S32826,1096770-84-1

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S32826

CAS No. : 1096770-84-1

MCE 国际站：S32826

产品活性：S32826 是一种有效的 autotaxin 抑制剂，IC₅₀ 值为 8.8 nM。S32826 对各种 autotaxin 同种型 (α、β 和 γ) 显示出相似的抑制作用。S32826 抑制脂肪细胞释放 LPA。

研究领域：Metabolic Enzyme/Protease

作用靶点：Phosphodiesterase (PDE)

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.
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.

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.
S32826 (∼2 µM; single intracameral injection) reduces the IOP in rabbits, with the ocular hypotensive response lasting for more than 48 hrs.
S32826 (10 mg/kg; p.o., i.p., s.c., and i.v.) shows poor in vivo stability and/or bioavailability.

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