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BMT-090605
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
BMT-090605图片
CAS NO:1551403-51-0
包装与价格:
包装价格(元)
5mg电议
10mg电议

产品介绍
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。
Cas No.1551403-51-0
分子式C21H24N4O2
分子量364.44
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation 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.