863031-24-7
863031-24-7 structure
- Name: azilsartan kamedoxomil
- Chemical Name: azilsartan kamedoxomil
- CAS Number: 863031-24-7
- Molecular Formula: C30H23KN4O8
- Molecular Weight: 606.62
- Catalog: Signaling Pathways GPCR/G Protein Angiotensin Receptor
- Create Date: 2018-08-23 18:57:32
- Modify Date: 2026-07-01 15:24:22
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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].
| Name | azilsartan kamedoxomil |
|---|---|
| Synonyms |
UNII-WEC6I2K1FC
Azilstan MedoxoMil PotassiuM salt Azilstan Impurity 50 Potassium Salt Azilstan MedoxoMil (MonopotassiuM) Azilstan Mehtyl ester Azilstan kaMedoxoMil 1-[[2'-(2,5-Dihydro-5-oxo-1,2,4-oxadiazol-3-yl)[1,1'-biphenyl]-4-yl]methyl]-2-ethoxy-1H-benzimidazole-7-cboxylic acid (5-methyl-2-oxo-1,3-dioxol-4-yl)methyl ester potassium salt TAK 491 kamedoxomil TAK-491 Azilsartan (medoxomil monopotassium) Potassium 3-(4'-((2-ethoxy-7-(((5-methyl-2-oxo-1,3-dioxol-4-yl)methoxy)carbonyl)-1H-benzo[d]imidazol-1-yl)methyl)-[1,1'-biphenyl]-2-yl)-5-oxo-5H-1,2,4-oxadiazol-2-ide Azilstan medoxomil monopotassium Azilstan KaModoxoMil Azilstan Medoxomil Potassium TAK-491 monopotassium Azilstan kaMedoxoMil (with 5 ints.) Azilstan MedoxMil PotassuiM (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]imidazol-7-cboxylate, potassium salt AZILSTAN KAMEDOXOMIL IH (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)-[1,1'-biphenyl]-4-yl)methyl)-1H-benzo[d]imidazole-7-cboxylate, potassium salt Azilstan Impurity 45 Potassium Salt Potassium 3-{4'-[(2-ethoxy-7-{[(5-methyl-2-oxo-1,3-dioxol-4-yl)methoxy]carbonyl}-1H-benzimidazol-1-yl)methyl]-2-biphenylyl}-5-oxo-1,2,4-oxadiazol-4-ide Azilsartan kamedoxomil (USAN) Azilstan MedoxoMil (MonopotassiuM salt) Azilstan MedoxiMil PotassiuM 1H-Benzimidazole-7-carboxylic acid, 1-[[2'-(4,5-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, potassium salt (1:1) Azilstan Impurity 60 Potassium Salt 1H-BenziMidazole-7-cboxylic 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, potassiuM salt Azilsartan medoxomil monopotassium WEC6I2K1FC Azilstan Medoxomil Potassium Crude potassium,(5-methyl-2-oxo-1,3-dioxol-4-yl)methyl 2-ethoxy-3-[[4-[2-(5-oxo-1-oxa-2-aza-4-azanidacyclopent-2-en-3-yl)phenyl]phenyl]methyl]benzimidazole-4-carboxylate Azilstan KaMedoximil |
| 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]. |
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| Related Catalog | |
| References |
| Molecular Formula | C30H23KN4O8 |
|---|---|
| Molecular Weight | 606.62 |
| PSA | 155.59000 |
| LogP | 4.70520 |
| Storage condition | 2-8℃ |