Name | TD139 |
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Synonyms |
TD-139
β-D-Galactopyranoside, 3-deoxy-3-[4-(3-fluorophenyl)-1H-1,2,3-triazol-1-yl]-β-D-galactopyranosyl 3-deoxy-3-[4-(3-fluorophenyl)-1H-1,2,3-triazol-1-yl]-1-thio- 60Y0GUO72B 3-Deoxy-3-[4-(3-fluorophenyl)-1H-1,2,3-triazol-1-yl]-β-D-galactopyranosyl 3-deoxy-3-[4-(3-fluorophenyl)-1H-1,2,3-triazol-1-yl]-1-thio-β-D-galactopyranoside |
Description | TD139 is an inhaled galectin-3 inhibitor with a Kd of 14 nM. |
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Related Catalog | |
Target |
Kd: 14 nM (galectin-3)[1] |
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]. |
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]. |
Animal Admin | 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 |
Density | 1.8±0.1 g/cm3 |
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Boiling Point | 1017.2±75.0 °C at 760 mmHg |
Molecular Formula | C28H30F2N6O8S |
Molecular Weight | 648.635 |
Flash Point | 569.0±37.1 °C |
Exact Mass | 648.181396 |
LogP | 2.19 |
Vapour Pressure | 0.0±0.3 mmHg at 25°C |
Index of Refraction | 1.761 |