AAK1-IN-5 是一种具有高选择性、可透过血脑屏障以及口服活性的接头蛋白2相关激酶1 (adaptor protein-2-associated kinase 1, AAK1) 抑制剂 (AAK1IC50=1.2 nM, FiltKi=0.05 nM, cellIC50=0.5 nM)。AAK1-IN-5 具有研究神经性疼痛的潜力。

AAK1-IN-5 is a highly selective, CNS-penetrable, and orally active adaptor protein-2-associated kinase 1 (AAK1) inhibitor (AAK1 IC 50 of 1.2 nM, Filt K i of 0.05 nM, and cell IC 50 of 0.5 nM). AAK1-IN-4 has the potential for the research for neuropathic pain [1].

AAK1-IN-5 (compound 58) (0.5 μM, 0-10 min) has a good metabolic stability, with half-life values of over 120 min in human and mouse liver microsomes, and 76.0, 17.6, 26.0 min in rat, cynomolgus monkey, and dog, respectively [1].

AAK1-IN-5 (compound 58) can reduce hyperalgesia in SD rats (chronic constriction injury) efficiently with good efficacy observed at doses of 1 and 3 mg/kg [1]. Animal Model: Male Sprague-Dawley rats (chronic constriction injury, CCI) [1] Dosage: 1-3 mg/kg Administration: p.o., 0-5.5 hours Result: Reduced hyperalgesia in CCI rats efficiently with good efficacy observed at doses of 1 and 3 mg/kg.

1815613-44-5

C19H23F4N3O

385.4

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