For research use only.
Catalog No.S2037 Synonyms: TCV-116
CAS No. 145040-37-5
Candesartan Cilexetil (TCV-116) is an angiotensin II receptor antagonist with IC50 of 0.26 nM, used in the treatment of hypertension.
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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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Choose Selective Angiotensin Receptor Inhibitors
|Description||Candesartan Cilexetil (TCV-116) is an angiotensin II receptor antagonist with IC50 of 0.26 nM, used in the treatment of hypertension.|
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. 
|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.  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.  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.  Candesartan cilexetil is absorbed from the small intestine and hydrolyzed completely to the pharmacologically active metabolite M-I during absorption process. |
-  See S, et al. Am J Health Syst Pharm,?000,?7(8), 739-746.
-  Arumugam S, et al. Toxicology,?012, 291(1-3), 139-145.
-  Shirai K, et al. Mol Cell Biochem,?005, 269(1-2), 137-142.
|In vitro||DMSO||122 mg/mL (199.78 mM)|
|Ethanol||4 mg/mL (6.55 mM)|
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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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