141799-76-0
| 中文名称 | 141799-76-0 |
|---|---|
| 中文同义词 | 化合物 T15187;化合物 E-5324 |
| 英文名称 | E 5324 |
| 英文同义词 | E 5324;Urea, N-butyl-N'-[2-[3-(5-ethyl-4-phenyl-1H-imidazol-1-yl)propoxy]-6-methylphenyl]-;E5324,E 5324 |
| CAS号 | 141799-76-0 |
| 分子式 | C26H34N4O2 |
| 分子量 | 434.57 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 141799-76-0.mol |
| 结构式 |  |
141799-76-0 性质
| 沸点 | 637.4±55.0 °C(Predicted) |
|---|---|
| 密度 | 1.11±0.1 g/cm3(Predicted) |
| 储存条件 | Store at -20°C |
| 溶解度 | 溶于二甲基亚砜 |
| 酸度系数(pKa) | 14.20±0.46(Predicted) |
IC50: 44 to 190 nM (ACAT)
E-5324 is a potent ACAT inhibitor with IC 50 s of 44 to 190 nM in microsomes. E-5324 shows no effect on triglyceride synthesis up to 10 μM. E-5324 also has no effect on bovine pancreatic cholesterol esterase or lecithin: cholesterol acyltransferase (LCAT) up to 10 μM. E-5324 inhibits the incorporation of [ 3 H]oleate into cholesteryl [ 3 H]oleate in a concentration-dependent manner with an IC 50 of 0.44 μM. E-5324 also inhibits [ 3 H]cholesteryl ester synthesis with an IC 50 of 0.41 μM.
The areas under the cholesterol-time curves for duration of this study (AUC) for control, E-5324 0.02% and E-5324 0.1% are 104985±4411, 106096±4476 and 105231±4 348 mg×day/dL, respectively. The high dose of E-5324 (0.1%) significantly reduces the surface involvement by 34% and 54% in the aortic arch and thoracic aorta, respectively. E-5324 treatment significantly reduces the wet weight and protein content. In the aortic arch, the high dose of E-5324 (0.1%) significantly reduces both cholesteryl ester and total cholesterol by 60% and 59%, respectively. The high dose of E-5324 (0.1%) markedly reduces the ACAT activities in the aortic arch and thoracic aorta by 35% and 44%, respectively.