Candesartan Cilexetil

Catalog No.S2037 Synonyms: TCV-116

Candesartan Cilexetil Chemical Structure

Molecular Weight(MW): 610.66

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

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In DMSO USD 130 In stock
USD 97 In stock
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Cited by 2 Publications

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  • (b) ASMCs were incubated with 1 µM candesartan or 10 µM PD123319 for 60 min before stimulation with 0.1 µM Ang II for 24 h in six-well plates. Western blot was used for analyses of the levels of MMP-2 expression in cell lysates. Top panel: Graphs show the relative MMP-2 protein levels normalized to GAPDH relative to control. Bottom panel: Ratio of MMP-2/GAPDH protein expression from a representative Western blot experiment. Shown are mean ± SEM of three individual experiments. **P < 0.01 vs. untreated control cells; ##P < 0.01 vs. cells treated with Ang II

    Exp Biol Med (Maywood), 2015, 240(12):1564-71.. Candesartan Cilexetil purchased from Selleck.

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Biological Activity

Description Candesartan Cilexetil 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

Solubility (25°C)

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

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 610.66
Formula

C33H34N6O6

CAS No. 145040-37-5
Storage powder
in solvent
Synonyms TCV-116

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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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID