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CAS No.: 123524-52-7

Azelnidipine/阿折地平 Catalog No. CSN10368

Synonyms: CS 905;UR-12592;RS 9054

Azelnidipine is a dihydropyridine L-type calcium channel blocker and an antihypertensive.

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技术信息

生物活性

描述Azelnidipine is a calcium blocker that has been shown to have antioxidant effects in endothelial cells and cardiomyocytes. Azelnidipine inhibited TGF-β1- and Ang II-induced HSC (hepatic stellate cells) activation in vitro and attenuated CCl4- and TAA-induced liver fibrosis, and it accelerated regression of CCl4-induced liver fibrosis in mice^[3]. Cultures of human mononuclear leukocytes collected from six healthy volunteers showed 100 nM of azelnidipine caused significant inhibition of formyl-methyonyl leucyl phenylalanine (fMLP)-induced production of IL-8. These results suggest that azelnidipine has anti-inflammatory effects independent of its anti-hypertensive action^[4]. Moreover, beneficial effect of Azelnidipine in diabetic cardiomyopathy via altering intracellular Ca2+ handling proteins and preventing apoptosis by its antioxidant property^[5]. Acute administration of azelnidipine could prevent a sudden drop of cardiac function after acute stress like IMO (immobilization stress: IMO). Azelnidipine might have a protective effect on stress-induced cardiac dysfunction like α and β adrenergic blockers^[6]. Azelnidipine has potent antiatherosclerotic properties by inhibition of macrophage activation through Cav1.2^[7].
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
NCT00134160	Hypertension ... more >>Cardiovascular Diseases Collapse <<	Phase 4	Completed	-	Japan ... more >> Department of Cardiovascular Medicine Graduate School of Medical Science Kumamoto University 1-1-1 Honjyo, Kumamoto-City, Kumamoto, Japan, 860-8556 OSCAR-Study Data Center ShinjukuParkTower30FN, 3-7-1 Nishi-Shinjuku, Shinjuku-ku, Tokyo, Japan, 163-1030 Collapse <<
NCT01819441	Cerebral Small Vessel Diseases	Phase 4	Unknown	December 2016	China, Beijing ... more >> Peking University First Hospital Recruiting Beijing, Beijing, China, 100034 Contact: Yining Huang ynhuang@sina.com Collapse <<
NCT00607035	Hypertension	Phase 4	Completed	-	Japan ... more >> Jichi Medical University School of Medicine Tochigi, Japan 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
- 1.7163 mL
- 8.5815 mL
- 17.1631 mL
- 5 mM
- 0.3433 mL
- 1.7163 mL
- 3.4326 mL
- 10 mM
- 0.1716 mL
- 0.8582 mL
- 1.7163 mL

技术信息

CAS号

123524-52-7

储存条件

粉末: Keep in dark place,Inert atmosphere,Room temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C33H34N4O6

运输

蓝冰

分子量

582.65

别名

CS 905;UR-12592;RS 9054;CCRIS-8650;brand name CalBlock;阿折地平

溶解度

DMSO	210.0 mg/mL (360.4 mM) warming
Water	insoluble

动物实验配方

IP	2% DMSO+2% Tween80+30% PEG300+water	4 mg/mL	clear
PO	0.5% CMC-Na	21 mg/mL	suspension

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NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点

NCT00134160	Hypertension ... more >>Cardiovascular Diseases Collapse <<	Phase 4	Completed	-	Japan ... more >> Department of Cardiovascular Medicine Graduate School of Medical Science Kumamoto University 1-1-1 Honjyo, Kumamoto-City, Kumamoto, Japan, 860-8556 OSCAR-Study Data Center ShinjukuParkTower30FN, 3-7-1 Nishi-Shinjuku, Shinjuku-ku, Tokyo, Japan, 163-1030 Collapse <<
NCT01819441	Cerebral Small Vessel Diseases	Phase 4	Unknown	December 2016	China, Beijing ... more >> Peking University First Hospital Recruiting Beijing, Beijing, China, 100034 Contact: Yining Huang ynhuang@sina.com Collapse <<
NCT00607035	Hypertension	Phase 4	Completed	-	Japan ... more >> Jichi Medical University School of Medicine Tochigi, Japan Collapse <<
NCT01028534	Obstructive Sleep Apnea ... more >> Hypertension Collapse <<	Not Applicable	Completed	-	Japan ... more >> Kirigaoka Tsuda Hospital Kitakyushu, Japan Kyoto University Hospital Kyoto, Japan Collapse <<
NCT00294567	Hypertension ... more >>Coronary Atherosclerosis Collapse <<	Phase 4	Completed	-	Japan ... more >> Department of Cardiology, Juntendo University School of Medicine Tokyo, Japan Collapse <<
NCT00454662	Hypertension ... more >>Cardiovascular Disease Diabetes Collapse <<	Phase 4	Completed	-	Japan ... more >> COLM-Study Data Center Kamiyacho MT Bld.14F, 4-3-20 Toranomon Minato-ku, Tokyo, Japan, 105-0001 Collapse <<

Azelnidipine/阿折地平 Catalog No. CSN10368

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