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AGU661

Chemical Structure : AGU661

CAS No.: 3038861-75-2

AGU661 (AGU-661)

货号: PC-25867Not For Human Use, Lab Use Only.

AGU661 (AGU-661) is a potent microsomal prostaglandin E2 synthase-1 (mPGES-1) inhibitor, inhibits the enzyme activity of mPGES-1 in microsomes with IC50 of 0.22 nM in cell-free assays.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

AGU661 (AGU-661) is a potent microsomal prostaglandin E2 synthase-1 (mPGES-1) inhibitor, inhibits the enzyme activity of mPGES-1 in microsomes with IC50 of 0.22 nM in cell-free assays.
AGU661 modulates exotoxin-induced LM formation in human macrophages.
AGU661 does not inhibit the murine ortholog of mPGES-1.
AGU661 specifically suppresses formation of PGE2 in circulating innate immune cells, but not IL-1β, IL-6, and TNFα.
AGU661 shows no inhibition of 5-LOX in cell-free and cell-based (PMNL) assays, and no effect on isolated COX-1 and COX-2.
Encapsulated AGU661 in PLGA-based solid nanoparticles revealed significantly enhanced potency in human whole blood (IC50 = 1.5 nM).

物理化学性质&存储条件

分子量 594.94
分子式 C28H21ClF6N4O2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

2-chloro-N-(4-(5-(trifluoromethyl)-1H-benzo[d]imidazol-2-yl)phenyl)-5-((1-(trifluoromethyl)cyclobutane-1-carboxamido)methyl)benzamide

参考文献

1. Dahlke P, et al. Mol Pharm. 2025 Nov 3;22(11):6803-6815.

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