NS 398

NS-398 (CAS 123653-11-2) is an orally bioavailable nonsteroidal anti-inflammatory compound, functioning as a selective inhibitor of cyclooxygenase-2 (COX-2) in inflammatory tissues and exhibiting minimal inhibitory activity against cyclooxygenase-1 (COX-1) in gastric tissues. Additionally, it mediates anti-inflammatory and antipyretic effects by decreasing the production of prostaglandins associated with inflammation.

In biochemical and cellular assays, NS-398 selectively inhibits COX-2 enzymatic activity with an IC50 value of 3.8 μM, tested against in vitro enzyme preparations and cell-based inflammatory models. It shows negligible inhibition of COX-1 activity at concentrations up to 100 μM in cultured gastric cell lines. NS-398 can also reduce the synthesis of prostaglandin E2 and suppress pro-inflammatory cytokine expression in lipopolysaccharide-stimulated macrophages.

In pharmacological and biomedical research, NS-398 is widely used for the study of pain relief, fever reduction, and elucidation of COX-2-related signaling pathways. Its selectivity for COX-2 over COX-1 makes it a valuable tool for dissecting the distinct roles of cyclooxygenase isoforms in inflammation, tissue injury, and related pathologies.