Candesartan

Catalog No.S1578 Synonyms: CV-11974

Candesartan  Chemical Structure

Molecular Weight(MW): 440.45

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

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In DMSO USD 140 In stock
USD 110 In stock
USD 670 In stock
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  • In vivo effects of candesartan and valsartan in post-MI rats overexpressing adrenal barr1. (A) Trichrome-Masson's staining in myocardial cross-sections from post-MI rats overexpressing barr1 specifically in their adrenals and treated for 7 days with either vehicle or 10 mg/kg body weight/day candesartan or 40 mg/kg body weight/day irbesartan (all via drinking water). Blue denotes collagen fibers, red denotes muscle fibers, and black represents cell nuclei. Representative images are shown from 5–6 rat hearts stained per group, along with staining in sham-operated rat hearts, in which no blue staining was detectable. (B,C) Heart mRNA levels of (B) collagen I (Col1a1) and brain natriuretic peptide (BNP) (C) in these rats at the end of the 7-day drug treatments. Values for post-MI rats receiving AdGFP in their adrenals instead of Adbarr1 (i.e. not overexpressing barr1 in their adrenals) were used as reference. *, p < 0.05, vs. Candesartan (Adbarr1), n=5 rat hearts/group.

    Sci Rep, 2015, 5:8116.. Candesartan purchased from Selleck.

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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

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

Kinase Assay:[1]
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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]
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  • 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
    (Only for Reference)
Animal Research:[2]
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  • Animal Models: Mouse KU-19-19 xenograft model
  • Formulation: Saline
  • Dosages: 10 mg/kg
  • Administration: Gavage
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 88 mg/mL (199.79 mM)
Ethanol 1 mg/mL (2.27 mM)
Water Insoluble
In vivo Add solvents individually and in order:
30% propylene glycol, 5% Tween 80, 65% D5W
30 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 440.45
Formula

C24H20N6O3

CAS No. 139481-59-7
Storage powder
Synonyms CV-11974

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02047019 Withdrawn Hypertension Bayer December 2017 Phase 3
NCT02988362 Not yet recruiting Hypertension HanAll BioPharma Co., Ltd. December 2016 Phase 1
NCT02521233 Withdrawn Essential Arterial Hypertension EMS November 2016 Phase 3
NCT02521246 Withdrawn Essential Arterial Hypertension EMS November 2016 Phase 3
NCT02646982 Recruiting Mild Cognitive Impairment Emory University June 2016 Phase 2
NCT02709187 Completed Healthy Alvogen Korea March 2016 Phase 1

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID