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Disopyramide/丙吡胺 {[allProObj[0].p_purity_real_show]}

货号:A342795 同义名: 达舒平 / SC-7031; Dicorantil

Disopyramide can block sodium channel, it is a class IA antiarrhythmic drug.

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Disopyramide/丙吡胺 化学结构 CAS号:3737-09-5
Disopyramide/丙吡胺 化学结构
CAS号:3737-09-5
Disopyramide/丙吡胺 3D分子结构
CAS号:3737-09-5
Disopyramide/丙吡胺 化学结构 CAS号:3737-09-5
Disopyramide/丙吡胺 3D分子结构 CAS号:3737-09-5
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Disopyramide/丙吡胺 纯度/质量文件 产品仅供科研

货号:A342795 标准纯度: {[allProObj[0].p_purity_real_show]}
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sodium channel, IC50: 160 μM

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Na(V1.8) channel, IC50: 8 nM

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Voltage-gated sodium channel, ED50: 3.4 mM

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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。

Disopyramide/丙吡胺 生物活性

描述 Disopyramide is a class IA antiarrhythmic drug with efficacy in ventricular and atrial arrhythmias. Disopyramide possesses a non-competitive blocking action at the neuromuscular junction, which is not reversible by anticholinesterase agents. HERG tail currents recorded at -40 mV following test pulses to +30 mV were inhibited in a dose-dependent fashion by Disopyramide concentrations within the clinical range (IC50=7.23 μM)[1]. Disopyramide inhibits multiple ion channels, leading to lower Ca transients and force, and shortens action potentials, thus reducing cellular arrhythmias[2]. Disopyramide may be effective for preventing tachyarrhythmias in SQTS1 (Short QT syndrome1)-patients carrying the N588K mutation in HERG channel by APD (action potential duration)-prolongation via enhancing ICa-L (inward L-type calcium channel current), late INa (the late sodium channel current), INCX (the Na/Ca exchanger current), and reducing ISK (outward small-conductance calcium-activated potassium channel current)[3].

Disopyramide/丙吡胺 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
NCT00589303 Atrial Fibrillation ... 展开 >> Heart Failure 收起 << Phase 3 Terminated(Lack of funding) - United States, Arizona ... 展开 >> Mayo Clinic Arizona Scottsdale, Arizona, United States, 85259 United States, Indiana The Heart Group Evansville, Indiana, United States, 47710 United States, Minnesota Mayo Clinic Rochester, Minnesota, United States, 55905 United States, Oregon Oregon Health and Science University Portland, Oregon, United States, 97239 United States, Tennessee Chattanooga Heart Institute Chattanooga, Tennessee, United States, 37404 Canada, Alberta University of Calgary and Calgary Health Region Calgary, Alberta, Canada, T2N-4N1 收起 <<
NCT00000556 Arrhythmia At... 展开 >>rial Fibrillation Cardiovascular Diseases Heart Diseases 收起 << Phase 3 Completed - -
NCT00589303 - Terminated(Lack of funding) - -

Disopyramide/丙吡胺 参考文献

[1]Jones SV, Marshall IG. Non-competitive effects of disopyramide at the neuromuscular junction: evidence for endplate ion channel block. Br J Anaesth. 1987 Jun;59(6):776-83

[2]Coppini R, Ferrantini C, Pioner JM, Santini L, Wang ZJ, Palandri C, Scardigli M, Vitale G, Sacconi L, Stefàno P, Flink L, Riedy K, Pavone FS, Cerbai E, Poggesi C, Mugelli A, Bueno-Orovio A, Olivotto I, Sherrid MV. Electrophysiological and Contractile Effects of Disopyramide in Patients With Obstructive Hypertrophic Cardiomyopathy: A Translational Study. JACC Basic Transl Sci. 2019 Oct 9;4(7):795-813

[3]Lan H, Xu Q, El-Battrawy I, Zhong R, Li X, Lang S, Cyganek L, Borggrefe M, Zhou X, Akin I. Ionic Mechanisms of Disopyramide Prolonging Action Potential Duration in Human-Induced Pluripotent Stem Cell-Derived Cardiomyocytes From a Patient With Short QT Syndrome Type 1. Front Pharmacol. 2020 Oct 12;11:554422

Disopyramide/丙吡胺 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.95mL

0.59mL

0.29mL

14.73mL

2.95mL

1.47mL

29.46mL

5.89mL

2.95mL

Disopyramide/丙吡胺 技术信息

CAS号3737-09-5
分子式C21H29N3O
分子量 339.47
SMILES Code O=C(N)C(C1=NC=CC=C1)(C2=CC=CC=C2)CCN(C(C)C)C(C)C
MDL No. MFCD00057366
别名 达舒平 ;SC-7031; Dicorantil; Ritmilen; (±)-Disopyramide
运输蓝冰
InChI Key UVTNFZQICZKOEM-UHFFFAOYSA-N
Pubchem ID 3114
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Inert atmosphere, room temperature

溶解方案 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
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