AF3442

AF3442 is a potent and selective mPGES-1 inhibitor (IC₅₀ = 0.06 μM) which reduces monocyte PGE₂ generation also in the presence of plasma proteins. AF3442 shows selectivity over other prostanoids (TXB₂, PGF_2α and 6-keto-PGF_1α). AF3442 can be used for research in analgesia^[1]. In Vitro:AF3442 (0.01-10 μM, 15 min) causes a concentration-dependent inhibition of PGE₂ generation by human recombinant mPGES-1 with an IC₅₀ of 0.06 μM^[1].
AF3442 (0.01-100 μM, 24 h) causes a concentration-dependent reduction of PGE₂ biosynthesis (IC₅₀ = 0.41 μM), while at 100 μM, the inhibition of PGE₂ was associated with a reduction in TXB₂, suggesting a possible off-target effect on COX-2 activity and expression^[1].
AF3442 (0.01-100 μM, 24 h) significantly reduces COX-2 levels in lipopolysaccharide (LPS) (HY-D1056)-stimulated human monocytes specifically at 100 μM, without affecting COX-1, mPGES-1, mPGES-2, cPGES and TXS levels^[1].
AF3442 (0.01-100 μM, 24 h) is a selective inhibitor of mPGES-1 in LPS-stimulated human whole blood, as evidenced by causing a potent inhibition of PGE₂ by approximately 70% at 100 μM without significantly affecting other prostanoids^[1].