GW559090 is a selective, competitive, and high-affinity α4 integrin antagonist with a Kd value of 0.19 nM for α4β1. It effectively inhibits the binding of α4β1 to vascular cell adhesion molecule 1 (VCAM-1) and fibronectin, with IC50 values of 7.72 and 8.04 nM, respectively. Additionally, GW559090 suppresses the interaction between α4β7 and mucosal addressin cell adhesion molecule 1 (MAdCAM-1) with an IC50 value of 23 nM. It also inhibits inflammatory infiltration in the eye, repairs the corneal barrier, and restores goblet cell function, making it useful for research into dry eye syndrome associated with Sjögren's syndrome.

α4β1:0.19 nM (Kd)