| CAS NO: | 1551403-51-0 |
| 包装 | 价格(元) |
| 5mg | 电议 |
| 10mg | 电议 |
| Cas No. | 1551403-51-0 |
| 分子式 | C21H24N4O2 |
| 分子量 | 364.44 |
| 储存条件 | Store at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
| 产品描述 | BMT-090605 is a potent, selective AAK1 inhibitor, with an IC50 of 0.6 nM. BMT-090605 shows antinociceptive activity. BMT-090605 inhibits BMP-2-inducible protein kinase (BIKE) and Cyclin G-associated kinase (GAK) with IC50s of 45 and 60 nM, respectively[1]. BMT-090605 shows a cellular IC50 of 0.63 ±0.39 nM for AAK1[1]. BMT-090605 (0.3-3 µg/rat; intrathecally at lumbar level L5/L6) causes antinociception by inhibiting AAK1 in the spinal cord[1].The high dose of BMT-090605 (3 µg/rat) showed efficacy comparable to intrathecal clonidine (3 µg/rat). Exposure measurements from this study indicated that brain and plasma levels of BMT-090605 were<4 nM, whereas measurable levels (90-317 nM) were observed in lumbar spinal cord[1]. [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. |
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