| Identification | Back Directory | [Name]
2-Pentanamine, 1-[[2',4-bis(difluoromethyl)[2,4'-bipyridin]-5-yl]oxy]-2,4-dimethyl-, (2S)- | [CAS]
1815613-44-5 | [Synonyms]
AAK1-IN-5
2-Pentanamine, 1-[[2',4-bis(difluoromethyl)[2,4'-bipyridin]-5-yl]oxy]-2,4-dimethyl-, (2S)- | [Molecular Formula]
C19H23F4N3O | [MOL File]
1815613-44-5.mol | [Molecular Weight]
385.4 |
| Hazard Information | Back Directory | [Uses]
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]. | [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. DOI:10.1021/acs.jmedchem.1c02132 |
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