| 靶点: |
IC50: 3.3 ± 0.7 nM (AAK1), 14 nM (BIKE), 320 ± 40 nM (GAK) |
| 体内研究: |
LP-935509(0-60 mg/kg;口服,单次)可显著减轻疼痛行为。 LP-935509(0.1-30 mg/kg;口服,单次剂量)在 CCI 模型中可剂量依赖性地逆转热痛觉过敏。 LP-935509(静脉注射(1 mg/kg)或口服(10 mg/kg);单次)口服生物利用度为 100%,血浆半衰期为 3.6 小时。 |
| 参考文献: |
1. Kostich W, et al. Inhibition of AAK1 Kinase as a Novel Therapeutic Approach to Treat Neuropathic Pain. J Pharmacol Exp Ther. 2016 Sep;358(3):371-86. 2. Mushtaq, et al. Role Of Endocytic Machinery Regulators in EGFR Traffic and Viral Entry (2021). Theses & Dissertations. 532. |
| 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 |
2.522 ml |
12.612 ml |
25.224 ml |
| 5 mM |
0.504 ml |
2.522 ml |
5.045 ml |
| 10 mM |
0.252 ml |
1.261 ml |
2.522 ml |
| 50 mM |
0.05 ml |
0.252 ml |
0.504 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。 |