CAY10678

Microsomal prostaglandin E synthase-1 (mPGES-1) converts the COX product PGH₂ into the biologically active PGE₂.¹ Like COX-2, the expression of mPGES-1 is induced in response to pro-inflammatory mediators, including LPS, IL-1β, and TNF-α.² CAY10678 is a benzoimidazole that potently inhibits human and rat recombinant mPGES-1 (IC₅₀ = 0.09 and 0.9 µM, respectively).³ It has minimal effects on COX-1, COX-2, PGIS, and hematopoietic PGDS at 50 μM but reduces lipocalin-type PGDS activity by 60% at this concentration.³ CAY10678 dose-dependently blocks PGE₂ synthesis in isolated cells and whole blood treated with LPS or IL-1β.³ It also dose-dependently reduces PGE₂ synthesis and cell recruitment during inflammation in mice.³

≥98%