Home GPCR & G Protein Angiotensin Receptor antagonist Candesartan Cilexetil For research use only.

Candesartan Cilexetil

Synonyms: TCV-116

Candesartan Cilexetil (TCV-116) is an angiotensin II receptor antagonist with IC50 of 0.26 nM, used in the treatment of hypertension.

Candesartan Cilexetil Chemical Structure

Candesartan Cilexetil Chemical Structure

CAS: 145040-37-5

Selleck's Candesartan Cilexetil has been cited by 4 Publications

1 Customer Review

Purity & Quality Control

Batch: Purity: 99.98%
99.98

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Biological Activity

Description Candesartan Cilexetil (TCV-116) is an angiotensin II receptor antagonist with IC50 of 0.26 nM, used in the treatment of hypertension.
Targets
Ang II receptor [1]
0.26 nM
In vitro
In vitro Candesartan blocks the effects of angiotensin II at the angiotensin II type 1 (AT1) receptor. Candesartan cilexetil is a prodrug that is activated to candesartan by ester hydrolysis during gastrointestinal absorption. [1]
In Vivo
In vivo Candesartan improves the functional markers in a dose-dependent manner and also upregulates Ang (1-7), ACE2 and mas1 in the myocardium of DCM rats. Candesartan reduces various ER stress and apoptosis markers and the number apoptotic cells in the Candesartan treated rats. [2] Candesartan cilexetil shows angiotensin-II blocking action in a dose-dependent manner in rats with dilated cardiomyopathy. Candesartan cilexetil reduces the left ventricular end-diastolic pressure and heart weight/body weight ratio, the area of myocardial fibrosis and expressions of transforming growth factor-beta1 and collagen-III mRNA. [3] Candesartan cilexetil (1 mg/kg, p.o.) and enalapril (10 mg/kg, p.o.) reduces blood pressure to the same extent 5 hours after administration on the 1st and the 7th day. Candesartan cilexetil significantly increases renal blood flow without any changes in the cardiac index. TCV-116 and enalapril also tends to increase splanchnic blood flow following the 1st dose but not the 7th dose. [4] Candesartan cilexetil is absorbed from the small intestine and hydrolyzed completely to the pharmacologically active metabolite M-I during absorption process. [5]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02609711 Unknown status
Healthy Male Subjects
Ahn-Gook Pharmaceuticals Co.Ltd
 November 2015 Phase 1
NCT00984529 Completed
Chronic Heart Failure
AstraZeneca
 September 2009 --
NCT00844324 Completed
Hypertension
AstraZeneca
 March 2009 Phase 1
NCT00244595 Completed
Hypertension
AstraZeneca
 September 2003 Phase 3
NCT00244634 Completed
Pediatric Hypertension
AstraZeneca
 September 2003 Phase 3
NCT00242346 Completed
Proteinuria
AstraZeneca
 April 2003 Phase 3

Chemical Information & Solubility

Molecular Weight 610.66 Formula

C33H34N6O6
CAS No. 145040-37-5 SDF Download Candesartan Cilexetil SDF
Smiles CCOC1=NC2=CC=CC(=C2N1CC3=CC=C(C=C3)C4=CC=CC=C4C5=NNN=N5)C(=O)OC(C)OC(=O)OC6CCCCC6
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 122 mg/mL ( (199.78 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 4 mg/mL

Water : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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