Home GPCR & G Protein Angiotensin Receptor antagonist Candesartan (CV-11974)

Candesartan (CV-11974)

Catalog No.S1578

For research use only.

Candesartan (CV-11974) is an angiotensin II receptor antagonist with IC50 of 0.26 nM.

Candesartan (CV-11974) Chemical Structure

CAS No. 139481-59-7

Selleck's Candesartan (CV-11974) has been cited by 13 publications

Purity & Quality Control

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Biological Activity

Description Candesartan (CV-11974) is an angiotensin II receptor antagonist with IC50 of 0.26 nM.
Features Primarily used for the treatment of hypertension.
Targets
AT1 receptor [1]
0.26 nM
In vitro

Candesartan binds with high specificity to the angiotensin II AT1 receptors in CHO-AT1 cells with K−1 of 0.001 min−1. [1] Candesartan does not affect cell viability or proliferation but increases the expression of VEGF and interleukin-8 in the cultured medium of KU-19-19 cells. [2] Candesartan (0.1 nM) could reduce the maximal contractile response to angiostensin II by approximately 50%. [3]

In vivo Candesartan (10 mg/kg) inhibits the growth of engrafted tumors and reduces the microvessel density and VEGF expression in a mouse KU-19-19 xenograft model [2] Candesartan (0.5 mg/kg) decreases blood pressure and inhibits AT1 binding in the subfornical organ (SFO), paraventricular nucleus of the hypothalamus (PVN), nucleus of the solitary tract (NTS) and area postrema (AP) in WKY rats. [4] Candesartan (0.3 mg/kg) pretreatment decreases the infarct area by 31% in adult spontaneously hypertensive rats, reduces the CBF decrease at the peripheral area of ischemia and the cortical volume of severe ischemic lesion. [5]

Protocol (from reference)

Kinase Assay:[1]
  • Binding assay:

    Cells are plated in 24-well plates and cultured until confluence. Before the experiment, the cells are washed three times with 0.5 mL per well of DMEM at room temperature. After removal of the medium, 400 μL binding DMEM is added and the plate is then left for 15 min at 37 ℃. For saturation binding assays cells are incubated with increasing concentrations [3H]Candesartan (final concentrations between 0.15 nM and 15 nM) in a final volume of 0.5 mL at 37 ℃ for 5 min to 180 min. For competition binding assays 50 μL of buffer or 50 μL of buffer containing increasing concentrations of unlabelled Candesartan is added. After 30 min, 50 μL of buffer containing [3H]Candesartan (final concentration 1.1 nM) or [3H]Candesartan (final concentration 1.0 nM) is added, and the cells are further incubated for 30 min at 37 ℃.
Cell Research:[2]
  • Cell lines: KU-19-19 cells
  • Concentrations: 10 μM
  • Incubation Time: 48 hours
  • Method: KU-19-19 cells are seeded at a cell density of 2 × 104 per well in 96-well plates and allowed to grow overnight. Then the cells are treated with various concentrations of Candesartan for various periods of time. Cell viability is determined by the Alamar Blue assay to examine the cytotoxicity and antiproliferative effect of candesartan. The absorbance value of each well is determined in a microplate reade
Animal Research:[2]
  • Animal Models: Mouse KU-19-19 xenograft model
  • Dosages: 10 mg/kg
  • Administration: Gavage

Solubility (25°C)

In vitro

 DMSO 88 mg/mL
(199.79 mM)
Water Insoluble
Ethanol '1 mg/mL

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
2% DMSO+40% PEG 300+2% Tween 80+ddH2O
For best results, use promptly after mixing.

 10mg/mL

Chemical Information

Molecular Weight 440.45
Formula

C24H20N6O3
CAS No. 139481-59-7
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CCOC1=NC2=CC=CC(=C2N1CC3=CC=C(C=C3)C4=CC=CC=C4C5=NNN=N5)C(=O)O

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

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% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04012307 Completed Drug: Candesartan Cilexetil 32mg|Drug: Atacand® PROTECT Bioequivalence Pharmtechnology LLC|Altasciences Company Inc. July 11 2019 Phase 1
NCT03017950 Completed Drug: CKD-330|Drug: D086|Drug: CKD-330 + D086 Hypertension|Hyperlipidemias Chong Kun Dang Pharmaceutical December 2016 Phase 1
NCT03460327 Recruiting Drug: Candesartan Obesity Morbid Norwegian University of Science and Technology|St. Olavs Hospital|Volvat Medisinsk Senter Stokkan|Namsos Hospital|Alesund Hospital November 2 2016 --
NCT02609711 Unknown status Drug: Candesartan cilexetil Healthy Male Subjects Ahn-Gook Pharmaceuticals Co.Ltd November 2015 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-01-17)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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