Candesartan Cilexetil

Catalog No.S2037 Synonyms: TCV-116

For research use only.

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

CAS No. 145040-37-5

Selleck's Candesartan Cilexetil has been cited by 3 Publications

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Purity & Quality Control

Choose Selective Angiotensin Receptor Inhibitors

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

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 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]

Protocol (from reference)

Solubility (25°C)

In vitro

DMSO 122 mg/mL
(199.78 mM)
Ethanol 4 mg/mL
(6.55 mM)
Water Insoluble

Chemical Information

Molecular Weight 610.66
Formula

C33H34N6O6

CAS No. 145040-37-5
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CCOC1=NC2=CC=CC(=C2N1CC3=CC=C(C=C3)C4=CC=CC=C4C5=NNN=N5)C(=O)OC(C)OC(=O)OC6CCCCC6

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Molarity Calculator

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02609711 Unknown status Drug: Candesartan cilexetil Healthy Male Subjects Ahn-Gook Pharmaceuticals Co.Ltd November 2015 Phase 1
NCT00984529 Completed -- Chronic Heart Failure AstraZeneca September 2009 --
NCT00844324 Completed Drug: Candesartan cilexetil Hypertension AstraZeneca March 2009 Phase 1
NCT00244595 Completed Drug: candsartan cilexetil Hypertension AstraZeneca September 2003 Phase 3
NCT00244634 Completed Drug: candsartan cilexetil Pediatric Hypertension AstraZeneca September 2003 Phase 3
NCT00242346 Completed Drug: candesartan cilexetil Proteinuria AstraZeneca April 2003 Phase 3

(data from https://clinicaltrials.gov, updated on 2022-01-17)

Tech Support

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Handling Instructions

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