化合物 T15187 T15187

Product Introduction
Bioactivity


英文名: E-5324

描述: E-5324 is potent cholesterol acyltransferase (ACAT) inhibitor (IC50s: 44 to 190 nM).

体外活性: E-5324 inhibits the incorporation of [3H]oleate into cholesteryl [3H]oleate in a concentration-dependent manner (IC50: 0.44 μM) and it also inhibits [3H]cholesteryl ester synthesis (IC50: 0.41 μM). E-5324 displays no effect on triglyceride synthesis up to 10 μM and it also has no effect on bovine pancreatic cholesterol esterase or lecithin: cholesterol acyltransferase (LCAT) up to 10 μM [1].

体内活性: E-5324 treatment significantly decreases the wet weight and protein content. The high dose of E-5324 (0.1%) obviously decreases the surface involvement by 34% and 54% in the aortic arch and thoracic aorta, respectively. In the aortic arch, the high dose of E-5324 (0.1%) obviously reduces both cholesteryl ester and total cholesterol by 60% and 59%, respectively. The high dose of E-5324 (0.1%) markedly decreases the ACAT activities in the aortic arch and thoracic aorta by 35% and 44%, respectively. 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 [2].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

关键字: E-5324 | E5324 | E 5324

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途