| Name | Candesartan Cilexetil |
| Description | Candesartan Cilexetil (TCV-116) is an angiotensin II receptor antagonist (IC50: 0.26 nM). Upon hydrolysis to candesartan during gastrointestinal absorption, it selectively competes with angiotensin II for binding to the angiotensin II receptor subtype 1 (AT1) in vascular smooth muscle, blocking angiotensin II-mediated vasoconstriction and inducing vasodilatation. |
| 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. |
| 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. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 70 mg/mL (114.63 mM), Sonication is recommended.
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| Keywords | inhibit | Angiotensin Receptor | Apoptosis | Inhibitor | TCV116 | Candesartan Cilexetil | TCV 116 |
| Inhibitors Related | Stavudine | Sodium 4-phenylbutyrate | Tributyrin |
| Related Compound Libraries | Membrane Protein-targeted Compound Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Inhibitor Library | Anti-Cancer Approved Drug Library | Bioactive Compounds Library Max | Anti-Cancer Drug Library |
United States
