Azilsartan阿齐沙坦,147403-03-0

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Azilsartan

CAS No. : 147403-03-0

MCE 国际站：Azilsartan

产品活性：Azilsartan (TAK-536) 是一种口服有效的、选择性和特异性的血管紧张素 Ⅱ 1 型受体 (AT1) 拮抗剂。Azilsartan 诱导 HepG2 细胞 ROS 形成和细胞凋亡 (apoptosis)。Azilsartan 具有神经保护和抗癌活性。Azilsartan 可以用于高血压和中风研究。

研究领域：GPCR/G Protein  |  Metabolic Enzyme/Protease  |  Immunology/Inflammation  |  NF-κB  |  Apoptosis

作用靶点：Angiotensin Receptor  |  Reactive Oxygen Species  |  Apoptosis

In Vitro: Azilsartan (0-200 μM, 0-72 h) decreases the viability of HepG2 cells.
Azilsartan (100 μM, 24 h) induces apoptosis in HepG2 cells.
Azilsartan inhibits the specific binding of ¹²⁵I-Sar¹-Ile⁸-AII to human angiotensin type 1 receptors with an IC₅₀ of 2.6 nM.
Azilsartan potently inhibits aortic endothelial and vascular cell proliferation in the absence of exogenous Ang II supplementation.
Azilsartan enhances adipogenesis and exerted greater effects than Valsartan (HY-18204) on expression of genes encoding peroxisome proliferator-activated receptor-α (PPARα), PPARδ, leptin, adipsin, and adiponectin.

In Vivo: Azilsartan (0-3 mg/kg, Oral gavage, once daily for 5 days) decreases SBP (systolic blood pressure) in obese Koletsky rats at 2 mg/kg.
Azilsartan (0-2 mg/kg, Oral gavage, once daily for 21 days) lowers blood pressure and basal plasma insulin concentration.
Azilsartan (2 and 4 mg/kg; PO, daily for 9 days) offers protection against ischemia induced secondary brain injury.

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