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Azilsartan

Cat. No. M2106
Azilsartan Structure
Synonym:

TAK-536

Size Price Availability Quantity
10mg USD 42  USD42 In stock
25mg USD 80  USD80 In stock
50mg USD 120  USD120 In stock
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Quality Control
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.

Product Citations
Protocol
Cell Experiment
Cell lines
Preparation method
Concentrations
Incubation time
Animal Experiment
Animal models male Wister rats, aged 6–8 weeks
Formulation Na-CMC
Dosages 3.5 mg/kg, 7 mg/kg
Administration p.o.
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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 456.45
Formula C25H20N4O5
CAS Number 147403-03-0
Purity 99.72%
Solubility DMSO 25 mg/mL
Storage at -20°C
References

[1] Yahya M Alzahrani, et al. Saudi Pharm J. Possible combined effect of perindopril and Azilsartan in an experimental model of dementia in rats

[2] Kajiya T, et al. J Hypertens. Molecular and cellular effects of azilsartan: a new generation angiotensin II receptor blocker.

[3] Zhao M, et al. Diabetes Obes Metab. Azilsartan treatment improves insulin sensitivity in obese spontaneously hypertensive Koletsky rats.

[4] Ojima M, et al. J Pharmacol Exp Ther. In vitro antagonistic properties of a new angiotensin type 1 receptor blocker, azilsartan, in receptor binding and function studies.

[5] Iwai M, et al. Am J Hypertens. TAK-536, a new AT1 receptor blocker, improves glucose intolerance and adipocyte differentiation.

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  Catalog
Abmole Inhibitor Catalog 2017




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

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