Olitigaltin

TD139 is a synthetic galectin-3 inhibitor. TD139 has high affinity for galectin-3 with a K_d of 68 nM, a K_d of 0.22 μM for galectin-1, and a K_d of 38 μM for galectin-7^[1]. IC50 & Target:Kd: 14 nM (galectin-3)^[1] In Vivo:In primary lung AECs TD139 reduces TGF-β1–induced β-catenin translocation to the nucleus, with most of the β-catenin remaining at the cell surface. TD139 blocks TGF-β1–induced β-catenin phosphorylation. A marked reduction in fibrosis and β-catenin activation accompanied by decreased galectin-3 expression is observed in the lungs of WT mice treated with TD139^[1]. Pretreatment of WT C57BL/6 mice with TD139 leads to the attenuation of liver injury and milder infiltration of IFNγ- and IL-17- and -4-producing CD4(+) T cells, as well as an increase in the total number of IL-10-producing CD4(+) T cells and F4/80(+) CD206(+) alternatively activates macrophages and preventes the apoptosis of liver-infiltrating MNCs^[2].