LP-922761

1454808-95-7

410.47

DMSO : 41.67 mg/mL (101.52 mM; ultrasonic and warming and heat to 80C)

Others

LP-922761 is a potent, selective and orally active adapter protein-2 associated kinase 1 (AAK1) inhibitor with IC₅₀s of 4.8 nM and 7.6 nM in enzyme and cell assays, respectively. LP-922761 also inhibits BMP-2-inducible protein kinase (BIKE) with an IC₅₀ of 24 nM. LP-922761 exhibits no significant activity at cyclin G-associated kinase (GAK), opioid, adrenergic alpha2 or GABAa receptors^[1]. IC50 & Target: IC50: 4.8 nM (Adapter protein-2 associated kinase 1 (AAK1) in enzyme assays); 7.6 nM (AAK1 in cell assays); 24 nM (BMP-2-inducible protein kinase (BIKE))^[1] In Vivo: In mouse, LP-922761 has a brain to plasma ratio of 0.007, indicating that LP-922761 is essentially restricted to the peripheral compartment^[1].