Candesartan
(Synonyms: 坎地沙坦; CV 11974) 目录号 : GC16978
Candesartan是一种口服血管紧张素II 1型受体（AT1R）阻断剂，IC50值为0.26nM。
Cas No.:139481-59-7
Sample solution is provided at 25 µL, 10mM.
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Candesartan is an oral blocker of AngII type-1 receptors (AT1R), with an IC50 value of 0.26nM[1]. Candesartan can inhibit the viral activity of SARS-CoV-2 with an IC50 value of 5.944μM[2]. Candesartan has been widely used to inhibit renal vasoconstriction in rodents, blocking AT1A and AT1B receptors in rodent renal resistance vessels[3].
In vitro, Candesartan treatment at 20µM for 24h significantly induced apoptosis and inhibited cell migration in CT-26 and SW-480 cells [4]. Treatment of human embryonic kidney epithelial cells with 100μM Candesartan for 24h significantly reduced TNF-α-induced TGF-β and IL-6 expression and blocked TNF-α-induced ROS activation[5]. Treatment with 1μM Candesartan for 48h specifically reversed the AngII-induced decrease in miR-301b levels in rat aortic smooth muscle cells (RASMCs) and significantly reduced the AngII-induced increase in STAT3 expression[6].
In vivo, Candesartan treatment via oral administration at a dose of 2mg/kg/day for 28 days significantly reduced tumor volume and inhibited tumor angiogenesis in the murine xenograft model of bladder cancer[7]. Intraperitoneal administration of Candesartan (10mg/kg/day) for 7 days significantly reduced pathological neovascularization and improved capillary perfusion in a mouse model of ischemic retinopathy[8]. Oral administration of Candesartan at a dose of 1mg/kg/day for 21 days significantly improved insulin resistance, hepatic steatosis, and dyslipidemia in the high-fat diet (HFD)-fed mice[9].
References:
[1] Abreu Diaz A M, Drumeva G O, Petrenyov D R, et al. Synthesis of the novel AT1 receptor tracer [18F] fluoropyridine–candesartan via click chemistry[J]. Acs Omega, 2020, 5(32): 20353-20362.
[2] Alnajjar R, Mostafa A, Kandeil A, et al. Molecular docking, molecular dynamics, and in vitro studies reveal the potential of angiotensin II receptor blockers to inhibit the COVID-19 main protease[J]. Heliyon, 2020, 6(12).
[3] Ruan X, Purdy K E, Oliverio M I, et al. Effects of candesartan on angiotensin II-induced renal vasoconstriction in rats and mice[J]. Journal of the American Society of Nephrology: JASN, 1999, 10: S202-7.
[4] Tabatabai E, Khazaei M, Asgharzadeh F, et al. Inhibition of angiotensin II type 1 receptor by candesartan reduces tumor growth and ameliorates fibrosis in colorectal cancer[J]. Excli Journal, 2021, 20: 863.
[5] Yu Y, Jiang H, Niu Y, et al. Candesartan inhibits inflammation through an angiotensin II type 1 receptor independent way in human embryonic kidney epithelial cells[J]. Anais da Academia Brasileira de Ciências, 2019, 91(02): e20180699.
[6] Zhang L, Yang F, Yan Q. Candesartan ameliorates vascular smooth muscle cell proliferation via regulating miR-301b/STAT3 axis[J]. Human Cell, 2020, 33(3): 528-536.
[7] Kosugi M, Miyajima A, Kikuchi E, et al. Angiotensin II type 1 receptor antagonist candesartan as an angiogenic inhibitor in a xenograft model of bladder cancer[J]. Clinical cancer research, 2006, 12(9): 2888-2893.
[8] Shanab A Y, Elshaer S L, El-Azab M F, et al. Candesartan stimulates reparative angiogenesis in ischemic retinopathy model: role of hemeoxygenase-1 (HO-1)[J]. Angiogenesis, 2015, 18(2): 137-150.
[9] Lee J W, Gu H O, Jung Y, et al. Candesartan, an angiotensin-II receptor blocker, ameliorates insulin resistance and hepatosteatosis by reducing intracellular calcium overload and lipid accumulation[J]. Experimental & molecular medicine, 2023, 55(5): 910-925.
Candesartan是一种口服血管紧张素II 1型受体（AT1R）阻断剂，IC50值为0.26nM[1]。Candesartan可抑制SARS-CoV-2的病毒活性（IC50=5.944μM）[2]。Candesartan广泛应用于啮齿类动物模型中抑制肾血管收缩，阻断肾阻力血管中的AT1A和AT1B受体[3]。
在体外，20µM的Candesartan处理CT-26和SW-480细胞24小时可显著诱导凋亡并抑制细胞迁移[4]。100μM的Candesartan处理人胚胎肾上皮细胞24小时能降低TNF-α诱导的TGF-β和IL-6表达，并阻断TNF-α引发的ROS激活[5]。1μM的Candesartan处理大鼠主动脉平滑肌细胞（RASMCs）48小时可特异性逆转AngII引起的miR-301b水平下降，并显著抑制AngII诱导的STAT3表达增加[6]。
在体内，膀胱癌异种移植小鼠模型每日口服Candesartan（2mg/kg/day；持续28天）可显著减小肿瘤体积并抑制肿瘤血管生成[7]。缺血性视网膜病变小鼠模型每日腹腔注射10mg/kg剂量的Candesartan（持续7天）能减少病理性新生血管并改善毛细血管灌注[8]。高脂饮食（HFD）小鼠每日口服1mg/kg剂量的Candesartan（持续21天）可显著改善胰岛素抵抗、肝脏脂肪变性和血脂异常[9]。
| Cell experiment [1]: | |
Cell lines | CT-26 cells |
Preparation Method | CT-26 cells were cultured in RPMI 1640 medium supplemented with 10% fetal bovine serum and 1% penicillin/streptomycin at 37.0°C and 5% CO2 humidity. CT-26 cells (1×103) were seeded in 96-well plates and treated with various concentrations of Candesartan (100, 200, 400, 600, 800, and 1000μM) for 24 hours. After cell treatment, 20μl of MTT solution (5mg/ml) was transferred to each well, and the culture plates were incubated at 37°C for 4h to investigate the production of formazan crystals by living cells. Subsequently, the medium was replaced with DMSO (100μl), and the optical density was then measured at 545-630nm. |
Reaction Conditions | 100, 200, 400, 600, 800, and 1000μM; 24h |
Applications | Candesartan significantly inhibited the viability of CT-26 cells in a dose-dependent manner. |
| Animal experiment [2]: | |
Animal models | Nude athymic BALB/c mice |
Preparation Method | Nude athymic BALB/c mice of 6 weeks of age with an average weight of 20g were maintained under standard conditions. KU-19-19 cells (2×106 cells) suspended in 50μl Matrigel were subcutaneously implanted into the flank of each nude mouse. The mice were divided into 2 groups, with about 20 mice in each group. Starting on the day of cell implantation, mice were injected with 2mg/kg Candesartan daily via gavage, and tumors were measured twice weekly. The tumor volume (V) was calculated according to the formula V = AB2/2, where A is the maximum diameter and B is the diameter perpendicular to A. Mice were sacrificed on day 28, and subcutaneous tumors were harvested for analysis. |
Dosage form | 2mg/kg/day for 28 days; p.o. |
Applications | Candesartan treatment significantly reduced tumor volume and inhibited tumor angiogenesis in mice. |
References: | |
| Cas No. | 139481-59-7 | SDF | |
| 别名 | 坎地沙坦; CV 11974 | ||
| 化学名 | 2-ethoxy-3-[[4-[2-(2H-tetrazol-5-yl)phenyl]phenyl]methyl]benzimidazole-4-carboxylic acid | ||
| Canonical SMILES | CCOC1=NC2=CC=CC(=C2N1CC3=CC=C(C=C3)C4=CC=CC=C4C5=NNN=N5)C(=O)O | ||
| 分子式 | C24H20N6O3 | 分子量 | 440.45 |
| 溶解度 | ≥ 14.65mg/mL in DMSO, ≥ 3.45 mg/mL in EtOH with ultrasonic | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.2704 mL | 11.352 mL | 22.7041 mL |
| 5 mM | 454.1 μL | 2.2704 mL | 4.5408 mL |
| 10 mM | 227 μL | 1.1352 mL | 2.2704 mL |
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| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
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| % DMSO % % Tween 80 % saline | ||||||||||
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2.
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