Amiodarone-d4 hydrochloride is the deuterium labeled Amiodarone hydrochloride. Amiodarone hydrochloride, a benzofuran-based Class III antiarrhythmic agent, inhibits WT outwardIhERG tails with an IC50 of ∼45 nM[1]. Amiodarone hydrochloride induces cell proliferation and myofibroblast differentiation via ERK1/2 and p38 MAPK signaling in fibroblasts[2]. Amiodarone hydrochloride can be used in the research of both supraventricular and ventricular arrhythmias[1].
体外研究 (In Vitro)
Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
685.80
Formula
C25H26D4ClI2NO3
CAS 号
1216715-80-8
中文名称
盐酸胺碘酮-d4
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder
-20°C
3 years
4°C
2 years
In solvent
-80°C
6 months
-20°C
1 month
参考文献
[1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.
[2]. 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.
[3]. 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.
[4]. 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.
Amiodarone hydrochloride, a benzofuran-based Class III antiarrhythmic agent, inhibits WT outwardIhERG tails with an IC50 of ∼45 nM[1]. Amiodarone hydrochloride induces cell proliferation and myofibroblast differentiation via ERK1/2 and p38 MAPK signaling in fibroblasts[2]. Amiodarone hydrochloride can be used in the research of both supraventricular and ventricular arrhythmias[1].
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[1]. 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[1]. 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[1]. Amiodarone (1-6 μg/mL) induces human embryonic lung fibroblasts (HELFs) cell proliferation and PD98059 or SB203580 suppresses this effect[2]. Amiodarone (1-6 ug/mL) does not induces HELFs cell apoptosis. Amiodarone (over 15 ug/mL) induces cell apoptosis[2]. 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[2].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Proliferation Assay[2]
Cell Line:
HELFs
Concentration:
1, 3 and 6 μg/mL
Incubation Time:
24 hours
Result:
Increased HELFs proliferation compared with the control group.
Western Blot Analysis[2]
Cell Line:
HELFs
Concentration:
1, 3 and 6 μg/mL
Incubation Time:
24 hours
Result:
α-SMA and vimentin were increased significantly in a dose-dependent manner.
RT-PCR[2]
Cell Line:
HELFs
Concentration:
1, 3 and 6 μg/mL
Incubation Time:
24 hours
Result:
Induced an increase of α-SMA and vimentin mRNA expression.
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[3].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model:
Ten-week-old male C57BL/6 mice[3]
Dosage:
30, 90, and 180 mg/kg/day
Administration:
Treated orally; for 6 weeks
Result:
Mice treated with 90 and 180 mg/kg/day had decreased body and heart weights, although their heart weight-to-body weight ratios were not significantly 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.
Clinical Trial
分子量
681.77
Formula
C25H30ClI2NO3
CAS 号
19774-82-4
中文名称
盐酸胺碘酮;盐酸乙碘酮;盐酸安律酮;盐酸胺碘达隆;盐酸胺碘呋酮;盐酸乙胺碘呋酮
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)
溶解性数据
In Vitro:
DMSO : 24.5 mg/mL (35.94 mM; Need ultrasonic and warming)
配制储备液
浓度溶剂体积质量
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
*
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
In Vivo:
请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:
[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.