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LP-922761 hydrate
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。
LP-922761 hydrate图片
包装:5mg
市场价:1440元

产品介绍
LP-922761 hydrate 是一种有效的，选择性的，具有口服活性的 AAK1 抑制剂，在酶和细胞分析中 IC50 分别为 4.8 nM 和 7.6 nM。LP-922761 hydrate 还抑制 BMP-2 诱导蛋白激酶 (BIKE)，IC50 为 24 nM。LP-922761 hydrate 对细胞 GAK，阿片类药物，肾上腺素 α2 或 GABAa 受体无明显活性。
分子式C21H26N6O3.1/4H2O
分子量414.98
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

LP-922761 hydrate is a potent, selective and orally active adapter protein-2 associated kinase 1 (AAK1) inhibitor with IC50s of 4.8 nM and 7.6 nM in enzyme and cell assays, respectively. LP-922761 hydrate also inhibits BMP-2-inducible protein kinase (BIKE) with an IC50 of 24 nM. LP-922761 hydrate shows less activity at cyclin G-associated kinase (GAK), opioid, adrenergic α2 or GABAa receptors[1].

In mouse, LP-922761 has a brain to plasma ratio of 0.007, indicating that LP-922761 is essentially restricted to the peripheral compartment[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.