Name | Azilsartan |
Synonyms | CS-865 AZATMint-E Azilsartan AZILSARTAN 2-Ethoxy-1-[[2'-(4,5-dihydro-5-oxo-1,2,4-oxadiazol-3-yl)biphenyl-4-yl]methyl]benzimidazole-7-carboxylic acid 2-Ethoxy-1-{[2′-(5-oxo-4,5-dihydro-1,2,4-oxadiazol-3-yl)biphenyl-4-yl]methyl}-1H-benzimidazole-7-carboxylic acid 2-Ethoxy-1-[[2'-(4,5-dihydro-5-oxo-1,2,4-oxadiazol-3-yl)biphenyl-4-yl]methyl]benzimidazole-7-carboxylic acid Azilsartan 2-ethoxy -1- {[2'-(5-oxo-4,5-dihydro -1,2,4 -oxadiazol-3-yl) biphenyl-4-yl ] methyl} -1H –benzimi[d]dazole-7-carboxylic acid 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-carboxylic acid |
CAS | 147403-03-0 |
EINECS | 808-058-6 |
InChIKey | KGSXMPPBFPAXLY-UHFFFAOYSA-N |
Molecular Formula | C25H20N4O5 |
Molar Mass | 456.45 |
Density | 1.42 |
Melting Point | 188 °C(dec.) |
Solubility | DMSO: soluble15mg/mL (clear solution) |
Appearance | powder |
Color | white to beige |
pKa | 2.05±0.10(Predicted) |
Storage Condition | Sealed in dry,2-8°C |
MDL | MFCD00916395 |
In vitro study | Azilsartan inhibits the increase in plasma glucose levels in the oral glucose tolerance test (OGTT),Azilsartan inhibits the increase in plasma glucose levels without significantly altering insulin concentrations or increasing insulin sensitivity. In skeletal muscle, the 0.001% dose of Azilsartan reduced the expression of TNF-α. In adipose tissue, Azilsartan decreased TNF-α expression, but increased adiponectin, PPARγ,C/ebα, and AP2. Azilsartan enhances adipogenesis in cultured 3T3-L1 preadipocytes, acting on the genes encoding peroxisome proliferator-activated receptor-α (PPARα),PPAR δ, leptin, lipase, and the expression of adiponectin, more effective than valsartan. Azilsartan also effectively inhibited vascular cell proliferation in the absence of exogenous supplemented angiotensin II. |
In vivo study | In Koletsky rats, Azilsartan treatment reduces blood pressure, basal plasma insulin concentration and homeostasis Pattern Assessment of insulin resistance index, and inhibits excessive increases in blood glucose and insulin concentration in the oral glucose tolerance test. Azilsartan down-regulates the expression of 11 β-hydroxysteroid dehydrogenase type 1. |
WGK Germany | 3 |