BMT-090605 is a potent, selective AAK1 inhibitor, with an IC50 of 0.6 nM. 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 antinociceptive activity.

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]. 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]. The high dose of BMT-090605 (3 μg/rat) showed efficacy comparable to intrathecal clonidine (3 μg/rat).

1551403-51-0

C21H24N4O2

364.44

BMT-090605

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years