Candesartan

Catalog No.S1578 Batch:S157802

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Technical Data

Formula

C24H20N6O3
Molecular Weight 440.45 CAS No. 139481-59-7
Solubility (25°C)* In vitro DMSO 94 mg/mL (213.41 mM)
Ethanol 16 mg/mL (36.32 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description Candesartan is an angiotensin II receptor antagonist with IC50 of 0.26 nM.
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]
Features Primarily used for the treatment of hypertension.

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 Assay:[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 Study:[2]
  • Animal Models

    Mouse KU-19-19 xenograft model

  • Dosages

    10 mg/kg

  • Administration

    Gavage

Customer Product Validation

, , Sci Rep, 2015, 5:8116.

Selleck's Candesartan has been cited by 17 publications

Propafenone facilitates mitochondrial-associated ferroptosis and synergizes with immunotherapy in melanoma [ J Immunother Cancer, 2024, 12(11)e009805] PubMed: 39581704
A Repurposed Drug Screen for Compounds Regulating Aquaporin 5 Stability in Lung Epithelial Cells [ Front Pharmacol, 2022, 13:828643] PubMed: 35145418
Maternal Angiotensin Increases Placental Leptin in Early Gestation via an Alternative Renin-Angiotensin System Pathway: Suggesting a Link to Preeclampsia [ Hypertension, 2021, 77(5):1723-1736] PubMed: 33775117
Angiotensin II Decreases Endothelial Nitric Oxide Synthase PhosphorylationviaAT1R Nox/ROS/PP2A Pathway [ Front Physiol, 2020-, Volume 11] PubMed: None
Role of Lectin-like Oxidized LDL Receptor-1 and Syncytiotrophoblast Extracellular Vesicles in the Vascular Reactivity of Mouse Uterine Arteries During Pregnancy [ Sci Rep, 2020, 8;10(1):6046] PubMed: 32269313
Angiotensin II Decreases Endothelial Nitric Oxide Synthase Phosphorylation via AT1R Nox/ROS/PP2A Pathway [ Front Physiol, 2020, 11:566410] PubMed: 33162896
Angiotensin II down-regulates transferrin receptor 1 and ferroportin 1 expression in Neuro-2a cells via activation of type-1 receptor. [ Neurosci Lett, 2020, 716:134684] PubMed: 31830506
Degradation of SARS-CoV-2 receptor ACE2 by tobacco carcinogen-induced Skp2 in lung epithelial cells [ bioRxiv, 2020, 10.1101/2020.10.13.337774] PubMed: None
Placental CX3CL1 is Deregulated by Angiotensin II and Contributes to a Pro-Inflammatory Trophoblast-Monocyte Interaction. [ Int J Mol Sci, 2019, 20(3)] PubMed: 30717334
Roles of I2PP2A in the downregulation of eNOS Ser1177 phosphorylation by angiotensin II-activated PP2A. [ Biochem Biophys Res Commun, 2019, 516(3):613-618] PubMed: 31239152

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.