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E-5324
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
E-5324图片
CAS NO:141799-76-0
规格:98%
分子量:434.57
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议

产品介绍
E-5324是一个强效的酰基辅酶A:胆固醇酰基转移酶(ACAT)抑制剂,其IC50值在44至190nM之间。
CAS:141799-76-0
分子式:C26H34N4O2
分子量:434.57
纯度:98%
存储:Store at -20°C

Background:

E-5324 is potent inhibitor of acyl-CoA:cholesterol acyltransferase (ACAT) with IC50s of 44 to 190 nM.


E-5324 is a potent ACAT inhibitor with IC50s 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 [3H]oleate into cholesteryl [3H]oleate in a concentration-dependent manner with an IC50 of 0.44 μM. E-5324 also inhibits [3H]cholesteryl ester synthesis with an IC50 of 0.41 μM[1].


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[2].


[1]. Kogushi M, et al. Effect of E5324, a novel inhibitor of acyl-CoA:cholesterol acyltransferase, on cholesteryl ester synthesis and accumulation in macrophages. Jpn J Pharmacol. 1995 Jun;68(2):191-9. [2]. Kogushi M, et al. Anti-atherosclerotic effect of E5324, an inhibitor of acyl-CoA:cholesterol acyltransferase, in Watanabe heritable hyperlipidemic rabbits. Atherosclerosis. 1996 Aug 2;124(2):203-10.