Amiodarone hydrochloride是一种 III 类抗心律失常剂,可抑制野生型IhERG钾通道及其尾电流,IC50约为 45 nM。Amiodarone hydrochloride通过成纤维细胞中,Amiodarone hydrochlorideERK1/2和p38 MAPK信号传导诱导细胞增殖和肌成纤维细胞分化。Amiodarone hydrochloride可用于室上性和室性心律失常的研究。
生物活性 | Amiodarone hydrochloride, a benzofuran-based Class III antiarrhythmic agent, inhibits WT outwardIhERGtails with anIC50of ~45 nM[1]. Amiodarone hydrochloride induces cell proliferation and myofibroblast differentiation viaERK1/2andp38 MAPKsignaling 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 IC50of 117.8 nM[1]. Amiodarone (1 μM) blocks inwardIhERG by 68.8±6.1%, with concentration response data yielding IC50and 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 IC50and 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].
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. |
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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].
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. |
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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 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 |
*请根据半岛bd体育手机客户端
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半岛bd体育手机客户端
失效。 储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture and light)。-80℃ 储存时,请在 6 个月内使用,-20℃ 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: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用;
以下溶剂前显示的百 分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂: 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.5 mg/mL (3.67 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (3.67 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂: 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.5 mg/mL (3.67 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (3.67 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。 3. 请依序添加每种溶剂: 10% DMSO 90%corn oil Solubility: ≥ 2.5 mg/mL (3.67 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (3.67 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。 *以上所有助溶剂都可在本网站选购。
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