产品
编 号:F036553
分子式:C21H34NNa2O4P
分子量:441.45
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5mg
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10mg
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25mg
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生物活性:
S32826 disodium is a potent autotaxin inhibitor, with an IC50 of 8.8 nM. S32826 disodium shows similar inhibitory effects at various autotaxin isoforms (α, β and γ). S32826 disodium inhibits LPA release from adipocytes.

体内研究:
Topical application of S32826 (2-10 mM; 2 h-5 d) disodium decreases intraocular pressure (IOP) in a dose- and time-dependent manner in rabbits.S32826 (~2 μM; single intracameral injection) disodium 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.) disodium shows poor in vivo stability and/or bioavailability.

体外研究:
S32826 (0.001-10 μM; 10 days) disodium 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) disodium inhibits Dexamethasone-induced increases in autotaxin (ATX) mRNA expression in HTM cells and lysoPLD activity in conditioned media. S32826 disodium 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.
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