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 No. 145040-37-5

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Candesartan Cilexetil Related Products

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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