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].

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

397.49

C₂₁H₃₆NO₄P

1096770-84-1

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Ferry G, et, al. S32826, a nanomolar inhibitor of autotaxin: discovery, synthesis and applications as a pharmacological tool. J Pharmacol Exp Ther. 2008 Dec;327(3):809-19.  [Content Brief]

  [2]. Honjo M, et, al. Role of the Autotaxin-LPA Pathway in Dexamethasone-Induced Fibrotic Responses and Extracellular Matrix Production in Human Trabecular Meshwork Cells. Invest Ophthalmol Vis Sci. 2018 Jan 1;59(1):21-30.  [Content Brief]

  [3]. Iyer P, et, al. Autotaxin-lysophosphatidic acid axis is a novel molecular target for lowering intraocular pressure. PLoS One. 2012;7(8):e42627.  [Content Brief]