Candesartan

製品コードS1578 バッチS157802

化学情報

	Synonyms	CV-11974	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₂₄H₂₀N₆O₃
	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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	Candesartan is an angiotensin II receptor antagonist with IC50 of 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]
特徴	Primarily used for the treatment of hypertension.

プロトコル(参考用のみ)

キナーゼアッセイ	Binding assay
キナーゼアッセイ	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

参考

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カスタマーフィードバック

: , , Sci Rep, 2015, 5:8116.

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

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

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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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