Candesartan cilexetil

Names

[ Name ]:
Candesartan cilexetil

[Synonym ]:
1-{[(Cyclohexyloxy)carbonyl]oxy}ethyl 2-ethoxy-1-{[2'-(1H-tetrazol-5-yl)-4-biphenylyl]methyl}-1H-benzimidazole-7-carboxylate
Candesartan cilexetil
1-{[(cyclohexyloxy)carbonyl]oxy}ethyl 2-ethoxy-1-{[2'-(2H-tetrazol-5-yl)biphenyl-4-yl]methyl}-1H-benzimidazole-7-carboxylate
2-Ethoxy-1-[[2'-(1H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]methyl]-1H-benzimidazole-7-carboxylic Acid 1-[[(Cyclohexyloxy)carbonyl]oxy]ethyl Ester
UNII:R85M2X0D68
MFCD00871371
1-{[(Cyclohexyloxy)carbonyl]oxy}ethyl 2-ethoxy-1-{[2'-(1H-tetrazol-5-yl)biphenyl-4-yl]methyl}-1H-benzimidazole-7-carboxylate
1H-Benzimidazole-7-carboxylic acid, 2-ethoxy-1-[[2'-(1H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]methyl]-, 1-[[(cyclohexyloxy)carbonyl]oxy]ethyl ester
Candesartan (Cilexetil)

Biological Activity

[Description]:

Candesartan Cilexetil (TCV-116) is an angiotensin II receptor antagonist used mainly for the treatment of hypertension.Target: Type-1 angiotensin II receptorCandesartan is generally well tolerated and significantly reduced cardiovascular deaths and hospital admissions for heart failure. Ejection fraction or treatment at baseline did not alter these effects [1]. In rats, TCV-116 inhibited the pressor responses to Ang I, Ang II, and Ang III without an effect on the bradykinin (BK)-induced depressor response. In SHR, the antihypertensive effect of TCV-116 (10 mg/kg) was larger than the maximum antihypertensive effect of enalapril and was not intensified by combination with enalapril. TCV-116 is more effective than enalapril in reducing blood pressure in SHR and 1K, 1C-HR, and that the BK- and/or prostaglandin-potentiating effect of enalapril contributes little to its antihypertensive mechanism in SHR [2].

[Related Catalog]:

Signaling Pathways >> GPCR/G Protein >> Angiotensin Receptor

Research Areas >> Cardiovascular Disease

[References]

[1]. Pfeffer, M.A., et al., Effects of candesartan on mortality and morbidity in patients with chronic heart failure: the CHARM-Overall programme. Lancet, 2003. 362(9386): p. 759-66.

[2]. Wada, T., et al., Comparison of the antihypertensive effects of the new angiotensin II (AT1) receptor antagonist candesartan cilexetil (TCV-116) and the angiotensin converting enzyme inhibitor enalapril in rats. Hypertens Res, 1996. 19(2): p. 75-81.

[Related Small Molecules]

Chemical & Physical Properties

[ Density]:
1.4±0.1 g/cm3

[ Boiling Point ]:
843.3±75.0 °C at 760 mmHg

[ Melting Point ]:
168-170?C

[ Molecular Formula ]:
C₃₃H₃₄N₆O₆

[ Molecular Weight ]:
610.660

[ Flash Point ]:
463.8±37.1 °C

[ Exact Mass ]:
610.253967

[ PSA ]:
143.34000

[ LogP ]:
7.79

[ Vapour Pressure ]:
0.0±3.1 mmHg at 25°C

[ Index of Refraction ]:
1.667

[ Storage condition ]:
-20°C Freezer

MSDS

Click to get detail MSDS

Safety Information

[ Symbol ]:

GHS08, GHS09

[ Signal Word ]:
Warning

[ Hazard Statements ]:
H361-H400

[ Precautionary Statements ]:
P280

[ Hazard Codes ]:
Xn: Harmful;

[ Risk Phrases ]:
R20/21/22

[ Safety Phrases ]:
26-36

[ RIDADR ]:
NONH for all modes of transport

[ HS Code ]:
2933990090

Synthetic Route

Click to get detail synthetic route

Precursor & DownStream

Precursor

DownStream

Customs

[ HS Code ]: 2933990090

[ Summary ]:
2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

Articles

Development and characterization of mixed niosomes for oral delivery using candesartan cilexetil as a model poorly water-soluble drug.

AAPS PharmSciTech 16(1) , 108-17, (2015)

The aim of this study was to prepare candesartan cilexetil-loaded niosomes and mixed niosomes to enhance the aqueous solubility of the drug, thus improving its oral bioavailability. The formulations w...

Use of compounded dispersing media for extemporaneous pediatric syrups with candesartan cilexetil and valsartan.

Acta. Pharm. 64(4) , 463-74, (2014)

Available tablets or capsules for adults are often used to prepare extemporaneously formulated medicines appropriate for children. The most acceptable drug forms in pediatric population are oral liqui...

Hepatic, intestinal, renal, and plasma hydrolysis of prodrugs in human, cynomolgus monkey, dog, and rat: implications for in vitro-in vivo extrapolation of clearance of prodrugs.

Drug Metab. Dispos. 42(9) , 1522-31, (2014)

Hydrolysis plays an important role in metabolic activation of prodrugs. In the current study, species and in vitro system differences in hepatic and extrahepatic hydrolysis were investigated for 11 pr...