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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Purity & Documentation Purity:
>98% (HPLC)
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
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M.Wt
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594.94
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Formula
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C28H21ClF6N4O2
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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2-chloro-N-(4-(5-(trifluoromethyl)-1H-benzo[d]imidazol-2-yl)phenyl)-5-((1-(trifluoromethyl)cyclobutane-1-carboxamido)methyl)benzamide
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References
1. Dahlke P, et al. Mol Pharm. 2025 Nov 3;22(11):6803-6815.
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