131420-84-3

DA-E 5090 is deacetylated form of E5090, is pharmacologically active metabolite of E 5090, is interleukin-1 antagonist._x000D_ DA-E 5090 is a novel inhibitor of IL-1 generation, in vitro inhibitory effects on the generation of IL-1 by human monocytes. E5090 is an orally active inhibitor of IL-1 generation, being converted in vivo into the pharmacologically active deacetylated form (DA-E5090). In vitro effects of DA-E5090 on the generation of IL-1 by human monocytes stimulated with LPS were examined. DA-E5090 inhibited both IL-1 alpha and IL-1 beta generation by human monocytes stimulated with 1 microgram/ml of LPS in a dose dependent-manner (1-10 microM), as determined by LAF assay and ELISA. Northern blotting analysis indicated that DA-E5090 inhibits transcription of IL-1 alpha and IL-1 beta m-RNAs.

DA-E 5090是一种口服有效的IL-1生成抑制剂，能在体内转化为具有药理活性的去乙酰化形式（DA-E5090）。本研究通过LPS刺激的人单核细胞检测了DA-E5090对IL-1生成的体外影响。结果显示，DA-E5090能剂量依赖性地抑制LPS刺激下的人单核细胞产生的IL-1α和IL-1β（1-10微M），这一效果通过LAF分析和ELISA确定。 Northern blotting分析表明，DA-E5090抑制了IL-1α和IL-1β mRNA的转录。