THI0019 is a highly potent agonist of the integrin α4β1 (VLA-4) receptor, with an EC 50 range of 1-2 μM. It effectively promotes the adhesion of stem/progenitor cells. Furthermore, THI0019 successfully modulates adhesion processes mediated by α4β7, α5β1, and αLβ2 integrins.

α4β1:1-2 μM (EC50)

In assays evaluating Jurkat cell adhesion, when bound to CS1-conjugated BSA, THI0019 enhanced cell binding in a dose-dependent manner, achieving an effective concentration (EC 50) of 1.7 μM. A more significant, 100-fold increase in Jurkat cell attachment was observed when using VCAM-1 as the ligand, with THI0019 demonstrating an EC 50 of 1.2 μM. Additionally, THI0019 increased EPC binding to VCAM-1 in a dose-dependent fashion (EC 50 of 3.7 μM). It also augmented cell rolling and spreading on VCAM-1 and enhanced cell migration toward SDF-1α[1].