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Candesartan Cilexetil

🥰Excellent
Catalog No. T2400Cas No. 145040-37-5
Alias TCV-116

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.

Candesartan Cilexetil

Candesartan Cilexetil

🥰Excellent
Purity: 100%
Catalog No. T2400Alias TCV-116Cas No. 145040-37-5
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.
Pack SizePriceAvailabilityQuantity
500 mg$54In Stock
1 g$72In Stock
1 mL x 10 mM (in DMSO)$66In Stock
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Purity:100%
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Product Introduction

Bioactivity
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.
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.
AliasTCV-116
Chemical Properties
Molecular Weight610.66
FormulaC33H34N6O6
Cas No.145040-37-5
SmilesC(N1C=2C(N=C1OCC)=CC=CC2C(OC(OC(OC3CCCCC3)=O)C)=O)C4=CC=C(C=C4)C5=C(C=CC=C5)C=6NN=NN6
Relative Density.1.37 g/cm3
Storage & Solubility Information
StoragePowder: -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.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM1.6376 mL8.1879 mL16.3757 mL81.8786 mL
5 mM0.3275 mL1.6376 mL3.2751 mL16.3757 mL
10 mM0.1638 mL0.8188 mL1.6376 mL8.1879 mL
20 mM0.0819 mL0.4094 mL0.8188 mL4.0939 mL
50 mM0.0328 mL0.1638 mL0.3275 mL1.6376 mL
100 mM0.0164 mL0.0819 mL0.1638 mL0.8188 mL

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