No. : 19774-82-4

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 61	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 61	In-stock	Estimated Time of Arrival: December 31
Solid
500 mg	USD 55	In-stock	Estimated Time of Arrival: December 31
1 g	USD 66	In-stock	Estimated Time of Arrival: December 31
5 g	USD 119	In-stock	Estimated Time of Arrival: December 31
10 g		Get quote
50 g		Get quote

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Based on 9 publication(s) in Google Scholar

Other Forms of Amiodarone hydrochloride:

Amiodarone-d₄ hydrochloride Get quote
Amiodarone Get quote
Amiodarone hydrochloride (Standard) Get quote

9 Publications Citing Use of MCE Amiodarone hydrochloride

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Biological Activity
Purity & Documentation
References
Customer Review

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 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 Mmodeling 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.

Correlated Product(s): /

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

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.

19774-82-4

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
10 mM	0.1467 mL	0.7334 mL	1.4668 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.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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: 0.5% CMC-Na/1% Tween-80 in Saline water
Solubility: 3.3 mg/mL (4.84 mM); Clear solution; Need ultrasonic
Protocol 2

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 3

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.
Protocol 4

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.

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

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

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: 99.86%

Select Batch:

Data Sheet (289 KB) SDS (393 KB)

COA (255 KB) LCMS (93 KB)

Handling Instructions (2659 KB)

References

[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]

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