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Candesartan/坎地沙坦 {[allProObj[0].p_purity_real_show]}

货号：A148921 同义名： CV 11974; Candesartan M1

Candesartan是一种来源于苯并咪唑的竞争性 AT1 受体抑制剂，IC50 值为 0.26 nM。

Candesartan/坎地沙坦 化学结构 CAS号：139481-59-7
Candesartan/坎地沙坦 化学结构
CAS号：139481-59-7
Candesartan/坎地沙坦 3D分子结构
CAS号：139481-59-7
Candesartan/坎地沙坦 化学结构 CAS号：139481-59-7
Candesartan/坎地沙坦 3D分子结构 CAS号：139481-59-7
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Candesartan/坎地沙坦 纯度/质量文件 产品仅供科研

货号：A148921 标准纯度： {[allProObj[0].p_purity_real_show]}
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Candesartan/坎地沙坦 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].

Candesartan/坎地沙坦 细胞实验

Cell Line
Concentration Treated Time Description References
J774A.1 macrophages 7.5, 15, 30 µM 0.5 hours Candesartan dose-dependently inhibited IL-1β secretion and reduced IL-18 secretion and active caspase-1 expression. Front Immunol. 2022 May 20;13:870627.
Human retinal endothelial cells 1μg/ml 24 hours To examine the proangiogenic effects of candesartan in human endothelial cells under normoxia and hypoxia, results showed that candesartan enhanced VEGFR2 activation and tube formation under hypoxia, and this effect was dependent on HO-1 expression. Angiogenesis. 2015 Apr;18(2):137-50.
Bovine Retinal Endothelial Cells (BREC) 1 µM 24 hours Candesartan restored GLO-I activity and mRNA levels in BREC and reduced NO● production. Diabetes. 2010 Dec;59(12):3208-15.
Bovine Retinal Pericytes (BRP) 1 µM 24 hours Candesartan restored GLO-I activity and mRNA levels in BRP and reduced NO● production. Diabetes. 2010 Dec;59(12):3208-15.
Monocytes 0.1 µM, 1 µM, 5 µM 24 hours Pretreatment with candesartan significantly reduced Pam3CSK4 or LPS-induced TLR2 and TLR4 expression at both mRNA and protein levels, along with decreased activity of NF-κB and expression of IL-1β, IL-6, TNF-α, and MCP-1 Atherosclerosis. 2009 Jan;202(1):76-83.
THP-1 cells 1 µM 24 hours Pretreatment with candesartan significantly reduced Pam3CSK4 or LPS-induced TLR2 and TLR4 expression Atherosclerosis. 2009 Jan;202(1):76-83.
BeWo cells 1 µM 48 hours To investigate the effect of candesartan on PPARγ and its target genes in BeWo cells. Results showed that candesartan had no significant effect on PPARγ target genes in BeWo cells. Int J Mol Sci. 2022 Oct 14;23(20):12326.
SGHPL-4 cells 1 µM 48 hours To investigate the effect of candesartan on PPARγ and its target genes in SGHPL-4 cells. Results showed that candesartan had no significant effect on PPARγ target genes in SGHPL-4 cells. Int J Mol Sci. 2022 Oct 14;23(20):12326.

Candesartan/坎地沙坦 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Chicken embryos Chorioallantoic membrane (CAM) model Chorioallantoic membrane 0.1 µM Single dose, 24 hours To investigate the effect of candesartan on angiogenesis in the chorioallantoic membrane of chicken embryos. Results showed that angiotensin II (AngII) treatment significantly increased angiogenesis. Int J Mol Sci. 2022 Oct 14;23(20):12326.
Rats Diabetes and atherosclerosis-induced ischemic stroke model Nasal administration 1 mg/kg Once daily for 10 days To evaluate the therapeutic effects of the CLEP formulation on diabetes-associated stroke. The results showed that the CLEP formulation significantly reduced infarction after stroke, decreased flexion, spontaneous motor activity, and time spent in the target quadrant, and enhanced grip strength. Int J Pharm X. 2024 Jan 2;7:100227
C57BL/6 mice Traumatic brain injury (TBI) model Subcutaneous injection 1 mg/kg/day Continuous administration until killing (3 or 28 days) Candesartan treatment reduced the lesion volume after CCI injury by approximately 50%, decreased the number of dying neurons, lessened the number of activated microglial cells, protected cerebral blood flow (CBF), and reduced the expression of the cytokine TGF b1 while increasing expression of TGF b3. Candesartan-treated mice also showed better motor skills on the rotarod 3 days after injury, and improved performance in the Morris water maze 4 weeks after injury. Neuropsychopharmacology. 2012 Dec;37(13):2817-29
C57Bl/6J mice Ischemic retinopathy model Intraperitoneal injection 1mg/kg and 10mg/kg Once daily for 5 days To examine the vascular protective effects of candesartan in an ischemic retinopathy model, results showed that candesartan significantly reduced pathological neovascularization and promoted physiological revascularization of the central retina by suppressing iNOS expression and restoring HO-1 expression. Angiogenesis. 2015 Apr;18(2):137-50.
C57BLJ/6 mice Normal mice Intraperitoneal injection 2 mg/kg Once daily for 10 days Candesartan treatment significantly reduced Pam3CSK4-induced TLR2 expression and LPS-induced TLR4 expression Atherosclerosis. 2009 Jan;202(1):76-83.
C57BL/6JNal mice MSU-induced peritonitis model Oral 30 mg/kg/day Once daily for 3 days Oral administration of candesartan significantly reduced NLRP3 inflammasome activity in the MSU-induced peritonitis mouse model, decreasing the levels of IL-1β and active caspase-1 in the peritoneal fluids. Front Immunol. 2022 May 20;13:870627.
Transgenic Ren-2 rats Diabetic model Gavage 5 mg/kg/day Once daily for 20 weeks Candesartan reduced retinal acellular capillaries, inflammation, and iNOS in diabetic Ren-2 rats and restored GLO-I activity. Diabetes. 2010 Dec;59(12):3208-15.

Candesartan/坎地沙坦 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 <<

Candesartan/坎地沙坦 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.

Candesartan/坎地沙坦 实验方案

计算器
存储液制备 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

Candesartan/坎地沙坦 技术信息

CAS号139481-59-7
分子式C24H20N6O3
分子量 440.45
SMILES Code C1=CC=C(C2=C1N=C([N]2CC3=CC=C(C=C3)C4=CC=CC=C4C5=N[NH]N=N5)OCC)C(O)=O
MDL No. MFCD00864463
别名 CV 11974; Candesartan M1
运输蓝冰
InChI Key HTQMVQVXFRQIKW-UHFFFAOYSA-N
Pubchem ID 2541
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Sealed in dry,2-8°C
溶解方案

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

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用； 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶
方案 一
方案 二

Tags: Candesartan | 139481-59-7 | CV 11974 | CV11974 | CV-11974 | GPCR/G Protein | Vitamin D Related/Nuclear Receptor | Metabolic Enzyme/Protease | Cell Cycle/DNA Damage | Angiotensin Receptor | PPAR | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Candesartan/坎地沙坦 纯度/质量文件 | Candesartan/坎地沙坦 生物活性 | Candesartan/坎地沙坦 临床数据 | Candesartan/坎地沙坦 参考文献 | Candesartan/坎地沙坦 实验方案 | Candesartan/坎地沙坦 技术信息

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