Name | Azilsartan medoxomil |
Synonyms | CS-306 TAK 491 Azilsaran medoxomil Azilsartan Medoxomil Azilsartan medoxomil 1-[[2'-(2,5-Dihydro-5-oxo-1,2,4-oxadiazol-3-yl)[1,1'-biphenyl]-4-yl]methyl]-2-ethoxy-1H-benzim (5-methyl-2-oxo-1,3-dioxol-4-yl)methyl 2-ethoxy-3-[[4-[2-(5-oxo-4H-1,2,4-+oxadiazol-3-yl)phenyl]phenyl]methyl]benzimidazole-4-carboxylate 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 (5-methyl-2-oxo-1,3-dioxol-4-yl)methyl ester 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 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 |
CAS | 863031-21-4 |
EINECS | 1308068-626-2 |
InChI | InChI:1S/C30H24N4O8/c1-3-38-28-31-23-10-6-9-22(27(35)39-16-24-17(2)40-30(37)41-24)25(23)34(28)15-18-11-13-19(14-12-18)20-7-4-5-8-21(20)26-32-29(36)42-33-26/h4-14H,3,15-16H2,1-2H3,(H,32,33,36) |
Molecular Formula | C30H24N4O8 |
Molar Mass | 568.53 |
Density | 1.45 |
Melting Point | 160-161oC |
Solubility | DMSO (Slightly), Methanol (Slightly, Heated, Sonicated) |
Appearance | Solid |
Color | White to Light Beige |
pKa | 6.99±0.20(Predicted) |
Storage Condition | Refrigerator |
In vitro study | Azilsartan medoxomil is a prodrug that can be rapidly converted to the active moiety in the intestine and plasma by ester hydrolysis, azilsartan (TAK-536). In vascular smooth muscle and adrenal glands, Azilsartan selectively blocks the binding of angiotensin II to AT1 (type 1 angiotensin II) receptors, thereby promoting vasodilation and reducing the effect of aldosterone. Azilsartan is a highly selective antagonist of the AT1 receptor with an IC50 of 2.6 nM, has more than 10,000-fold affinity for the AT1 receptor as compared to the AT2 receptor, and has no affinity for other cardiac receptors or ion channels. The inhibitory effect of Azilsartan was still present after washing with free compound (IC50 value of 7.4 nM). Azilsartan also inhibited angiotensin II-induced accumulation of inositol -1-phosphate (IP1) at the cellular level with an IC50 value of 9.2 nM, and this effect is resistant to washing (IC50 value of 81.3 nM). Azilsartan medoxomil is a prodrug that can be rapidly converted to the active moiety in the intestine and plasma by ester hydrolysis, azilsartan (TAK-536). In vascular smooth muscle and adrenal glands, Azilsartan selectively blocks the binding of angiotensin II to AT1 (type 1 angiotensin II) receptors, thereby promoting vasodilation and reducing the effect of aldosterone. Azilsartan is a highly selective antagonist of the AT1 receptor with an IC50 of 2.6 nM, has more than 10,000-fold affinity for the AT1 receptor as compared to the AT2 receptor, and has no affinity for other cardiac receptors or ion channels. The inhibitory effect of Azilsartan was still present after washing with free compound (IC50 value of 7.4 nM). Azilsartan also inhibited angiotensin II-induced accumulation of inositol -1-phosphate (IP1) at the cellular level with an IC50 value of 9.2 nM, and this effect is resistant to washing (IC50 value of 81.3 nM). |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 1.759 ml | 8.795 ml | 17.589 ml |
5 mM | 0.352 ml | 1.759 ml | 3.518 ml |
10 mM | 0.176 ml | 0.879 ml | 1.759 ml |
5 mM | 0.035 ml | 0.176 ml | 0.352 ml |