TD139 is an inhaled galectin-3 inhibitor with a Kd of 14 nM.
CAS：1450824-22-2
分子式：C28H30F2N6O8S
分子量：648.64
纯度：98%
存储：Store at -20°C

Background:

TD139 is an inhaled galectin-3 inhibitor with a Kd of 14 nM.

TD139 is a novel synthetic inhibitor of galectin-3. TD139 has high affinity for galectin-3 with a Kd of 14 nM and 10 nM for galectin-1, but low affinity for galectins 2, 4N, 4C, 7, 8N, or 9N[1].

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].

参考文献:
[1]. Mackinnon AC, et al. Regulation of transforming growth factor-β1-driven lung fibrosis by galectin-3. Am J Respir Crit Care Med. 2012 Mar 1;185(5):537-46.
[2]. Volarevic V, et al. Galectin-3 deficiency prevents concanavalin A-induced hepatitis in mice. Hepatology. 2012 Jun;55(6):1954-64.