BMT-090605 是一种有效的选择性 AAK1 抑制剂，IC50 为 0.6 nM。BMT-090605 显示抗伤害活性。BMT-090605 抑制 BMP-2 诱导蛋白激酶 (BIKE) 和细胞周期蛋白 G 相关激酶 GAK，IC50 分别为 45 和 60 nM。
货号:ajcx38316
CAS:1551403-51-0
分子式:C21H24N4O2
分子量：364.44
溶解度:N/A
纯度：98%
存储：Store at -20°C
库存： 现货

Background:

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 ?g/rat; intrathecally at lumbar level L5/L6) causes antinociception by inhibiting AAK1 in the spinal cord[1].The high dose of BMT-090605 (3 ?g/rat) showed efficacy comparable to intrathecal clonidine (3 ?g/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.