| 产品描述: | 血清和糖皮质激素调节激酶(SGK)抑制剂;Serum- and glucocorticoid-regulated kinase (SGK) inhibitor;; |
| 体内研究: |
GSK650394(1、10 和 30 μM,10 μL/只大鼠,鞘内注射)剂量依赖性地预防 CFA 诱导的疼痛行为,并在 CFA 给药后 1 天与 SGK1 磷酸化、GluR1 运输和蛋白质-蛋白质相互作用相关。 GSK650394 (浓度为 10、30 和 100 nM(10 μL))而非载体溶液(分别为 SNL 3D+Veh 和 SNL 7D+Veh),在术后第 3 天和第 7 天(分别为 SNL 3D+GSK 和 SNL 7D+GSK)注射后 1-3 和 1-5 小时剂量依赖性地增加同侧后爪的缩足潜伏期。 GSK650394(术后第 0 至 6 天;100 nM,10 μL,i.t.)给药可缓解 SNL 动物术后第 3、5 和 7 天的 SNL 诱发的异常性疼痛。 |
| 参考文献: |
1. Sherk AB, et al. Development of a small-molecule serum- and glucocorticoid-regulated kinase-1 antagonist and its evaluation as a prostate cancer therapeutic. Cancer Res. 2008 Sep 15;68(18):7475-83. 2. Mansley MK, et al. Effects of nominally selective inhibitors of the kinases PI3K, SGK1 and PKB on the insulin-dependent control of epithelial Na+ absorption. Br J Pharmacol. 2010 Oct;161(3):571-88. 3. Peng HY, et al. Spinal SGK1/GRASP-1/Rab4 is involved in complete Freund's adjuvant-induced inflammatory pain via regulating dorsal horn GluR1-containing AMPA receptor trafficking in rats. Pain. 2012 Dec;153(12):2380-92. 4. Peng HY, et al. Spinal serum-inducible and glucocorticoid-inducible kinase 1 mediates neuropathic pain via kalirin and downstream PSD-95-dependent NR2B phosphorylation in rats. J Neurosci. 2013 Mar 20;33(12):5227-40. 5. Alamares-Sapuay JG, et al. Serum- and glucocorticoid-regulated kinase 1 is required for nuclear export of the ribonucleoprotein of influenza A virus. J Virol. 2013 May;87(10):6020-6. |
| 保存条件: |
-80℃(运输条件:冰袋低温运输) |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
2.615 ml |
13.074 ml |
26.147 ml |
| 5 mM |
0.523 ml |
2.615 ml |
5.229 ml |
| 10 mM |
0.261 ml |
1.307 ml |
2.615 ml |
| 50 mM |
0.052 ml |
0.261 ml |
0.523 ml |
|
| 注意: |
部分产品我司仅能提供部分信息,我司不保证所提供信息的权威性,仅供客户参考交流研究之用。 |