Cas No.: | 1450824-22-2 |
Synonyms: | TD-139; TD 139 |
SMILES: | O[C@H]([C@@H](N1N=NC(C2=CC=CC(F)=C2)=C1)[C@H]([C@@H](CO)O3)O)[C@@H]3S[C@H]4[C@@H]([C@@H](N5N=NC(C6=CC=CC(F)=C6)=C5)[C@H]([C@@H](CO)O4)O)O |
Formula: | C28H30F2N6O8S |
M.Wt: | 648.64 |
Purity: | >98% |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Description: | TD139 is an inhaled galectin-3 inhibitor with a Kd of 14 nM. |
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]. |
In Vitro: | 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]. |
Animal Administration: | Mice: The susceptibility to Con A-induced hepatitis in galectin-3-deficient mice is tested and the effects of pretreatment with a selective inhibitor of Gal-3 (TD139) in wild-type(WT) C57BL/6 mice are analyzed, as evaluated by a liver enzyme test, quantitative histology, mononuclear cell (MNC) infiltration, cytokine production, intracellular staining of immune cells, and percentage of apoptotic MNCs in the liver[2]. |
References: | [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. |