Amiodarone . HCl

Specifications / Handling

More Information
Product Details
Synonyms	Cordarone; Pacerone; Nexterone; 2-Butyl-3-benzofuranyl 4-(2-(diethylamino)ethoxy)-3,5-diiodophenyl ketone hydrochloride
Product Type	Chemical
Properties
Formula	C₂₅H₂₉I₂NO₃ . HCl
MW	645.3 . 36.5
CAS	19774-82-4
RTECS	OB1361000
Source/Host Chemicals	Synthetic.
Purity Chemicals	≥98%
Appearance	White to off-white powder.
Solubility	Soluble in DMF (10 mg/ml), DMSO (10 mg/ml) or ethanol (5 mg/ml). Only slightly soluble in water (<1mg/ml at 25 °C).
InChi Key	ITPDYQOUSLNIHG-UHFFFAOYSA-N
Smiles	O=C(C1=CC(I)=C(OCCN(CC)CC)C(I)=C1)C2=C(CCCC)OC3=CC=CC=C32.Cl
Shipping and Handling
Shipping	AMBIENT
Short Term Storage	+4°C
Long Term Storage	-20°C
Handling Advice	Keep cool and dry. Protect from light and moisture.
Use/Stability	Stable for at least 2 years after receipt when stored at -20°C.
Documents
Product Specification Sheet
Datasheet	Download PDF

Product-specific References

Description

Amiodarone hydrochloride is a non-selective ion channel blocker (potassium, sodium and calcium channels). Amiodarone is a class III antiarrhythmic agent, in that it prolongs both cardiac action potential and refractoriness by blocking potassium currents. It inhibits the voltage-gated potassium channel hERG, also known as KCNH2. In addition, amiodarone binds with high affinity to the σ-1 opioid receptor, 3-β-hydroxysteroid Δ8Δ7 isomerase, and C-8 sterol isomerase and inhibits human thyroid hormone receptors α and β. It also inhibits the cytochrome P450 (CYP) isoforms CYP2C8 and CYP3A4 in vitro at low micromolar concentrations.

Amiodarone induces cell proliferation and myofibroblast differentiation via ERK1/2 and p38 MAPK signaling in fibroblasts. Recently, this K+ efflux inhibitor has been used to block the colocalisation of miniNLRP3 and ASC in red blood cells (RBCs), in a new process involving miniNLRP3 and RBC lysis, called spectosis.

Product References

Inhibition of ATP-sensitive potassium channels of adult rat heart cells by antiarrhythmic drugs: R.A. Haworth, et al.; Circ. Res. 65, 1157 (1989)
Therapeutic drug monitoring: Antiarrhythmic drugs: T.J. Campbell & K.M. Williams; Br. J. Clin. Pharmacol. 46, 307 (1998)
Amiodarone inhibits cardiac ATP-sensitive potassium channels: D.S. Holmes, et al.; J. Cardiovasc. Electrophysiol. 11, 1152 (2000)
Synthesis and preliminary characterization of a novel antiarrhythmic compound (KB130015) with an improved toxicity profile compared with amiodarone: B. Carlsson, et al.; J. Med. Chem. 45, 623 (2002)
Mechanism-based inactivation of human cytochrome P4502C8 by drugs in vitro: T.M. Polasek, et al.; J. Pharmacol. Exp. Ther. 311, 996 (2004)
Discovery of high-affinity ligands of σ1 receptor, ERG2, and emopamil binding protein by pharmacophore modeling and virtual screening: C. Laggner, et al.; J. Med. Chem. 48, 4754 (2005)
Predicting hERG activities of compounds from their 3D structures: Development and evaluation of a global descriptors based QSAR model: N. Sinha & S. Sen; Eur. J. Med. Chem. 46, 618 (2011)
Amiodarone induces cell proliferation and myofibroblast differentiation via ERK1/2 and p38 MAPK signaling in fibroblasts: J. Weng, et al.; Biomed. Pharmacother. 115, 108889 (2019)
Amiodarone Advances the Apoptosis of Cardiomyocytes by Repressing Sigmar1 Expression and Blocking KCNH2-related Potassium Channels: H. Liang, et al.; Curr. Mol. Med. 25, 69 (2025)
Red blood cells undergo lytic programmed cell death involving NLRP3: Y. Chen, et al.; Cell 188, 3013 (2025)

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