A class III antiarrhythmic agent; inhibits KCNH2 with an IC50 value of 1 µM; also inhibits CYP2C8 and CYP3A4 in vitro at low micromolar concentrations

Amiodarone (hydrochloride) – 500 mg

Brand:
Cayman
CAS:
19774-82-4
Storage:
-20
UN-No:
Non-Hazardous - /

Amiodarone is a class III antiarrhythmic agent, in that it prolongs both cardiac action potential and refractoriness by blocking potassium currents.{22478} It inhibits the voltage-gated potassium channel hERG, also known as KCNH2, with an IC50 value of 1 µM.{24593} In addition, amiodarone binds with high affinity to the sigma-1 opioid receptor, 3-β-hydroxysteroid Δ8Δ7 isomerase, and C-8 sterol isomerase (Kis = 1, 25, and 62 nM, respectively) and inhibits human thyroid hormone receptors α and β (IC50s = 0.6, 0.65 µM, respectively).{24575,24578} It also inhibits the cytochrome P450 (CYP) isoforms CYP2C8 and CYP3A4 in vitro at low micromolar concentrations.{24577}  

 

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Description

A class III antiarrhythmic agent; inhibits KCNH2 with an IC50 value of 1 µM; also inhibits CYP2C8 and CYP3A4 in vitro at low micromolar concentrations

Formal name: (2-butyl-3-benzofuranyl)[4-[2-(diethylamino)ethoxy]-3,5-diiodophenyl]-methanone, monohydrochloride

Synonyms: 

Molecular weight: 681.8

CAS: 19774-82-4

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Ion Channel Modulation|Blockers||Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Product Type|Biochemicals|Small Molecule Inhibitors|Cytochrome P450||Product Type|Biochemicals|Small Molecule Inhibitors|MMPs||Research Area|Cardiovascular System|Heart|Arrhythmia

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