Amiodarone-D4 HCl Chemical Properties

Flash point:

9℃

storage temp. 

-20°C

solubility 

DMF: 10 mg/ml,DMSO: 10 mg/ml,Ethanol: 5 mg/ml

form 

A solid

color 

White to off-white

Stability:

Very Hygroscopic

Safety Information

Hazard Codes 

F,T

Risk Statements 

11-23/24/25-39/23/24/25

Safety Statements 

7-16-36/37-45

RIDADR 

UN1230 - class 3 - PG 2 - Methanol, solution

WGK Germany 

1

Amiodarone-D4 HCl Usage And Synthesis

Description

Amiodarone-d₄ is intended for use as an internal standard for the quantification of amiodarone by GC- or LC-MS. 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, with an IC₅₀ value of 1 μM. In addition, amiodarone binds with high affinity to the sigma-1 opioid receptor, 3-β-hydroxysteroid Δ⁸Δ⁷ isomerase, and C-8 sterol isomerase (K_is = 1, 25, and 62 nM, respectively) and inhibits human thyroid hormone receptors α and β (IC₅₀s = 0.6 and 0.65 μM, respectively). It also inhibits the cytochrome P450 (CYP) isoforms CYP2C8 and CYP3A4 in vitro at low micromolar concentrations.

Uses

A Labelled non-selective ion channel blocker. Antiarrhythmic (class III).

General Description

A Certified Spiking Solution^?and stable-labeled internal standard for use in therapeutic drug monitoring analyses by LC/MS. Amiodarone, an antiarrhythmic agent marketed as Pacerone^?, Cordarone^?, Aratac, Atlansil, is monitored by clinical labs to ensure patients remain within the drug′s therapeutic range.

References

[1] T. J. CAMPBELL  K. M W. Therapeutic drug monitoring: antiarrhythmic drugs[J]. British journal of clinical pharmacology, 2003, 46 4: 307-319. DOI: 10.1046/j.1365-2125.1998.t01-1-00768.x
[2] NANDITA SINHA  Srikanta S. Predicting hERG activities of compounds from their 3D structures: Development and evaluation of a global descriptors based QSAR model[J]. European Journal of Medicinal Chemistry, 2011, 46 2: Pages 618-630. DOI: 10.1016/j.ejmech.2010.11.042
[3] CHRISTIAN LAGGNER. Discovery of High-Affinity Ligands of σ1 Receptor, ERG2, and Emopamil Binding Protein by Pharmacophore Modeling and Virtual Screening[J]. Journal of Medicinal Chemistry, 2005, 48 15: 4754-4764. DOI: 10.1021/jm049073+
[4] BO CARLSSON. Synthesis and Preliminary Characterization of a Novel Antiarrhythmic Compound (KB130015) with an Improved Toxicity Profile Compared with Amiodarone[J]. Journal of Medicinal Chemistry, 2002, 45 3: 623-630. DOI: 10.1021/jm001126+
[5] THOMAS M POLASEK. Mechanism-based inactivation of human cytochrome P4502C8 by drugs in vitro.[J]. Journal of Pharmacology and Experimental Therapeutics, 2004, 311 3: 996-1007. DOI: 10.1124/jpet.104.071803

Amiodarone-D4 HCl(1216715-80-8)Related Product Information

• 1-Methoxy AMiodarone
• 3-(4-HYDROXY-3-IODOBENZOYL)-2-BUTYLBENZOFURAN
• Amiodarone
• Amiodarone hydrochloride
• [[p-(2-methoxyethyl)phenoxy]methyl]oxirane
• Desethyl Amiodarone Hydrochloride
• N-Desethylamiodarone-D4 HCl
• Bis Des-iodo amiodarone HCl(Amiodarone impurity)
• (2-butylbenzofuran-3-yl) (4-methoxyphenyl) ketone
• Amiodarone Impurity 13
• 2-Butyl-3-(3,5-Diiodo-4-hydroxy benzoyl) benzofuran
• Di(N-desethyl) AMiodarone Hydrochloride
• 2-Butylbenzofuran
• 2-Diethylaminoethylchloride hydrochloride
• 2-Butyl-3-(4-hydroxybenzoyl)benzofuran
• Dideiodo AMiodarone Hydrochloride
• Amiodarone Impurity 2
• Amiodarone N-oxide