Candesartan cilexetil

Modify Date: 2024-01-03 00:38:07

Candesartan cilexetil Structure
Candesartan cilexetil structure
Common Name Candesartan cilexetil
CAS Number 145040-37-5 Molecular Weight 610.660
Density 1.4±0.1 g/cm3 Boiling Point 843.3±75.0 °C at 760 mmHg
Molecular Formula C33H34N6O6 Melting Point 168-170?C
MSDS Chinese USA Flash Point 463.8±37.1 °C
Symbol GHS08 GHS09
GHS08, GHS09
Signal Word Warning

 Use of Candesartan cilexetil


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].

 Names

Name Candesartan cilexetil
Synonym More Synonyms

 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
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.

 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

 Safety Information

Symbol GHS08 GHS09
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

 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%

 Articles29

More 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...

 Synonyms

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)
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