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阿折地平 /Azelnidipine {[allProObj[0].p_purity_real_show]}

货号:A110442 同义名: CS 905;RS 9054

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

Azelnidipine 化学结构 CAS号:123524-52-7
Azelnidipine 化学结构
CAS号:123524-52-7
Azelnidipine 3D分子结构
CAS号:123524-52-7
Azelnidipine 化学结构 CAS号:123524-52-7
Azelnidipine 3D分子结构 CAS号:123524-52-7
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Azelnidipine 纯度/质量文件 产品仅供科研

货号:A110442 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 Ca2+ channel-like protein Calcium Channel Cav 2.2 其他靶点 纯度
CDC25B-IN-2 Akt 99%+
Clevidipine 97%
Verapamil HCl 99%
Amlodipine 99%
Amlodipine maleate 98%
(+)-cis-Diltiazem HCl 95%
Zegocractin ++

Orai1/STIM1-mediated Ca2+ currents, IC50: 120 nM

99%+
Tanshinone IIA sulfonate sodium 98%
Ulixacaltamide ++

hCaV3.1, IC50: 50 nM

hCaV3.2, IC50: 110 nM

99%+
Dronedarone Hydrochloride 95%
Nitrendipine +

Calcium channel, IC50: 95 nM

98%
Efonidipine HCl monoethanolate 98%
Cinnarizine 98%
SEA0400 ++

NCX, IC50: 33 nM

ROS,p38 MAPK,ERK 99%+
Fasudil HCl Rho,PKA 98%
ML-9 MLCK,Akt 99%+
Flunarizine 2HCl +

Calcium channel, Ki: 68 nM

95%
Lomerizine 2HCl 98%
Efonidipine 98%
Levamlodipine 97%
Nisoldipine ++

L-type Cav1.2, IC50: 10 nM

97%
Isradipine 98%
Lacidipine 98%
Lercanidipine 98%
Loureirin B Potassium Channel 99%+
Tetracaine HCl 98%
Manidipine +++

Calcium channel, IC50: 2.6 nM

98%
Manidipine Dihydrochlorid +++

Calcium channel, IC50: 2.6 nM

98%
Nicardipine 98%
Wilforgine 98+%
Econazole 99%+
Ginsenoside Rd NF-κB 98%
Fendiline HCl 98+%
Mesaconitine 98%
Tetrandrine 95%
Nifedipine 95%
Nilvadipine ++++

Calcium channel, IC50: 0.03 nM

98%
Barnidipine ++++

[3H]nitrendipine, Ki: 0.21 nM

95+%
Azelnidipine 97%
Levetiracetam 98%
Nimodipine 95%
Benidipine HCl 98%
Pinaverium bromide 98%
Pranidipine 98%
NP118809 +

N-type Ca2+ channel, IC50: 0.11 μM

L-type calcium channel, IC50: 12.2 μM

98%
Amlodipine Besylate +++

Calcium channel, IC50: 1.9 nM

97%
Cilnidipine 98%
Cinepazide Maleate 98%
Terfenadine 98%
YM-58483 99%+
Ranolazine 98%
Praeruptorin A p38 MAPK,Akt 98%
Ranolazine 2HCl 98%
Felodipine ++++

L-type calcium channel, IC50: 0.15 nM

98%
PD173212 +++

N-type Ca2+ channel, IC50: 36 nM

98%
Levamlodipine besylate 97%
Carboxyamidotriazole Orotate 98%
IGS-1.76 98+%
WH-4-023 ++++

Cav 2.2, IC50: 0.001 μM

++++

Cav 2.2, IC50: 0.001 μM

99%+
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。

Azelnidipine 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].

Azelnidipine 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 <<

Azelnidipine 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

Azelnidipine 实验方案

计算器
存储液制备 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

Azelnidipine 技术信息

CAS号123524-52-7
分子式C33H34N4O6
分子量 582.646
别名 CS 905;RS 9054;brand name CalBlock.;CCRIS 8650;UR-12592
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Keep in dark place,Inert atmosphere,Room temperature

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

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