Amiodarone hydrochloride, a benzofuran-based Class III antiarrhythmic agent, inhibits WT outwardIhERG tails with an IC 50 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.
性状
Solid
体外研究(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. 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. 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. Amiodarone (1-6?μg/mL) induces human embryonic lung fibroblasts (HELFs) cell proliferation and PD98059 or SB203580 suppresses this effect.Amiodarone (1-6?ug/mL) does not induces HELFs cell apoptosis. Amiodarone (over 15?ug/mL) induces cell apoptosis.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.
体内研究(In Vivo)
Long-term Amiodarone (90, and 180 mg/kg/day) treatment induces a dose-dependent remodeling of ion-channel expression that is correlated with the cardiac electrophysiologic effects of Amiodarone. has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model:
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
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)
ClinicalTrial
参考文献
[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.
溶解度数据
In Vitro: DMSO : 24.5 mg/mL (35.94 mM; Need ultrasonic and warming)配制储备液