MedChemExpress -Model Azilsartan -147403-03-0

FromMedChemExpress LLC (MCE)

Azilsartan (TAK-536) is an orally active, potent, selective and specific angiotensin II type 1 receptor (AT1) antagonist. Azilsartan induces ROS formation and apoptosis in HepG2 cells. Azilsartan shows neuroprotective and anticancer activity. Azilsartan can be used for hypertension and stroke research[1][2][3][4][5].

Azilsartan

MCE China：Azilsartan

Brand：MedChemExpress (MCE)

Cat. No.HY-14914

CAS：147403-03-0

Synonyms：TAK-536

Purity：99.51%

Storage：Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year

Shipping：Room temperature in continental US; may vary elsewhere.

Description：Azilsartan (TAK-536) is an orally active, potent, selective and specific angiotensin II type 1 receptor (AT1) antagonist. Azilsartan induces ROS formation and apoptosis in HepG2 cells. Azilsartan shows neuroprotective and anticancer activity. Azilsartan can be used for hypertension and stroke research.

In Vitro：Azilsartan (0-200 μM, 0-72 h) decreases the viability of HepG2 cells[5]. Azilsartan (100 μM, 24 h) induces apoptosis in HepG2 cells[5]. Azilsartan inhibits the specific binding of 125I-Sar1-Ile8-AII to human angiotensin type 1 receptors with an IC50 of 2.6 nM[3]. Azilsartan potently inhibits aortic endothelial and vascular cell proliferation in the absence of exogenous Ang II supplementation[5]. 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[1].

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[2]. Azilsartan (0-2 mg/kg, Oral gavage, once daily for 21 days) lowers blood pressure and basal plasma insulin concentration[2]. Azilsartan (2 and 4 mg/kg; PO, daily for 9 days) offers protection against ischemia induced secondary brain injury[4].

IC50 & Target：AT1 Receptor

References：

[1]. Kajiya T, et al. Molecular and cellular effects of azilsartan: a new generation angiotensin II receptor blocker. J Hypertens. 2011 Dec;29(12):2476-83. [Content Brief]

[2]. Zhao M, et al. Azilsartan treatment improves insulin sensitivity in obese spontaneously hypertensive Koletsky rats. Diabetes Obes Metab. 2011 Dec;13(12):1123-9. [Content Brief]

[3]. Ojima M, et al. In vitro antagonistic properties of a new angiotensin type 1 receptor blocker, azilsartan, in receptor binding and function studies. J Pharmacol Exp Ther. 2011 Mar;336(3):801-8. [Content Brief]

[4]. Gupta V, et al. Neuroprotective potential of azilsartan against cerebral ischemic injury: Possible involvement of mitochondrial mechanisms. Neurochem Int. 2020 Jan;132:104604. [Content Brief]

[5]. Ahmadian E, et al. Novel angiotensin receptor blocker, azilsartan induces oxidative stress and NFkB-mediated apoptosis in hepatocellular carcinoma cell line HepG2. Biomed Pharmacother. 2018 Mar;99:939-946. [Content Brief]

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