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Candesartan Cilexetil

Catalog No. T2400 CAS 145040-37-5

Synonyms: TCV-116

Candesartan Cilexetil (TCV-116) is an angiotensin II receptor antagonist (IC50: 0.26 nM). After hydrolysis of candesartan cilexetil to candesartan during gastrointestinal absorption, candesartan selectively competes with angiotensin II for the binding of the angiotensin II receptor subtype 1 (AT1) in vascular smooth muscle, blocking angiotensin II-mediated vasoconstriction and inducing vasodilatation.

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Candesartan Cilexetil Chemical Structure

Candesartan Cilexetil, CAS 145040-37-5

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500 mg	In stock	$ 54.00
1 g	In stock	$ 72.00
1 mL * 10 mM (in DMSO)	In stock	$ 50.00

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Purity: 100%

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Description	Candesartan Cilexetil (TCV-116) is an angiotensin II receptor antagonist (IC50: 0.26 nM). After hydrolysis of candesartan cilexetil to candesartan during gastrointestinal absorption, candesartan selectively competes with angiotensin II for the binding of the angiotensin II receptor subtype 1 (AT1) in vascular smooth muscle, blocking angiotensin II-mediated vasoconstriction and inducing vasodilatation.
Targets&IC50	Ang II receptor:0.26 nM
In vitro	Five hours post-administration, Candesartan (1 mg/kg, orally) reduced blood pressure to a similar extent as Enalapril (10 mg/kg, orally) on both the 1st and 7th days. Candesartan significantly increased renal blood flow without altering the cardiac index. In rat myocardium with dilated cardiomyopathy (DCM), Candesartan dose-dependently improved functional markers and upregulated angiotensin (1-7), ACE2, and MAS1. Treatment with Candesartan in rats led to a reduction in various endoplasmic reticulum (ER) stress markers, apoptotic markers, and the number of apoptotic cells. Furthermore, Candesartan demonstrated a dose-dependent blockade of angiotensin-II in rats with dilated cardiomyopathy.
In vivo	The prodrug of Candesartan is absorbed through the gastrointestinal tract and activated by ester hydrolysis into Candesartan. Candesartan then blocks the effects of angiotensin II on the angiotensin II type 1 receptors.
Kinase Assay	Kinetic Methods: In a typical kinetic run, 2.00 mL of assay buffer (20 mM HEPES, 0.5 mM EDTA, 0.035% SDS, pH 7.8) and Suc-Leu-Leu-Val-Tyr-AMC in DMSO are added to a 3 mL fluorescence cuvette, and the cuvette is placed in the jacketed cell holder of a fluorescence spectrophotometer. Reaction temperature is maintained at 37℃ by a circulating water bath. After the reaction solution has reached thermal equilibrium (5 minutes), 1 μL?10 μL of the stock enzyme solution is added to the cuvette. Reaction progress is monitored by the increase in fluorescence emission at 440 nm (λex= 380 nm) that accompanies cleavage of AMC from peptide-AMC substrates.

Synonyms	TCV-116
Molecular Weight	610.66
Formula	C33H34N6O6
CAS No.	145040-37-5

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 61.1 mg/mL (100 mM)

References and Literature

1. See S, et al. Am J Health Syst Pharm,2000,7(8), 739-746. 2. Arumugam S, et al. Toxicology,2012, 291(1-3), 139-145. 3. Shirai K, et al. Mol Cell Biochem,2005, 269(1-2), 137-142. 4. Kanagawa R, et al. Jpn J Pharmacol,1997, 73(3), 185-190. 5. Kondo T, et al. Arzneimittelforschung,1996, 46(6), 594-600.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Approved Drug Library Inhibitor Library Drug Repurposing Compound Library Anti-Cancer Clinical Compound Library Anti-Cancer Drug Library Membrane Protein-targeted Compound Library CNS-Penetrant Compound Library Bioactive Compounds Library Max Anti-Cancer Compound Library NO PAINS Compound Library

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Keywords

Candesartan Cilexetil 145040-37-5 Apoptosis Endocrinology/Hormones RAAS inhibit Angiotensin Receptor TCV-116 Inhibitor TCV116 TCV 116 inhibitor

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