LP 922761 是一种有效的、选择性的和口服活性的接头蛋白 2 相关激酶 1 (AAK1) 抑制剂,在酶和细胞试验中的 IC50 分别为 4.8 nM 和 7.6 nM。
Cas No. | 1454808-95-7 |
Canonical SMILES | CN(C(OC(C)(C)C)=O)CCNC1=NN2C(C=C1)=NC=C2C3=CC=C(C(N)=O)C=C3 |
分子式 | C21H26N6O3 |
分子量 | 410.47 |
溶解度 | Soluble in DMSO |
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 | Potent AAK1 inhibitor (IC50 values are 4.8 and 7.6 nM in enzyme and cell assays, respectively). Exhibits some selectivity for AAK1 over BIKE, and exhibits no significant activity at opioid, adrenergic α2 or GABAA receptors. Orally bioavailable. Peripherally restricted. Kostich et al (2016) Inhibition of AAK1 kinase as a novel therapeutic approach to treat neuropathic pain. J.Pharmacol.Exp.Ther. 358 371 PMID:27411717 |