S32826 is a highly potent inhibitor of autotaxin, exhibiting an IC50 value of 8.8 nM. It displays comparable inhibitory properties towards various autotaxin isoforms, including α, β, and γ. Furthermore, S32826 effectively inhibits the release of LPA from adipocytes.

ATX:8.8 nM (IC50)

S32826 (0.001-10 μM; 10 days) dose-dependently inhibits the release of lyso-phosphatidic acid (LPA) by 3T3-F442A adipocytes with an IC 50 of 90 nM and a maximal inhibition of 80% at 500 nM[1]. S32826 (1 μM; 24 h) inhibits Dexamethasone-induced increases in autotaxin (ATX) mRNA expression in HTM cells and lysoPLD activity in conditioned media. S32826 inhibits Dexamethasone-induced the phosphorylation of MLC and cofilin, mRNA upregulation of COL1A1 and COL4A1, and expression of α-SMA, fibronectin and collagen-1 in the HTM cells[2].

Topical application of S32826 (2-10 mM; 2 h-5 d) decreases intraocular pressure (IOP) in a dose- and time-dependent manner in rabbits[2]. S32826 (～2 μM; single intracameral injection) reduces the IOP in rabbits, with the ocular hypotensive response lasting for more than 48 hrs[2]. S32826 (10 mg/kg; p.o., i.p., s.c., and i.v.) shows poor in vivo stability and/or bioavailability[1].