货号:A110442 同义名: CS 905;RS 9054
Azelnidipine is a dihydropyridine L-type calcium channel blocker and an antihypertensive.
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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 |
ERK,p38 MAPK,ROS | 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 |
+
L-type calcium channel, IC50: 12.2 μM N-type Ca2+ channel, IC50: 0.11 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。 |
靶点 |
|
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]. |
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 << |
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 |
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 |