D-Phenylalanine, N-[(phenylmethoxy)carbonyl]-L-phenylalanyl-, methyl ester

Description

GSK-256066 is a PDE4 inhibitor.

in vitro

GSK256066 potently inhibited PDE4B enzymatic activity at sub-picomolar EC50 as previously reported._x000D_ _x000D_ Reference: Mol Ther. 2016 Dec;24(12):2078-2089. https://pubmed.ncbi.nlm.nih.gov/27731313/

in vivo

When administered intratracheally to rats, GSK256066 inhibited LPS-induced pulmonary neutrophilia with ED(50) values of 1.1 μg/kg (aqueous suspension) and 2.9 μg/kg (dry powder formulation) and was more potent than an aqueous suspension of the corticosteroid fluticasone propionate (ED(50) 9.3 μg/kg)._x000D_ _x000D_ Reference: J Pharmacol Exp Ther. 2011 Apr;337(1):145-54. https://pubmed.ncbi.nlm.nih.gov/21205923/

target

GSK-256066 is a PDE4 inhibitor.