受注:045-509-1970 |
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Synonyms | CV-11974 | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C24H20N6O3 |
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分子量 | 440.45 | CAS No. | 139481-59-7 | |
Solubility (25°C)* | 体外 | 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. |
製品説明 | Candesartan is an angiotensin II receptor antagonist with IC50 of 0.26 nM. |
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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] |
特徴 | Primarily used for the treatment of hypertension. |
キナーゼアッセイ | Binding assay | |
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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 ℃. | ||
細胞アッセイ | 細胞株 | KU-19-19 cells |
濃度 | 10 μM | |
反応時間 | 48 hours | |
実験の流れ | 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 | |
動物実験 | 動物モデル | Mouse KU-19-19 xenograft model |
投薬量 | 10 mg/kg | |
投与方法 | Gavage |
, , Sci Rep, 2015, 5:8116.
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 |
Alterations in vascular function by syncytiotrophoblast extracellular vesicles via lectin-like oxidized low-density lipoprotein receptor-1 in mouse uterine arteries [ Clin Sci (Lond), 2018, 132(21):2369-2381] | PubMed: 30352791 |
長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
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