S32826

S32826 is a potent autotaxin inhibitor, with an IC₅₀ of 8.8 nM. S32826 shows similar inhibitory effects at various autotaxin isoforms (α, β and γ). S32826 inhibits LPA release from adipocytes^[1]. In Vitro: S32826 (0.001-10 μM; 10 days) dose-dependently inhibits the release of lyso-phosphatidic acid (LPA) by 3T3-F442A adipocytes with an IC₅₀ 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].
In Vivo: 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].