AGU654 is a Potent mPGES-1 Inhibitor for the Potential Treatment of Inflammation, Pain, and Fever. AGU654 demonstrated remarkable selectivity for mPGES-1 (IC50 = 2.9 nM) over COX-1, COX-2, 5-LOX, and FLAP, along with excellent bioavailability. Metabololipidomics analysis with activated human monocyte-derived macrophages and human whole blood revealed that AGU654 selectively suppresses PGE2 production triggered by bacterial exotoxins while sparing other prostaglandins. Furthermore, in vivo studies showed that AGU654 significantly alleviated fever, inflammation, and inflammatory pain in preclinical guinea pig models, suggesting that it could be an effective strategy for managing inflammatory diseases.
MedKoo Cat#: 128194
Name: AGU654
CAS#: N/A
Chemical Formula: C27H19ClF6N4O2
Exact Mass: 580.1101
Molecular Weight: 580.92
Elemental Analysis: C, 55.83; H, 3.30; Cl, 6.10; F, 19.62; N, 9.64; O, 5.51
The following data is based on the product molecular weight 580.92 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
