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Candesartan cilexetil

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Chemical Structure| 145040-37-5 同义名 : 坎地沙坦西酯 ;TCV-116;Candesartan M1 Cilexetil
CAS号 : 145040-37-5
货号 : A259269
分子式 : C33H34N6O6
纯度 : 98%
分子量 : 610.66
MDL号 : MFCD00871371
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

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
动物实验配方：
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].
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 <<
实验方案
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
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.