产品说明书

Azelnidipine

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Chemical Structure| 123524-52-7 同义名 : CS 905;RS 9054;brand name CalBlock.;CCRIS 8650;UR-12592
CAS号 : 123524-52-7
货号 : A110442
分子式 : C33H34N4O6
纯度 : 97%
分子量 : 582.646
MDL号 : MFCD00865803
存储条件：

粉末 Keep in dark place,Inert atmosphere,Room temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(180.21 mM)，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：

IP 2% DMSO+2% Tween80+30% PEG300+water 4 mg/mL clear

PO 0.5% CMC-Na 21 mg/mL suspension

生物活性
靶点

  • Calcium Channel
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 ... 展开 >>Cardiovascular Diseases 收起 << Phase 4 Completed - Japan ... 展开 >> 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 收起 <<
NCT01819441 Cerebral Small Vessel Diseases Phase 4 Unknown December 2016 China, Beijing ... 展开 >> Peking University First Hospital Recruiting Beijing, Beijing, China, 100034 Contact: Yining Huang       ynhuang@sina.com 收起 <<
NCT00607035 Hypertension Phase 4 Completed - Japan ... 展开 >> Jichi Medical University School of Medicine Tochigi, Japan 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.72mL

0.34mL

0.17mL

8.58mL

1.72mL

0.86mL

17.16mL

3.43mL

1.72mL
参考文献

[1]Chen BL, Zhang YZ, et al. Clinical use of azelnidipine in the treatment of hypertension in Chinese patients. Ther Clin Risk Manag. 2015 Feb 24;11:309-18. doi: 10.2147/TCRM.S64288. eCollection 2015.

[2]Miyazaki S, Hamada T, et al. Effects of azelnidipine on uric acid metabolism in patients with essential hypertension. Clin Exp Hypertens. 2014;36(7):447-53.

[3]Ohyama T, Sato K, Kishimoto K, et al. Azelnidipine is a calcium blocker that attenuates liver fibrosis and may increase antioxidant defence. Br J Pharmacol. 2012;165(4b):1173‐1187

[4]Komoda H, Inoue T, Node K. Anti-inflammatory properties of azelnidipine, a dihydropyridine-based calcium channel blocker. Clin Exp Hypertens. 2010;32(2):121‐128

[5]Kain V, Kumar S, Sitasawad SL. Azelnidipine prevents cardiac dysfunction in streptozotocin-diabetic rats by reducing intracellular calcium accumulation, oxidative stress and apoptosis. Cardiovasc Diabetol. 2011;10:97. Published 2011 Nov 4

[6]Takano Y, Ueyama T, Ishikura F. Azelnidipine, unique calcium channel blocker could prevent stress-induced cardiac dysfunction like α·β blocker. J Cardiol. 2012;60(1):18‐22

[7]Komoda H, Shiraki A, Oyama JI, Nishikido T, Node K. Azelnidipine Inhibits the Differentiation and Activation of THP-1 Macrophages through the L-Type Calcium Channel. J Atheroscler Thromb. 2018;25(8):690‐697