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.
|Related Angiotensin Receptor Products|
A-779 is a specific antagonist of G-protein coupled receptor (Mas receptor).
Angiotensin (1-7) is a synthetic heptapeptide identical to endogenous angiotensin-(1-7), inhibits purified canine angiotensin converting enzyme (ACE) activity with an IC50 of 0.65 μM.
Losartan is an angiotensin II receptor antagonist, competing with the binding of angiotensin II to AT1 receptors with IC50 of 20 nM.
EMA401 (also known as Olodanrigan and PD-126055) is a highly selective angiotensin AT2 antagonist.
Tranilast is an antiallergic agent.
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2017 AbMole BioScience. All Rights Reserved.