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Purity: ≥98%
Amiodarone HCl (formerly NSC-85442; NSC85442; NSC 85442; Cordarone), the hydrochloride salt of amiodarone, is an antiarrhythmic drug used to treat and prevent an irregular heartbeat. It acts as a sodium/potassium-ATPase inhibitor and an autophagy activator used to treat various types of cardiac dysrhythmias.
| ln Vitro |
Amiodarone hydrochloride inhibits the inward IhERG tail with an IC50 of 117.8 nM in 94 mM high-K+ external solution ([K+]e) [1]. Amiodarone hydrochloride (1 μM) blocks inwardIhERG by 68.8±6.1%, and concentration response data gave IC50 with h values of 765.5±287.8 nM and 0.9±0.4 for T623A hERG [1]. Amiodarone (1 μM) blocks inward IhERG with IC50 and h values of 979.2±84.3 nM and 1.1±0.1 for S624A hERG [1]. Amiodarone (1-6 μg/mL) promotes cell proliferation in human embryonic lung fibroblasts (HELFs), while PD98059 or SB203580 decreases this action [2]. Amiodarone (1-6 μg/mL) does not induce apoptosis in HELFs cells. Amiodarone hydrochloride (greater than 15 μg/mL) causes apoptosis [2]. Amiodarone hydrochloride (1, 3 and 6 μg/mL; 24 hours) stimulates α-SMA and vimentin mRNA and protein expression associated by an increase in ERK1/2 and p38 MAPK phosphorylation [2].
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| ln Vivo |
Animal models of pulmonary fibrosis can be created with the use of amiodarone hydrochloride in animal modeling. Chronic administration of 90 and 180 mg/kg/day of amiodarone hydrochloride causes a dose-dependent modification of ion channel expression, which is correlated with the drug's effects on cardiac electrophysiology [3].
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| Cell Assay |
Cell Proliferation Assay[2]
Cell Types: HELFs Tested Concentrations: 1, 3 and 6 μg/mL Incubation Duration: 24 hrs (hours) Experimental Results: Increased HELFs proliferation compared with the control group. Western Blot Analysis[2] Cell Types: HELFs Tested Concentrations: 1, 3 and 6 μg/mL Incubation Duration: 24 hrs (hours) Experimental Results: α-SMA and vimentin were increased Dramatically in a dose-dependent manner. RT-PCR[2] Cell Types: HELFs Tested Concentrations: 1, 3 and 6 μg/mL Incubation Duration: 24 hrs (hours) Experimental Results: Induced an increase of α-SMA and vimentin mRNA expression. |
| Animal Protocol |
Animal/Disease Models: Tenweeks old male C57BL/6 mice[3]
Doses: 30, 90, and 180 mg/kg/day Route of Administration: Treated po (oral gavage) for 6 weeks Experimental Results: Mice treated with 90 and 180 mg/kg/day had diminished body and heart weights, although their heart weight-to-body weight ratios were not Dramatically 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. |
| 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.
[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. [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. |
| Molecular Formula |
C25H29I2NO3.HCL
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| Molecular Weight |
681.77
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| CAS # |
19774-82-4
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| Related CAS # |
Amiodarone-d4 hydrochloride;1216715-80-8;Amiodarone;1951-25-3
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| SMILES |
IC1C([H])=C(C([H])=C(C=1OC([H])([H])C([H])([H])N(C([H])([H])C([H])([H])[H])C([H])([H])C([H])([H])[H])I)C(C1C2=C([H])C([H])=C([H])C([H])=C2OC=1C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H])=O.Cl[H]
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| InChi Key |
ITPDYQOUSLNIHG-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C25H29I2NO3.ClH/c1-4-7-11-22-23(18-10-8-9-12-21(18)31-22)24(29)17-15-19(26)25(20(27)16-17)30-14-13-28(5-2)6-3;/h8-10,12,15-16H,4-7,11,13-14H2,1-3H3;1H
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| Chemical Name |
2-Butyl-3-benzofuryl 4-(2-(diethylamino)ethoxy)-3,5-diiodophenyl ketone hydrochloride
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| Synonyms |
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (3.67 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (3.67 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (3.67 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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