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CAS No.: 63675-72-9

Nisoldipine/尼索地平 Catalog No. CSN17095

Synonyms: BAY-k 5552;(±)-BAY-K-5552;Sular

Nisoldipine is a calcium channel blocker belonging to the dihydropyridines class, specific for L-type Cav1.2 with IC50 of 10 nM.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 Calcium Channel Cav1.2

IC50:10nM
描述Nisoldipine, a dihydropyridine calcium antagonist, has greater vascular selectivity than other calcium channel antagonists and does not depress the intact myocardium in vivo. It should be taken on an empty stomach. In patients with stable angina pectoris nisoldipine coat-core increases exercise duration, reduces anginal frequency and myocardial ischemia, and is effective as monotherapy or in combination with a beta-blockers^[3]. The drug exhibits higher potency, longer duration of action, and a higher binding affinity in vitro and in vivo than nifedipine. The influence of nisoldipine on cardiac stimulus formation and conduction is also very slight in anesthetized animals, and is completely eliminated in awake animals and humans by counter-regulation up to very high doses. Clinically, nisoldipine was found more potent and prolonged in its action in comparison with nifedipine. In comparative studies, nisoldipine, 10 mg once a day, was found equieffective with nifedipine 10 mg three times or 20 mg twice a day in angina or hypertension, respectively^[4]. Nisoldipine coat core (CC) is an extended-release formulation that allows nisoldipine to be released gradually over 24 hours, minimizing fluctuations in plasma concentration and providing a good trough/peak ratio. Nisoldipine CC improves cardiac function and exercise tolerance in patients recovering from acute myocardial infarction, without increasing the risk of mortality compared with placebo. It also improves exercise performance in patients with stable angina pectoris^[5].
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
NCT00684489	Hypertension	Not Applicable	Completed	-	-
NCT00730197	Healthy	Phase 1	Completed	-	United States, North Dakota ... more >> PRACS Institute, Ltd. Fargo, North Dakota, United States, 58104 Collapse <<
NCT00979537	Healthy	Phase 1	Completed	-	United States, North Dakota ... more >> Pracs Institute, Ltd Fargo, North Dakota, United States, 58104 Collapse <<

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参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.5746 mL
- 12.8728 mL
- 25.7457 mL
- 5 mM
- 0.5149 mL
- 2.5746 mL
- 5.1491 mL
- 10 mM
- 0.2575 mL
- 1.2873 mL
- 2.5746 mL

技术信息

CAS号

63675-72-9

储存条件

粉末: Keep in dark place,Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C20H24N2O6

运输

蓝冰

分子量

388.41

别名

BAY-k 5552;(±)-BAY-K-5552;Sular;Baymycard;Nisocor;Syscor;尼索地平

溶解度

DMSO	77.0 mg/mL (198.2 mM)
Water	Insoluble
Ethanol	60.0 mg/mL (154.5 mM) warming

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