1454808-95-7

1454808-95-7 structure

Name: LP 922761
Chemical Name: LP-922761
CAS Number: 1454808-95-7
Molecular Formula: C₂₁H₂₆N₆O₃
Molecular Weight: 410.47
Catalog: Research Areas Neurological Disease
Create Date: 2020-06-01 18:04:05
Modify Date: 2024-01-31 06:45:14
LP-922761 is a potent, selective and orally active adapter protein-2 associated kinase 1 (AAK1) inhibitor with an in vitro IC50 of 4.8 nM and a cellular IC50 of 7.6 nM. 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 α2 or GABAa receptors[1].

Name	LP-922761

Description	LP-922761 is a potent, selective and orally active adapter protein-2 associated kinase 1 (AAK1) inhibitor with an in vitro IC50 of 4.8 nM and a cellular IC50 of 7.6 nM. 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 α2 or GABAa receptors[1].
Related Catalog	Signaling Pathways >> Others >> Others Research Areas >> Neurological Disease
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].
References	[1]. Kostich W, et al. Inhibition of AAK1 Kinase as a Novel Therapeutic Approach to Treat Neuropathic Pain. J Pharmacol Exp Ther. 2016 Sep;358(3):371-86.

Molecular Formula	C₂₁H₂₆N₆O₃
Molecular Weight	410.47