NB-598: a potent competitive inhibitor of squalene epoxidase.

作者: M Horie , Y Tsuchiya , M Hayashi , Y Iida , Y Iwasawa

DOI: 10.1016/S0021-9258(17)44716-8

关键词:

摘要: NB-598, (E)N-ethyl-N-(6,6-dimethyl-2-hepten-4-ynyl)-3-[(3,3'-bith iophen-5-yl)methoxy]benzene-methanamine, was found to inhibit human microsomal squalene epoxidase (from Hep G2 cells) in a competitive manner. NB-598 inhibited cholesterol synthesis from [14C]acetate dose dependently cells and increased the intracellular radioactivity of squalene. A single oral administration rats. Moreover, multiple dogs decreased serum total low density lipoprotein levels levels. After termination treatment, reduced returned their control values.

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