Home GPCR & G Protein Angiotensin Receptor antagonist Candesartan For research use only.

Candesartan

Synonyms: CV-11974

Candesartan is an angiotensin II receptor antagonist with IC50 of 0.26 nM.

Candesartan Chemical Structure

Candesartan Chemical Structure

CAS: 139481-59-7

Selleck's Candesartan has been cited by 16 Publications

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Purity & Quality Control

Batch: S157802 DMSO] 94 mg/mL] false] Ethanol] 16 mg/mL] false] Water] Insoluble] false Purity: 99.52%
99.52

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Biological Activity

Description Candesartan 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
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]
Kinase Assay 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 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
In Vivo
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]
Animal Research Animal Models Mouse KU-19-19 xenograft model
Dosages 10 mg/kg
Administration Gavage
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05321875 Recruiting Cardiomyopathy Dilated Cristina Avendaño Solá|Puerta de Hierro University Hospital June 2 2022 Phase 3
NCT04012307 Completed Bioequivalence Pharmtechnology LLC|Altasciences Company Inc. July 11 2019 Phase 1
NCT03017950 Completed Hypertension|Hyperlipidemias Chong Kun Dang Pharmaceutical December 2016 Phase 1
NCT03460327 Recruiting Obesity Morbid Norwegian University of Science and Technology|St. Olavs Hospital|Volvat Medisinsk Senter Stokkan|Namsos Hospital|Alesund Hospital November 2 2016 --

Chemical lnformation & Solubility

Molecular Weight 440.45 Formula

C24H20N6O3
CAS No. 139481-59-7 SDF Download Candesartan SDF
Smiles CCOC1=NC2=CC=CC(=C2N1CC3=CC=C(C=C3)C4=CC=CC=C4C5=NNN=N5)C(=O)O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 94 mg/mL ( (213.41 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 16 mg/mL

Water : Insoluble


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In vivo
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