产品说明书

Candesartan

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Chemical Structure| 139481-59-7 同义名 : CV 11974;Candesartan M1;Candesartan, CV11974, CV-1197, CV 11974, Trade names: Blopress, Atacand, Amias, and Ratacand
CAS号 : 139481-59-7
货号 : A148921
分子式 : C24H20N6O3
纯度 : 95%
分子量 : 440.454
MDL号 : MFCD00864463
存储条件:

粉末 Inert atmosphere,Room Temperature

液体 -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 105 mg/mL(238.39 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:

2% DMSO+40% PEG 300+2% Tween 80+water 10 mg/mL

生物活性
靶点
  • AT1 receptor

    AT1 receptor, IC50:0.26 nM

描述 Candesartan is an angiotensin II receptor antagonist with IC50 of 0.26 nM. In vivo research shows that conducted on 5XFAD mice, 2-months intranasal treatment with candesartan resulted in reduced Aβ deposits and microglial accumulation in the hippocampus but not in the cortex. In vitro, reduced IL-1β levels in 4-hour LPS-stimulated cortical microglia (100 ng/mL) following 2-hour pretreatment with candesartan (10 μM)[3]. It is a prolonged angiogenic effect, associated with enhanced VEGF-A and VEGF-B expression in vitro and in vivo, in response to a single dose of candesartan treatment[4].
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
NCT00863980 Acute Myocardial Infarction ... 展开 >> Angina Pectoris Myocardial Ischemia Acute Coronary Syndrome Hypertension 收起 << Not Applicable Terminated(Principle investiga... 展开 >>tor resigned in 2013) 收起 << - Japan ... 展开 >> Shakaihoken Kobe Central Hospital Kobe, Japan, 651-1145 Akashi Municipal Hospital Kobe, Japan, 673-8501 Kouseikai Takeda Hospital Kyoto, Japan, 600-8558 Aijyukai Dohjin Hospital Kyoto, Japan, 602-0917 Kyoto Second Red Cross Hospital Kyoto, Japan, 602-8026 Kyoto Prefectural University of Medicine Kyoto, Japan, 602-8566 Social Insurance Kyoto Hospital Kyoto, Japan, 603-8151 Kyoto Kojyo Hokenkai Kyoto, Japan, 604-8472 Kyoto City Hospital Kyoto, Japan, 604-8845 Kyoto First Red Cross Hospital Kyoto, Japan, 605-0981 Aiseikai Yamashina Hospital Kyoto, Japan, 607-8086 Tanabe Central Hospital Kyoto, Japan, 610-0334 Rakusai Simizu Hospital Kyoto, Japan, 610-1106 Uji Hospital Kyoto, Japan, 611-0011 Kyoto Yawata Hospital Kyoto, Japan, 614-8114 Seizinkai Simizu Hospital Kyoto, Japan, 615-8237 Saiseikai Kyoto Hospital Kyoto, Japan, 617-0814 Public Yamasiro Hospital Kyoto, Japan, 619-0214 Gakkentoshi Hospital Kyoto, Japan, 619-0238 Fukuchiyama City Hospital Kyoto, Japan, 620-8505 Ayabe City Hospital Kyoto, Japan, 623-0011 Maizuru Red Cross Hospital Kyoto, Japan, 624-0906 National Hospital Organization Maizuru Medical Center Kyoto, Japan, 625-8502 Maizuru Kyosai Hospital Kyoto, Japan, 625-8585 Public Nantan Hospital Kyoto, Japan, 629-0197 Kyoto Prefectural Yosanoumi Hospital Kyoto, Japan, 629-2261 Kumihama Hospital Kyoto, Japan, 629-3403 Sakurakai Takahashi Hospital Kyoto, Japan, 654-0026 Yuuseikai Midorigaoka Hospital Osaka, Japan, 569-1121 Matsushita Memorial Hospital Osaka, Japan, 570-8540 Saiseikai Shiga Hospital Shiga, Japan, 520-3046 Omihachiman Community Medical Center Shiga, Japan, 523-0892 收起 <<
NCT00130975 Atrial Fibrillation Phase 3 Completed - Norway ... 展开 >> Ulleval University Hospital Oslo, Norway, 0407 Asker & Baerum Hospital Rud, Norway, 1309 收起 <<
NCT00150631 Hypertension Phase 3 Unknown December 2014 Denmark ... 展开 >> Karin Skov Aarhus, Denmark, 8000 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.27mL

0.45mL

0.23mL

11.35mL

2.27mL

1.14mL

22.70mL

4.54mL

2.27mL

参考文献

[1]Kosugi M, Miyajima A, et al. Angiotensin II type 1 receptor antagonist candesartan as an angiogenic inhibitor in a xenograft model of bladder cancer. Clin Cancer Res. 2006 May 1;12(9):2888-93.

[2]Ojima M, Inada Y, et al. Candesartan (CV-11974) dissociates slowly from the angiotensin AT1 receptor. Eur J Pharmacol. 1997 Jan 14;319(1):137-46.

[3]Torika N, Asraf K, Apte RN, Fleisher-Berkovich S. Candesartan ameliorates brain inflammation associated with Alzheimer's disease. CNS Neurosci Ther. 2018 Mar;24(3):231-242. doi: 10.1111/cns.12802. Epub 2018 Jan 24. PMID: 29365370; PMCID: PMC6489976.

[4]Soliman S, Ishrat T, Pillai A, Somanath PR, Ergul A, El-Remessy AB, Fagan SC. Candesartan induces a prolonged proangiogenic effect and augments endothelium-mediated neuroprotection after oxygen and glucose deprivation: role of vascular endothelial growth factors A and B. J Pharmacol Exp Ther. 2014 Jun;349(3):444-57. doi: 10.1124/jpet.113.212613. Epub 2014 Mar 28. PMID: 24681872; PMCID: PMC4019323.