AGU654 | mPGES-1 inhibitor | Probechem Biochemicals

Chemical Structure : AGU654

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AGU654 (AGU-654)

货号: 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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生物&药学活性

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.

物理化学性质&存储条件

分子量	580.92
分子式	C27H19ClF6N4O2
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-benzimidazol-2-yl)phenyl)-5-((1-(trifluoromethyl)cyclopropane-1-carboxamido)methyl)benzamide

参考文献

1. Ergül AG, et al. J Med Chem. 2024 Dec 2. doi: 10.1021/acs.jmedchem.4c01883.

AGU654 (AGU-654)

生物&药学活性

物理化学性质&存储条件

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AGU654 (AGU-654)

生物&药学活性

物理化学性质&存储条件

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