Azilsartan medoxomil

Modify Date: 2024-01-02 20:04:31

Azilsartan medoxomil Structure
Azilsartan medoxomil structure
 Common Name Azilsartan medoxomil
CAS Number 863031-21-4 Molecular Weight 568.534
Density 1.5±0.1 g/cm3 Boiling Point 748.0±70.0 °C at 760 mmHg
Molecular Formula C30H24N4O8 Melting Point N/A
MSDS N/A Flash Point 406.2±35.7 °C

 Use of Azilsartan medoxomil


Azilsartan medoxomil(TAK 491) is an orally administered angiotensin II receptor type 1 antagonist with IC50 of 0.62 nM, which used in the treatment of adults with essential hypertension. IC50 Value: 0.62 nM [2]Target: AT1 receptorin vitro: In aortic endothelial cells, azilsartan inhibited cell proliferation at concentrations as low as 1 μmol/l, whereas valsartan showed little or no antiproliferative effects at concentrations below 10 μmol/l. Antiproliferative effects of azilsartan were also observed in cells lacking AT1 receptors[1].in vivo: Oral administration of 0.1-3 mg/kg olmesartan medoxomil reduced blood pressure; however, only the two highest doses significantly reduced blood pressure 24h after dosing. ED(25) values were 0.41 and 1.3 mg/kg for azilsartan medoxomil and olmesartan medoxomil, respectively [2]. Over a longer treatment period of 24 weeks, azilsartan medoxomil showed sustained BP-lowering efficacy, with the reduction in 24-hour mean SBP at week 24 significantly greater with azilsartan medoxomil 40 or 80 mg once daily than with valsartan 320 mg once daily. Mean reductions from baseline in mean clinic SBP and DBP as well as DBP by ABPM were also significantly greater with azilsartan medoxomil 40 or 80 mg once daily than with valsartan[3]. In 4 randomized controlled trials (3 published to date), azilsartan medoxomil/chlorthalidone 40 mg/12.5 mg and 40 mg/25 mg reduced blood pressure (BP) significantly more than comparators did, including an approximately 5-mm Hg greater BP reduction than olmesartan medoxomil/hydrochlorothiazide 40 mg/25 mg and azilsartan medoxomil/hydrochlorothiazide [4].Clinical trial: Effect of Azilsartan on Aldosterone in Post-menopausal Females . Phase not specified

 Names

Name azilsartan medoxomil
Synonym More Synonyms

 Azilsartan medoxomil Biological Activity

Description Azilsartan medoxomil(TAK 491) is an orally administered angiotensin II receptor type 1 antagonist with IC50 of 0.62 nM, which used in the treatment of adults with essential hypertension. IC50 Value: 0.62 nM [2]Target: AT1 receptorin vitro: In aortic endothelial cells, azilsartan inhibited cell proliferation at concentrations as low as 1 μmol/l, whereas valsartan showed little or no antiproliferative effects at concentrations below 10 μmol/l. Antiproliferative effects of azilsartan were also observed in cells lacking AT1 receptors[1].in vivo: Oral administration of 0.1-3 mg/kg olmesartan medoxomil reduced blood pressure; however, only the two highest doses significantly reduced blood pressure 24h after dosing. ED(25) values were 0.41 and 1.3 mg/kg for azilsartan medoxomil and olmesartan medoxomil, respectively [2]. Over a longer treatment period of 24 weeks, azilsartan medoxomil showed sustained BP-lowering efficacy, with the reduction in 24-hour mean SBP at week 24 significantly greater with azilsartan medoxomil 40 or 80 mg once daily than with valsartan 320 mg once daily. Mean reductions from baseline in mean clinic SBP and DBP as well as DBP by ABPM were also significantly greater with azilsartan medoxomil 40 or 80 mg once daily than with valsartan[3]. In 4 randomized controlled trials (3 published to date), azilsartan medoxomil/chlorthalidone 40 mg/12.5 mg and 40 mg/25 mg reduced blood pressure (BP) significantly more than comparators did, including an approximately 5-mm Hg greater BP reduction than olmesartan medoxomil/hydrochlorothiazide 40 mg/25 mg and azilsartan medoxomil/hydrochlorothiazide [4].Clinical trial: Effect of Azilsartan on Aldosterone in Post-menopausal Females . Phase not specified
Related Catalog
References

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

[2]. Kusumoto K, Igata H, Ojima M, Antihypertensive, insulin-sensitising and renoprotective effects of a novel, potent and long-acting angiotensin II type 1 receptor blocker, azilsartan medoxomil, in rat and dog models.

[3]. Perry CM. Azilsartan medoxomil: a review of its use in hypertension. Clin Drug Investig. 2012 Sep 1;32(9):621-39.

[4]. Pierini D, Anderson KV. Azilsartan medoxomil/chlorthalidone: a new fixed-dose combination antihypertensive. Ann Pharmacother. 2013 May;47(5):694-703.

 Chemical & Physical Properties

Density 1.5±0.1 g/cm3
Boiling Point 748.0±70.0 °C at 760 mmHg
Molecular Formula C30H24N4O8
Molecular Weight 568.534
Flash Point 406.2±35.7 °C
Exact Mass 568.159424
PSA 155.59000
LogP 5.73
Vapour Pressure 0.0±2.5 mmHg at 25°C
Index of Refraction 1.680
Storage condition -20℃

 Synthetic Route

 Synonyms

Azilsartan kamedoxomil
(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
(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-benzo[d]imidazole-7-carboxylate
TAK 491
azilsartanum medoxomilum
Azilsartan
(5-Methyl-2-oxo-1,3-dioxol-4-yl)methyl 2-ethoxy-1-{[2'-(5-oxo-2,5-dihydro-1,2,4-oxadiazol-3-yl)-4-biphenylyl]methyl}-1H-benzimidazole-7-carboxylate
(5-methyl-2-oxo-1,3-dioxol-4-yl)methyl ester of 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
UNII-LL0G25K7I2
Azilsartan medoxomil
Azilsartan (medoxomil)
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
Edarbi
[14C]-Azilsartan medoxomil
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Related Compounds: More...
Azilsartan medoxomil monopotassium
863031-24-7
Azilsartan mepixetil
1596357-16-2
Azilsartan mopivabil
2271428-31-8
Azilsartan Impurity
1675221-59-6
Azilsartan Impurity
859843-08-6
Azilsartan Impurity
1863930-34-0
Azilsartan D5
1346599-45-8
Azilsartan-d5 Methyl Ester
1794766-42-9
Azilsartan
147403-03-0
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