Modecainide (BMY 40327)
(Synonyms: 莫地卡尼,BMY 40327; MJ 14030) 目录号 : GC32535Modecainide (BMY 40327) 是 Encainide 的主要代谢物,Encainide 是一种抗心律失常药物。
Cas No.:81329-71-7
Sample solution is provided at 25 µL, 10mM.
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Modecainide is a major metabolite of Encainide, which is an antiarrhythmic agent.
The effect of Encainide and its two major metabolites, O-demethylated Encainide (MJ 9444) and 3-O-methoxy Encainide (MJ 14030), on cardiac conduction is studied by recording His bundle potentials in isolated perfused rabbit hearts and Purkinje and muscle conduction in vivo in dog hearts after destruction of the atrioventricular node. Both metabolites are 4 to 15 times more potent than Encainide in slowing conduction through the atria, the AV-node and the His-Purkinje system of the rabbit heart. In the dog, Encainide (0.8-3.2 mg/kg i.v.) slows conduction of extrasystoles in both Purkinje and muscle at all coupling intervals, increases the effective refractory period and the functional refractory period of the Purkinje pathway. MJ 9444 (0.05-0.4 mg/kg) speeds Purkinje conduction of early (less than 300 msec) without affecting or while slowing conduction of late (greater than 350 msec) extrasystoles. Higher doses (0.4-1.6 mg/kg) slows conduction at all intervals. The effective refractory period and the functional refractory period are decreased but in some cases returned to control values at the higher doses. Muscle conduction is slowed at doses of 0.4 mg/kg or more. MJ 14030 (0.05-3.2 mg/kg) has variable effects, behaving like MJ 9444 in three experiments but like the parent compound in two others[1].
[1]. Dresel PE. Effect of encainide and its two major metabolites on cardiac conduction. J Pharmacol Exp Ther. 1984 Jan;228(1):180-6.
Cas No. | 81329-71-7 | SDF | |
别名 | 莫地卡尼,BMY 40327; MJ 14030 | ||
Canonical SMILES | O=C(NC1=CC=CC=C1CCC2N(C)CCCC2)C3=CC=C(O)C(OC)=C3 | ||
分子式 | C22H28N2O3 | 分子量 | 368.47 |
溶解度 | Methanol : ≥ 250 mg/mL (678.48 mM); DMSO : 100 mg/mL (271.39 mM; Need ultrasonic) | 储存条件 | Store at -20°C |
General tips | 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 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。 为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。 |
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1 mg | 5 mg | 10 mg | |
1 mM | 2.7139 mL | 13.5696 mL | 27.1393 mL |
5 mM | 0.5428 mL | 2.7139 mL | 5.4279 mL |
10 mM | 0.2714 mL | 1.357 mL | 2.7139 mL |
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% DMSO % % Tween 80 % saline | ||||||||||
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2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
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