Azilsartan (codenamed TAK-536) is an angiotensin II receptor antagonist used in the treatment of hypertension. Azilsartan potently inhibited vascular cell proliferation in the absence of exogenously supplemented angiotensin II. Azilsartan increased tissue glucose uptake, especially in skeletal muscle and adipose tissue. In cultured 3T3-L1 preadipocytes, azilsartan enhanced adipogenesis and exerted greater effects than valsartan on expression of genes encoding peroxisome proliferator-activated receptor-α (PPARα), PPARδ, leptin, adipsin, and adiponectin. In adipose tissue, Azilsartan (TAK-536) reduced TNF-alpha expression but increased the expression of adiponectin, PPARgamma, C/EBalpha, and aP2. In addition, azilsartan downregulated 11β-hydroxysteroid dehydrogenase type 1 expression. Azilsartan is currently in a phase IV clinical trial in the treatment of hypertension.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||DMSO 90 mg/mL|
Molecular and cellular effects of azilsartan: a new generation angiotensin II receptor blocker.
Kajiya T, et al. J Hypertens. 2011 Dec;29(12):2476-83. PMID: 21986624.
Azilsartan treatment improves insulin sensitivity in obese spontaneously hypertensive Koletsky rats.
Zhao M, et al. Diabetes Obes Metab. 2011 Dec;13(12):1123-9. PMID: 21749604.
In vitro antagonistic properties of a new angiotensin type 1 receptor blocker, azilsartan, in receptor binding and function studies.
Ojima M, et al. J Pharmacol Exp Ther. 2011 Mar;336(3):801-8. PMID: 21123673.
TAK-536, a new AT1 receptor blocker, improves glucose intolerance and adipocyte differentiation.
Iwai M, et al. Am J Hypertens. 2007 May;20(5):579-86. PMID: 17485025.
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|Angiotensin II human
Angiotensin II human is converted by Angiotensin I through removal of two C-terminal residues by the enzyme angiotensin-converting enzyme (ACE). Angiotensin II is mediated by AT1 and AT2 receptors, which are seven transmembrane glycoproteins with 30% sequence similarity.
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