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AAK1-IN-5

Names

[ CAS No. ]:
1815613-44-5

[ Name ]:
AAK1-IN-5

Biological Activity

[Description]:

AAK1-IN-5 is a highly selective, CNS-penetrable, and orally active adaptor protein-2-associated kinase 1 (AAK1) inhibitor (AAK1 IC50 of 1.2 nM, Filt Ki of 0.05 nM, and cell IC50 of 0.5 nM). AAK1-IN-4 has the potential for the research for neuropathic pain[1].

[Related Catalog]:

Signaling Pathways >> Others >> Others
Research Areas >> Neurological Disease

[Target]

IC50: 1.2 nM (AAK1)[1]. Ki: 0.05 nM (AAK1)[1]


[In Vitro]

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].

[In Vivo]

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.

[References]

[1]. Luo G, et al. Discovery and Optimization of Biaryl Alkyl Ethers as a Novel Class of Highly Selective, CNS-Penetrable, and Orally Active Adaptor Protein-2-Associated Kinase 1 (AAK1) Inhibitors for the Potential Treatment of Neuropathic Pain. J Med Chem. 2022;65(6):4534-4564.

Chemical & Physical Properties

[ Molecular Formula ]:
C19H23F4N3O

[ Molecular Weight ]:
385.40

Related Compounds