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AGU661

Chemical Structure : AGU661

CAS No.: 3038861-75-2

AGU661 (AGU-661)

Catalog No.: 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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    Biological Activity

    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).

    Physicochemical Properties

    M.Wt 594.94
    Formula C28H21ClF6N4O2
    Appearance Solid
    CAS No.
    Storage
    Solide Powder
    -20°C 12 Months; 4°C 6 Months
    In Solvent
    -80°C 6 Months; -20°C 6 Months
    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

    References

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

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