| 产品描述: | 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. |
| 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. |
| 参考文献: |
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. 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. 3. Iyer P, et, al. Autotaxin-lysophosphatidic acid axis is a novel molecular target for lowering intraocular pressure. PLoS One. 2012;7(8):e42627. |
| 保存条件: |
-20°C |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
2.255 ml |
11.275 ml |
22.549 ml |
| 5 mM |
0.451 ml |
2.255 ml |
4.51 ml |
| 10 mM |
0.225 ml |
1.127 ml |
2.255 ml |
| 50 mM |
0.045 ml |
0.225 ml |
0.451 ml |
|
| 注意: |
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