1. Immunology/Inflammation
  2. PGE synthase
  3. AGU654

AGU654 (Compound 44) 是一种选择性 mPGES-1 抑制剂,对 mPGES-1IC50 值为 2.9 nM。此外,AGU654 通过抑制 mPGES-1,阻断由 COX-1/2 将花生四烯酸转化为前列腺素 E2 (PGE2) 的途径,从而有效缓解炎症反应、疼痛和发热症状。在活化的人单核细胞衍生巨噬细胞和人全血模型中,AGU654 能够选择性抑制由细菌外毒素诱导的 PGE2 生成,同时保留其他前列腺素的产生。AGU654 在豚鼠模型中显著缓解了发热、炎症和炎症性疼痛,表现出优异的抗炎、镇痛和退热效果。AGU654 有望成为研究炎症性疾病和疼痛的新策略。

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AGU654 Chemical Structure

AGU654 Chemical Structure

CAS No. : 3038861-74-1

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  • 生物活性

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生物活性

AGU654 (Compound 44) is a selective mPGES-1 inhibitor with an IC50 of 2.9 nM against mPGES-1. AGU654 inhibits mPGES-1 to block the pathway converting arachidonic acid into prostaglandin E2 (PGE2) by COX-1/2, thereby alleviating inflammatory responses, pain, and fever. In activated human monocyte-derived macrophages and human whole blood models, AGU654 selectively suppresses bacterial exotoxin-induced PGE2 production while preserving the production of other prostaglandins. In guinea pig models, AGU654 significantly alleviates fever, inflammation, and inflammatory pain, exhibiting excellent anti-inflammatory, analgesic, and antipyretic effects. AGU654 holds promise as a strategy for studying inflammatory diseases and pain[1].

分子量

580.91

Formula

C27H19ClF6N4O2

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

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参考文献
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
AGU654
目录号:
HY-169430
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