[CAS NO. 863031-21-4] Azilsartan Medoxomil

Name: Azilsartan Medoxomil
Brand: Arctom Scientific
SKU: SLK-S3057

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PRODUCTS SPECIFICATIONS [863031-21-4]

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Catalog

SLK-S3057

Brand

Selleck

CAS

863031-21-4

DESCRIPTION [863031-21-4]

Overview

MDL	-
Molecular Weight	568.53
Molecular Formula	C30H24N4O8
SMILES	C(N1C=2C(N=C1OCC)=CC=CC2C(OCC=3OC(=O)OC3C)=O)C4=CC=C(C=C4)C5=C(C=CC=C5)C=6NC(=O)ON6

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	1.7589 mL	8.7946 mL	17.5892 mL
5 mM	0.3518 mL	1.7589 mL	3.5178 mL
10 mM	0.1759 mL	0.8795 mL	1.7589 mL
50 mM	0.0352 mL	0.1759 mL	0.3518 mL

Description

Azilsartan Medoxomil (TAK-491) is a potent antagonist, inhibits the , with an of 2.6 nM, exhibits >10,000-fold selectivity over AT2.

Targets

AT1 receptor ^[1]

2.6 nM

In vitro

Azilsartan medoxomil is a prodrug, which is rapidly converted to the active moiety, azilsartan (TAK-536), by ester hydrolysis in the gut and plasma during absorption after oral administration. Azilsartan selectively blocks the binding of angiotensin II to the AT1 (angiotensin II type 1) receptors found in the vascular smooth muscle and the adrenal gland, thereby promoting vasodilation and a decrease in the effects of aldosterone. Azilsartan is a highly selective antagonist to the AT1 receptor, with an IC50 of 2.6 nM, exhibiting a >10,000-fold affinity for the AT1 receptor compared with the AT2 receptor, and has not shown affinity for other cardiac receptors or ion channels. The inhibitory effect of Azilsartan persists after washout of the free compound (IC50 value of 7.4 nM). Azilsartan also inhibits the accumulation of angiotensin II -induced inositol 1-phosphate (IP1) in the cell-based assay with an IC50 value of 9.2 nM, and this effect is resistant to washout (IC50 value of 81.3 nM).

References

[1] Ojima M, et al. J Pharmacol Exp Ther, 2011, 336(3), 801-808.
[2] Zaiken K, et al. Clin Ther, 2011, 33(11), 1577-1589.

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-, (5-methyl-2-oxo-1,3-dioxol-4-yl)methyl ester

Azilsartan medoxomil

TAK 491

(5-Methyl-2-oxo-1,3-dioxol-4-yl)methyl 2-ethoxy-1-[[2′-(5-oxo-4,5-dihydro-1,2,4-oxadiazol-3-yl)biphenyl-4-yl]methyl]-1H-benzimidazole-7-carboxylate

Edarbi

(5-Methyl-2-oxo-1,3-dioxol-4-yl)methyl 2-ethoxy-3-[[4-[2-(5-oxo-2H-1,2,4-oxadiazol-3-yl)phenyl]phenyl]methyl]benzimidazole-4-carboxylate

Ipreziv