LP-935509

LP-935509 is an orally active, potent, selective, ATP-competitive and brain-penetrant inhibitor of adaptor protein-2 associated kinase 1 (AAK1) with an IC₅₀ of 3.3 nM and a K_i of 0.9 nM, respectively. LP-935509 is also a potent inhibitor of BIKE (IC₅₀=14 nM) and a modest inhibitor of GAK (IC₅₀=320 nM). LP-935509 shows antinociceptive activity. LP-935509 can be used for neuropathic pain and SARS-CoV-2 research^[1]. IC50 & Target: IC50: 3.3 ± 0.7 nM (AAK1), 14 nM (BIKE), 320 ± 40 nM (GAK)^[1] In Vitro: LP-935509 inhibits μ2 phosphorylation with an IC₅₀ value of 2.8 ± 0.4 nM, inhibits phosphorylation of a peptide derived from the μ2 protein with an IC₅₀ value of 3.3 ± 0.7 nM^[1].
LP-935509 exhibits a dose-dependent inhibition of the SARS-CoV-2 S-RBD internalization into host cells^[2]. In Vivo: LP-935509 (0-60 mg/kg; PO, single) causes a robust reduction in pain behavior^[1].
LP-935509 (0.1-30 mg/kg; PO, single dosage) causes a dose-dependent reversal of thermal hyperalgesia in CCI model^[1].
LP-935509 (IV (1 mg/kg) or orally (10 mg/kg); once) has 100% oral bioavailability and a plasma half life of 3.6 hours^[1].