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

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

Amiodarone HCl is an antiarrhythmic drug for inhibition of ATP-sensitive potassium channel with IC50 of 19.1 μM.

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

货号:A143592 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 Autophagy 其他靶点 纯度
SBI-0206965 +++

ULK2, IC50: 711 nM

ULK1, IC50: 108 nM

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

PFKFB3, IC50: 207 nM

99%+
MRT68921 hydrochloride ++++

ULK2, IC50: 1.1 nM

ULK1, IC50: 2.9 nM

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

Autophagy, IC50: 40 nM

97%
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 Hydrochloride 95%
Gliquidone ++

Potassium channel, IC50: 27.2 nM

98%
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 hydrochloride dihydrate 98%
ML133 HCl +

Kir2.1, IC50: 290 nM

97%
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 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 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 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 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 技术信息

CAS号19774-82-4
分子式C25H30ClI2NO3
分子量 681.77
别名 盐酸胺碘酮 ;Amiodarone (hydrochloride);Amiodarone hydrochloride
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Keep in dark place,Inert atmosphere,2-8°C

溶解度

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

动物实验配方

2% DMSO+30% PEG 300+2% Tween 80+water 3 mg/mL

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