Chemical Structure : AGU654
CAS No.:
3038861-74-1
AGU654
(AGU-654)
Catalog No.: PC-23561Not For Human Use, Lab Use Only.
AGU654 is a potent, selective microsomal prostaglandin E2 synthase 1 (mPGES-1) inhibitor with IC50 of 2.9 nM in cell-free assays.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
AGU654 is a potent, selective microsomal prostaglandin E2 synthase 1 (mPGES-1) inhibitor with IC50 of 2.9 nM in cell-free assays.
AGU654 shows no activities of isolated COX-1/2 or 5-LOX in cell-free assays, nor FLAP in human neutrophils at 1 uM.
AGU654 blocks mPGES-1 in a reversible manner.
AGU654 selectively inhibits PGE2 formation in human macrophages and in human whole blood, without reducing the generation of other COX/LOX-derived LM.
AGU654 (10 and 30 mg/kg, oral) shows anti-inflammatory and analgesic effect in the carrageenan-induced paw edema model of guinea pig.
Physicochemical Properties
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M.Wt
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580.92
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Formula
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C27H19ClF6N4O2
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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-benzimidazol-2-yl)phenyl)-5-((1-(trifluoromethyl)cyclopropane-1-carboxamido)methyl)benzamide
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References
1. Ergül AG, et al. J Med Chem. 2024 Dec 2. doi: 10.1021/acs.jmedchem.4c01883.
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