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Amiodarone HCl/胺碘酮盐酸盐 {[allProObj[0].p_purity_real_show]}

货号:A143592 同义名: 盐酸胺碘酮 / Amiodarone (hydrochloride); Amiodarone hydrochloride

Amiodarone HCl 是一种抗心律失常化合物,用于抑制ATP敏感的钾通道,IC50为19.1 μM。

Amiodarone HCl/胺碘酮盐酸盐 化学结构 CAS号:19774-82-4
Amiodarone HCl/胺碘酮盐酸盐 化学结构
CAS号:19774-82-4
Amiodarone HCl/胺碘酮盐酸盐 3D分子结构
CAS号:19774-82-4
Amiodarone HCl/胺碘酮盐酸盐 化学结构 CAS号:19774-82-4
Amiodarone HCl/胺碘酮盐酸盐 3D分子结构 CAS号:19774-82-4
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Amiodarone HCl/胺碘酮盐酸盐 纯度/质量文件 产品仅供科研

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产品名称 Autophagy 其他靶点 纯度
SBI-0206965 +++

ULK1, IC50: 108 nM

ULK2, IC50: 711 nM

95%
Hydroxychloroquine sulfate 99%
Valproic acid sodium HDAC 97%
PFK-015 ++

PFKFB3, IC50: 207 nM

99%+
MRT68921 HCl ++++

ULK1, IC50: 2.9 nM

ULK2, IC50: 1.1 nM

99%+
ROC-325 99%+
Autophinib +++

Autophagy, IC50: 40 nM

99%
Lys05 99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。
产品名称 Potassium Channel 其他靶点 纯度
Tolbutamide 98%
Glimepiride ++++

SUR2B, IC50: 7.3 nM

SUR1, IC50: 5.4 nM

97%
Dronedarone HCl 95%
Gliquidone ++

Potassium channel, IC50: 27.2 nM

99%
TRAM-34 +++

IKCa1 (KCa3.1), Kd: 20 nM

98%
Glibenclamide 98%
Amiodarone HCl 97%
Gliclazide ++

Potassium channel, IC50: 184 nM

98%
Repaglinide 98%
Dofetilide 98%
Nateglinide 99%
Quinine HCl dihydrate 98%
ML133 HCl +

Kir2.1, IC50: 290 nM

99%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Amiodarone HCl/胺碘酮盐酸盐 生物活性

靶点
  • Potassium Channel

描述 Amiodarone hydrochloride is an antiarrhythmic drug for inhibition of ATP-sensitive potassium channel with IC50 of 19.1 μM. Amiodarone may act as an antioxidant/antiatherosclerotic agent in humans[3]. Amiodarone stimulates the accumulation of ethidium bromide by inhibiting its efflux from the cells. The effect of amiodarone is much stronger on wild-type cells compared to the mutant with inactivated ABC-transporters[4]. Chronic treatment with oral amiodarone for 4 weeks reduced Ip when myocytes were dialyzed with patch-pipettes containing either 10 mM Na+ or 80 mM Na+. Amiodarone had no effect on the voltage dependence of the pump or the affinity of the pump for extracellular K+ either after chronic treatment or during acute exposure. An amiodarone-induced inhibition of the hyperpolarizing Na(+)-K+ pump current may contribute to the action potential prolongation observed during treatment with this drug[5]. Cells treated with amiodarone were seen to have detached from the dish, with cell rounding, cytoplasmic blebbing and irregularity in shape. An increase in the sub-G1 phase fraction, from 15.43 to 21.34% and 79.83% and a reduction in the G1 phase fraction, from 48.83 to 41.63% and 11.52%, were observed in cells treated with amiodarone at concentrations of 0.1 and 1 mM, respectively[6].

Amiodarone HCl/胺碘酮盐酸盐 细胞实验

Cell Line
Concentration Treated Time Description References
CAFs 2.5 μM 24 h To evaluate the effect of Amiodarone on the activated state of CAFs, results showed that Amiodarone partially reversed the activated state of CAFs and reduced the protumor effects of CAFs on PCa cell growth. J Exp Clin Cancer Res. 2024 Jun 11;43(1):161.
DU145 cells 2.5 μM 24 h To evaluate the effect of Amiodarone on the growth of DU145 cells, results showed that Amiodarone reduced the protumor effects of CAFs on DU145 cell growth. J Exp Clin Cancer Res. 2024 Jun 11;43(1):161.
BEAS-2B cells 1, 3, 9 μM 24 h Amiodarone significantly decreased the viability of BEAS-2B cells, increased LDH release, ROS generation, caspase 3 activation, and apoptosis. Redox Rep. 2025 Dec;30(1):2447721.
BEAS-2B cells 3 μM 24 h Amiodarone significantly induced ROS generation and mitochondrial membrane potential depolarization in BEAS-2B cells, while artemisinin pretreatment significantly inhibited these effects. Redox Rep. 2025 Dec;30(1):2447721.
BEAS-2B cells 3 μM 24 h Amiodarone significantly increased caspase 3 activity and apoptosis in BEAS-2B cells, while artemisinin pretreatment significantly inhibited these effects. Redox Rep. 2025 Dec;30(1):2447721.
RAW 264.7 cells 0.312 μM 1, 3, 5, 7 days To investigate the effect of amiodarone on BMP accumulation in RAW 264.7 cells, the results showed that amiodarone treatment significantly increased cellular BMP levels. J Lipid Res. 2024 Jul;65(7):100574.
NR8383 rat alveolar macrophages 5 µM 24 h To evaluate the effects of Amiodarone on macrophage morphology and function, the results showed that amiodarone-induced foamy macrophages displayed characteristics of proinflammatory macrophages, including significantly increased nitric oxide production, vacuolation and lipidosis, and decreased phagocytic activity. Front Immunol. 2021 Sep 1;12:611280.
A549 cells 0.16-10 μM 24 h Test whether Amiodarone induces phospholipidosis, results showed Amiodarone significantly induced NBD-PE fluorescence, while sangivamycin did not. JCI Insight. 2022 Jan 11;7(1):e153165.

Amiodarone HCl/胺碘酮盐酸盐 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Mice C57BL/6J mice Oral 300 mg/kg 5 times per week for 4 weeks To study the amiodarone-induced interstitial lung disease (ILD) model, results showed that amiodarone caused a gradual decrease in in mice, with macrophage infiltration observed in the lungs, while co-treatment with dabigatran significantly attenuated these changes. Front Pharmacol. 2021 Sep 21;12:635293
SCID mice PCa xenograft model Intratumoral injection 250 μl 5 consecutive days for 2 weeks To evaluate the effect of Amiodarone on the growth of PCa xenograft tumors, results showed that Amiodarone reduced the protumor effects of CAFs on tumor growth. J Exp Clin Cancer Res. 2024 Jun 11;43(1):161.
Mice Awake and freely moving CD-1 male mice Intraperitoneal injection 5 mg/kg Single administration, observed for 6 hours Amiodarone did not revert the JWH-018-induced bradycardia but reduced tachyarrhythmic events, completely suppressing them during the last three hours of the experiment. Additionally, amiodarone slightly reverted the JWH-018-induced vasoconstriction during the fourth hour and restored the breathing rate reduction caused by JWH-018. Int J Mol Sci. 2023 Apr 19;24(8):7515
C57Bl6/J mice Amiodarone-induced lung injury model Tracheal injection 3 mg/kg Single injection Amiodarone significantly increased TUNEL-positive cells and cleaved caspase 3 protein levels in the lung tissue of mice, while artemisinin pretreatment significantly inhibited these effects and increased p-AMPK and Nrf2 protein levels. Redox Rep. 2025 Dec;30(1):2447721.

Amiodarone HCl/胺碘酮盐酸盐 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT02814903 - Unknown August 2017 France ... 展开 >> Joachim ALEXANDRE Recruiting Caen, Basse Normandie, France, 14000 Contact: Mathieu CHEQUEL, MD    +33625342363    chequel-m@chu-caen.fr    Contact: Pierre OLLITRAULT, MD    +33624922671    ollitrault-p@chu-caen.fr 收起 <<
NCT03685149 Arrhythmogenic Right Ventricul... 展开 >>ar Cardiomyopathy 收起 << Phase 2 Not yet recruiting August 2020 United States, New York ... 展开 >> University of Rochester Medical Center Not yet recruiting Rochester, New York, United States, 14642 Contact: Spencer Rosero, MD    585-275-4775    spencer_rosero@urmc.rochester.edu    Contact: Laura Wing    585-273-4128    laura_wing@urmc.rochester.edu 收起 <<
NCT00589303 - Terminated(Lack of funding) - -

Amiodarone HCl/胺碘酮盐酸盐 参考文献

[1]Knorre DA, Krivonosova TN, et al. Amiodarone inhibits multiple drug resistance in yeast Saccharomyces cerevisiae. Arch Microbiol. 2009 Aug;191(8):675-9.

[2]Lapenna D, Ciofani G, et al. Antioxidant activity of amiodarone on human lipoprotein oxidation. Br J Pharmacol. 2001 Jul;133(5):739-45.

[3]Lapenna D, Ciofani G, Bruno C, Pierdomenico SD, Cuccurullo F. Antioxidant activity of amiodarone on human lipoprotein oxidation. Br J Pharmacol. 2001;133(5):739-745

[4]Knorre DA, Krivonosova TN, Markova OV, Severin FF. Amiodarone inhibits multiple drug resistance in yeast Saccharomyces cerevisiae. Arch Microbiol. 2009;191(8):675-679

[5]Gray DF, Mihailidou AS, Hansen PS, et al. Amiodarone inhibits the Na(+)-K+ pump in rabbit cardiac myocytes after acute and chronic treatment. J Pharmacol Exp Ther. 1998;284(1):75-82

[6]Choi IS, Kim BS, Cho KS, et al. Amiodarone induces apoptosis in L-132 human lung epithelial cell line. Toxicol Lett. 2002;132(1):47-55

Amiodarone HCl/胺碘酮盐酸盐 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.47mL

0.29mL

0.15mL

7.33mL

1.47mL

0.73mL

14.67mL

2.93mL

1.47mL

Amiodarone HCl/胺碘酮盐酸盐 技术信息

CAS号19774-82-4
分子式C25H30ClI2NO3
分子量 681.77
SMILES Code CCCCC1=C(C(C2=CC(I)=C(OCCN(CC)CC)C(I)=C2)=O)C3=C(O1)C=CC=C3.Cl
MDL No. MFCD00069204
别名 盐酸胺碘酮 ;Amiodarone (hydrochloride); Amiodarone hydrochloride
运输蓝冰
InChI Key ITPDYQOUSLNIHG-UHFFFAOYSA-N
Pubchem ID 441325
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Keep in dark place, inert atmosphere, 2-8°C

溶解方案

DMSO: 20 mg/mL(29.34 mM),配合低频超声,并水浴加热至45℃助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的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
方案 一
方案 二
方案 三
配制的工作液建议现用现配,短期内尽快用完。 以下溶剂前显示的百分比是指该溶剂在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
方案 一
方案 二
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