Azilsartan-d4

Modify Date: 2024-01-20 20:51:30

Azilsartan-d4 Structure
Azilsartan-d4 structure
Common Name Azilsartan-d4
CAS Number 1794817-45-0 Molecular Weight 460.475
Density 1.4±0.1 g/cm3 Boiling Point N/A
Molecular Formula C25H16D4N4O5 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of Azilsartan-d4


Azilsartan-d4 is the deuterium labeled Azilsartan[1]. Azilsartan is an orally active, potent, selective and specific angiotensin II type 1 receptor (AT1) antagonist. Azilsartan induces ROS formation and apoptosis in HepG2 cells. Azilsartan shows neuroprotective and anticancer activity. Azilsartan can be used for hypertension and stroke research[2][3][4][5][6].

 Names

Name 2-Ethoxy-1-{[2'-(5-oxo-4,5-dihydro-1,2,4-oxadiazol-3-yl)(2,3,5,6-2H4)-4-biphenylyl]methyl}-1H-benzimidazole-7-carboxylic acid
Synonym More Synonyms

 Azilsartan-d4 Biological Activity

Description Azilsartan-d4 is the deuterium labeled Azilsartan[1]. Azilsartan is an orally active, potent, selective and specific angiotensin II type 1 receptor (AT1) antagonist. Azilsartan induces ROS formation and apoptosis in HepG2 cells. Azilsartan shows neuroprotective and anticancer activity. Azilsartan can be used for hypertension and stroke research[2][3][4][5][6].
Related Catalog
In Vitro Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].
References

[1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019 Feb;53(2):211-216.  

[2]. Kajiya T, et al. Molecular and cellular effects of azilsartan: a new generation angiotensin II receptor blocker. J Hypertens. 2011 Dec;29(12):2476-83.  

[3]. Zhao M, et al. Azilsartan treatment improves insulin sensitivity in obese spontaneously hypertensive Koletsky rats. Diabetes Obes Metab. 2011 Dec;13(12):1123-9.  

[4]. Ojima M, et al. In vitro antagonistic properties of a new angiotensin type 1 receptor blocker, azilsartan, in receptor binding and function studies. J Pharmacol Exp Ther. 2011 Mar;336(3):801-8.  

[5]. Gupta V, et al. Neuroprotective potential of azilsartan against cerebral ischemic injury: Possible involvement of mitochondrial mechanisms. Neurochem Int. 2020 Jan;132:104604.  

[6]. Ahmadian E, et al. Novel angiotensin receptor blocker, azilsartan induces oxidative stress and NFkB-mediated apoptosis in hepatocellular carcinoma cell line HepG2. Biomed Pharmacother. 2018 Mar;99:939-946.  

 Chemical & Physical Properties

Density 1.4±0.1 g/cm3
Molecular Formula C25H16D4N4O5
Molecular Weight 460.475
Exact Mass 460.168488
LogP 4.21
Index of Refraction 1.695
Storage condition 2-8°C

 Synonyms

1H-Benzimidazole-7-carboxylic acid, 1-[[2'-(4,5-dihydro-5-oxo-1,2,4-oxadiazol-3-yl)[1,1'-biphenyl]-4-yl-2,3,5,6-d4]methyl]-2-ethoxy-
2-Ethoxy-1-{[2'-(5-oxo-4,5-dihydro-1,2,4-oxadiazol-3-yl)(2,3,5,6-2H4)-4-biphenylyl]methyl}-1H-benzimidazole-7-carboxylic acid