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/ Candesartan cilexetil/坎地沙坦酯

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

货号：A259269 同义名： 坎地沙坦西酯 / TCV-116; Candesartan M1 Cilexetil

Candesartan cilexetil是一种苯并咪唑衍生的竞争性AT1受体抑制剂，IC50值为0.26 nM。

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There will be a HazMat fee per item when shipping a dangerous goods. The HazMat fee will be charged to your UPS/DHL/FedEx collect account or added to the invoice unless the package is shipped via Ground service. Ship by air in Excepted Quantity (each bottle), which is up to 1g/1mL for class 6.1 packing group I or II, and up to 25g/25ml for all other HazMat items.

Type HazMat fee for 500 gram (Estimated)
Excepted Quantity USD 0.00
Limited Quantity USD 15-60
Inaccessible (Haz class 6.1), Domestic USD 80+
Inaccessible (Haz class 6.1), International USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic USD 100+
Accessible (Haz class 3, 4, 5 or 8), International USD 200+
Candesartan cilexetil/坎地沙坦酯 化学结构 CAS号：145040-37-5
Candesartan cilexetil/坎地沙坦酯 化学结构
CAS号：145040-37-5
Candesartan cilexetil/坎地沙坦酯 3D分子结构
CAS号：145040-37-5
Candesartan cilexetil/坎地沙坦酯 化学结构 CAS号：145040-37-5
Candesartan cilexetil/坎地沙坦酯 3D分子结构 CAS号：145040-37-5
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Candesartan cilexetil/坎地沙坦酯 纯度/质量文件 产品仅供科研

货号：A259269 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

全球学术期刊中引用的产品

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Candesartan cilexetil/坎地沙坦酯 生物活性

靶点

  • RAAS

    Ang II receptor, IC50:0.26 nM
描述 Candesartan Cilexetil (CC) is a potent, highly selective, angiotensin II type 1 (AT1) blocker receptor. CC was effective in lowering BP(blood pressure) in diabetic and non-diabetic hypertensive patients[3]. At a dosage of up to 32 mg/day candesartan cilexetil demonstrated greater antihypertensive efficacy than losartan 50 or 100 mg/day[4]. A single oral dose of candesartan cilexetil at 0.3 mg/kg reduced maximal blood pressure by about 25 mm Hg, and the antihypertensive effect of candesartan cilexetil lasted the longest, continuing for more than 1 week, without an effect on circadian rhythm[5]. In rats, Candesartan Cilexetil(TCV-116) inhibited the pressor responses to Ang I, Ang II, and Ang III without an effect on the bradykinin (BK)-induced depressor response[6].

Candesartan cilexetil/坎地沙坦酯 细胞实验

Cell Line
Concentration Treated Time Description References
Triple-negative breast cancer cells (MDA-MB-231, BT20) IC50 ~18-20μM 4 days Evaluate the effect of Candesartan cilexetil on the viability of triple-negative breast cancer cells, showing significant inhibition of cell proliferation. Genes Dis. 2022 Apr 13;10(1):267-283.
Colorectal cancer cells (HT29, HCT116, DLD1) IC50 ~15-17μM 4 days Evaluate the effect of Candesartan cilexetil on the viability of colorectal cancer cells, showing significant inhibition of cell proliferation. Genes Dis. 2022 Apr 13;10(1):267-283.
Pancreatic cancer cells (PANC1, MiaPaCa2, AsPC1) IC50 ~20μM 4 days Evaluate the effect of Candesartan cilexetil on the viability of pancreatic cancer cells, showing significant inhibition of cell proliferation. Genes Dis. 2022 Apr 13;10(1):267-283.
Caco-2 cells 5, 10, 20, 40, 80 µg/mL 24 hours To evaluate the biocompatibility of candesartan cilexetil and its formulations with Caco-2 cells. Results showed that the IC50 of free CC was 8.5 µg/mL (24 hours), while the IC50 of F7 and C1 niosomes was 29.5 µg/mL, indicating that niosomes reduced the cytotoxicity of the drug. Int J Nanomedicine. 2021 Aug 16;16:5581-5601.

Candesartan cilexetil/坎地沙坦酯 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Sprague-Dawley rats Bleomycin-induced pulmonary fibrosis model Oral 10 mg/kg/day Once daily for 21 days Candesartan cilexetil significantly inhibited the increase in total protein and albumin, as well as the increase in total cells and neutrophils in BAL fluid. On day 21 candesartan cilexetil also ameliorated morphological changes and an increased amount of hydroxyproline in lung homogenates. In addition, BLM increased the expression of transforming growth factor (TGF)-β1 in BAL fluid on day 7; this increase was significantly reduced by candesartan cilexetil. Thorax. 2004 Jan;59(1):31-8
New Zealand White rabbits Atherosclerosis model Oral gavage 0.5 mg/kg/d Once daily for 8 weeks Candesartan attenuated the degree of atherosclerosis, reduced the frequency of plaque disruption and thrombosis, decreased macrophage accumulation within the plaque, and increased collagen deposition. Circulation. 2004 Oct 5;110(14):2060-5
NSG mice Pancreatic cancer (PANC1) and colorectal cancer (HT29) xenograft models Oral gavage 100 mg/kg Daily administration for the duration of the experiment Evaluate the inhibitory effect of Candesartan cilexetil on tumor growth, showing significant reduction in tumor volume without affecting body weight. Genes Dis. 2022 Apr 13;10(1):267-283.
Male KKAy diabetic mice Diabetic model Mixed in diet 0.005% 3 weeks Comparison of the effects of candesartan cilexetil and azilsartan on vascular function in diabetic mice. Candesartan cilexetil did not significantly improve acetylcholine-induced endothelium-dependent relaxation, whereas azilsartan did. Cardiovasc Diabetol. 2014 Jan 31;13:30
Sprague Dawley rats Hypertension model Oral 50 mg/kg Single dose To evaluate the oral absolute bioavailability of candesartan cilexetil niosomes. Results showed that the bioavailability of F7-SMCC and C1-SMCC was 36.4% and 37.46%, respectively, significantly higher than that of free candesartan cilexetil (6.23%). Int J Nanomedicine. 2021 Aug 16;16:5581-5601.
UM-HET3 male mice Genetically heterogeneous mouse model Oral 30 ppm Continuous administration starting at 8 months of age Tested the effect of candesartan cilexetil on lifespan; results showed no significant effect on lifespan in either male or female mice Aging Cell. 2021 May;20(5):e13328

Candesartan cilexetil/坎地沙坦酯 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
NCT00319202 Glucose Intolerance ... 展开 >> Obesity 收起 << Phase 4 Terminated(Difficulties in com... 展开 >>pleting the required sample size) 收起 << - Colombia ... 展开 >> Fundación Cardiovascular de Colombia Floridablanca, Santander, Colombia, 10000 收起 <<
NCT01062451 Methamphetamine Dependence ... 展开 >> Methamphetamine Abuse Substance Abuse 收起 << Phase 1 Active, not recruiting December 2018 United States, Texas ... 展开 >> Michael E. DeBakey VA Medical Center Houston, Texas, United States, 77030 收起 <<
NCT00526279 - Completed - Korea, Republic of ... 展开 >> Research Site Seoul, Jongro-gu, Korea, Republic of Research Site Seoul, Kangnam-gu, Korea, Republic of Research Site Seoul, Songpa-gu, Korea, Republic of 收起 <<

Candesartan cilexetil/坎地沙坦酯 参考文献

[1]Shirai K, Watanabe K, et al. Effects of angiotensin-II receptor blocker candesartan cilexetil in rats with dilated cardiomyopathy. Mol Cell Biochem. 2005 Jan;269(1-2):137-42.

[2]See S, Stirling AL. Candesartan cilexetil: an angiotensin II-receptor blocker. Am J Health Syst Pharm. 2000 Apr 15;57(8):739-46.

[3]Féghali RE, Nisse-Durgeat S, Asmar R. Effect of candesartan cilexetil on diabetic and non-diabetic hypertensive patients: meta-analysis of five randomized double-blind clinical trials. Vasc Health Risk Manag. 2007;3(1):165-71. PMID: 17583187; PMCID: PMC1994048.

[4]Easthope SE, Jarvis B. Candesartan cilexetil: an update of its use in essential hypertension. Drugs. 2002;62(8):1253-87. doi: 10.2165/00003495-200262080-00016. PMID: 12010090.

[5]Inada Y, Ojima M, Kanagawa R, Misumi Y, Nishikawa K, Naka T. Pharmacologic properties of candesartan cilexetil--possible mechanisms of long-acting antihypertensive action. J Hum Hypertens. 1999 Jan;13 Suppl 1:S75-80. doi: 10.1038/sj.jhh.1000749. PMID: 10076925.

[6]Pfeffer MA, Swedberg K, Granger CB, Held P, McMurray JJ, Michelson EL, Olofsson B, Ostergren J, Yusuf S, Pocock S; CHARM Investigators and Committees. Effects of candesartan on mortality and morbidity in patients with chronic heart failure: the CHARM-Overall programme. Lancet. 2003 Sep 6;362(9386):759-66. doi: 10.1016/s0140-6736(03)14282-1. Erratum in: Lancet. 2009 Nov 21-2009 Nov 27;(9703):1744. PMID: 13678868.

Candesartan cilexetil/坎地沙坦酯 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.64mL

0.33mL

0.16mL

8.19mL

1.64mL

0.82mL

16.38mL

3.28mL

1.64mL

Candesartan cilexetil/坎地沙坦酯 技术信息

CAS号145040-37-5
分子式C33H34N6O6
分子量 610.66
SMILES Code O=C(C1=C2N(CC3=CC=C(C4=CC=CC=C4C5=NNN=N5)C=C3)C(OCC)=NC2=CC=C1)OC(OC(OC6CCCCC6)=O)C
MDL No. MFCD00871371
别名 坎地沙坦西酯 ;TCV-116; Candesartan M1 Cilexetil
运输蓝冰
InChI Key GHOSNRCGJFBJIB-UHFFFAOYSA-N
Pubchem ID 2540
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: 50 mg/mL(81.88 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 Cilexetil | 145040-37-5 | TCV-116 | TCV116 | TCV 116 | Angiotensin II receptor Inhibitor | GPCR/G Protein | Apoptosis | Angiotensin Receptor | Apoptosis | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Candesartan cilexetil/坎地沙坦酯 纯度/质量文件 | Candesartan cilexetil/坎地沙坦酯 生物活性 | Candesartan cilexetil/坎地沙坦酯 临床数据 | Candesartan cilexetil/坎地沙坦酯 参考文献 | Candesartan cilexetil/坎地沙坦酯 实验方案 | Candesartan cilexetil/坎地沙坦酯 技术信息

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