AGU654

AGU654 (Compound 44) is a selective mPGES-1 inhibitor with an IC50 of 2.9 nM against mPGES-1. AGU654 inhibits mPGES-1 to block the pathway converting arachidonic acid into prostaglandin E2 (PGE2) by COX-1/2, thereby alleviating inflammatory responses, pain, and fever. In activated human monocyte-derived macrophages and human whole blood models, AGU654 selectively suppresses bacterial exotoxin-induced PGE2 production while preserving the production of other prostaglandins. In guinea pig models, AGU654 significantly alleviates fever, inflammation, and inflammatory pain, exhibiting excellent anti-inflammatory, analgesic, and antipyretic effects. AGU654 holds promise as a strategy for studying inflammatory diseases and pain[1].

Product Specifications

CAS Number

[3038861-74-1]

UNSPSC

12352005

Target

PGE synthase

Type

Reference compound

Related Pathways

Immunology/Inflammation

Field of Research

Neurological Disease

Assay Protocol

https://www.medchemexpress.com/agu654.html

Smiles

O=C(NC1=CC=C(C2=NC3=CC(C(F)(F)F)=CC=C3N2)C=C1)C4=CC(CNC(C5(C(F)(F)F)CC5)=O)=CC=C4Cl

Molecular Formula

C27H19ClF6N4O2

Molecular Weight

580.91

References & Citations

[1]Ergül AG, et al. Novel Benzimidazole Derivatives as Potent Inhibitors of Microsomal Prostaglandin E2 Synthase 1 for the Potential Treatment of Inflammation, Pain, and Fever. J Med Chem. 2024 Dec 12;67 (23) :21143-21162.