[CAS NO. 147403-03-0] Azilsartan

Name: Azilsartan
Brand: Arctom Scientific
SKU: SLK-S3046

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PRODUCTS SPECIFICATIONS [147403-03-0]

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Catalog

SLK-S3046

Brand

Selleck

CAS

147403-03-0

DESCRIPTION [147403-03-0]

Overview

MDL	MFCD20278186
Molecular Weight	456.45
Molecular Formula	C25H20N4O5
SMILES	C(N1C=2C(N=C1OCC)=CC=CC2C(O)=O)C3=CC=C(C=C3)C4=C(C=CC=C4)C5=NOC(=O)N5

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Concentration Volume Mass	1 mg	5 mg	10 mg
1 mM	2.1908 mL	10.9541 mL	21.9082 mL
5 mM	0.4382 mL	2.1908 mL	4.3816 mL
10 mM	0.2191 mL	1.0954 mL	2.1908 mL
50 mM	0.0438 mL	0.2191 mL	0.4382 mL

Description

Azilsartan (TAK-536) is an receptor antagonist with of 2.6 nM.

Features

A potent, orally active and specific AII receptor antagonist.

Targets

AT1 receptor ^[1]

2.6 nM

In vitro

Azilsartan inhibits the specific binding of I-Sar-Ile-AII to human angiotensin type 1 receptors. Azilsartan also inhibits the accumulation of AII-induced inositol 1-phosphate (IP1) in the cell-based assay with an IC50 value of 9.2 nM. In isolated rabbit aortic strips, Azilsartan reduces the maximal contractile response to AII with a pD'2 value of 9.9. The inhibitory effects of Azilsartan on contractile responses induced by AII persists after the strips are washed. Azilsartan suppresses the increase in plasma glucose level in the oral glucose tolerance test (OGTT) without significant change in insulin concentration and improved insulin sensitivity. In skeletal muscle, Azilsartan decreases the expression of TNF-α at doses of 0.001%. In adipose tissue, Azilsartan reduces TNF-α expression but increases the expression of adiponectin, PPARγ, C/EBα, and aP2. In cultured 3T3-L1 preadipocytes, Azilsartan enhances adipogenesis and exertes greater effects than valsartan on expression of genes encoding peroxisome proliferator-activated receptor-α (PPARα), PPARδ, leptin, adipsin, and adiponectin. Azilsartan also potently inhibits vascular cell proliferation in the absence of exogenously supplemented angiotensin II.

In vivo

In Koletsky rats, Azilsartan treatment lowers blood pressure, basal plasma insulin concentration and the homeostasis model assessment of insulin resistance index, and inhibited over-increase of plasma glucose and insulin concentrations during oral glucose tolerance test. Azilsartan downregulates 11β-hydroxysteroid dehydrogenase type 1 expression.

References

[1] Ojima M, et al. J Pharmacol Exp Ther, 2011, 336(3), 801-808.
[2] Iwai M, et al. Am J Hypertens, 2007, 20(5), 579-586.
[3] Kajiya T, et al. J Hypertens, 2011, 29(12), 2476-2483.
[4] Zhao M, et al. Diabetes Obes Metab, 2011, 13(12), 1123-1129.

Synonyms

1H-Benzimidazole-7-carboxylic acid, 1-[[2′-(2,5-dihydro-5-oxo-1,2,4-oxadiazol-3-yl)[1,1′-biphenyl]-4-yl]methyl]-2-ethoxy-

1-[[2′-(2,5-Dihydro-5-oxo-1,2,4-oxadiazol-3-yl)[1,1′-biphenyl]-4-yl]methyl]-2-ethoxy-1H-benzimidazole-7-carboxylic acid

TAK 536

2-Ethoxy-1-[[2′-(4,5-dihydro-5-oxo-1,2,4-oxadiazol-3-yl)biphenyl-4-yl]methyl]benzimidazole-7-carboxylic acid

Azilsartan

2-Ethoxy-1-[[2′-(5-oxo-4,5-dihydro-1,2,4-oxadiazol-3-yl)biphenyl-4-yl]methyl]-1H-benzimidazole-7-carboxylic acid

Azilva

2-Ethoxy-3-[[4-[2-(5-oxo-2H-1,2,4-oxadiazol-3-yl)phenyl]phenyl]methyl]benzimidazole-4-carboxylic acid

2-Ethoxy-1-([4-[2-(5-oxo-2,5-dihydro-1,2,4-oxadiazol-3-yl)phenyl]phenyl]methyl)-1H-1,3-benzodiazole-7-carboxylic acid