131420-84-3
131420-84-3 結(jié)構(gòu)式
應(yīng)用領(lǐng)域
用途一
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.常見(jiàn)問(wèn)題列表
概述
DA-E 5090是一種口服有效的IL-1生成抑制劑，能在體內(nèi)轉(zhuǎn)化為具有藥理活性的去乙酰化形式（DA-E5090）。本研究通過(guò)LPS刺激的人單核細(xì)胞檢測(cè)了DA-E5090對(duì)IL-1生成的體外影響。結(jié)果顯示，DA-E5090能劑量依賴性地抑制LPS刺激下的人單核細(xì)胞產(chǎn)生的IL-1α和IL-1β（1-10微M），這一效果通過(guò)LAF分析和ELISA確定。 Northern blotting分析表明，DA-E5090抑制了IL-1α和IL-1β mRNA的轉(zhuǎn)錄。