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Azilsartan

Cat. No. M2106
Azilsartan Structure
Synonym:

TAK-536

Size Price Availability Quantity
25mg USD 100 In stock
50mg USD 150 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
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.

Chemical Information
Molecular Weight 456.45
Formula C25H20N4O5
CAS Number 147403-03-0
Purity >98%
Solubility DMSO 90 mg/mL
Storage at -20°C
References

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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  Catalog
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Keywords: Azilsartan, TAK-536 supplier, Angiotensin Receptor, inhibitors

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