An inhibitor of galectin-3; binds selectively to galectin-3 (Kd = 0.036 µM) over galectin-1 and galectin-7 (Kds = 2.2 and 32 µM

TD139 – 1 mg

Brand:
Cayman
CAS:
1450824-22-2
Storage:
-20
UN-No:
Non-Hazardous - /

TD139 is an inhibitor of galectin-3.{45421} It binds selectively to galectin-3 (Kd = 0.036 µM) over galectin-1 and galectin-7 (Kds = 2.2 and 32 µM, respectively) at 4°C, but it is not selective over galectin-1 in a fluorescence anisotropy assay (Kds = 0.014 and 0.01 µM for galectin-3 and -1, respectively).{45421,45422} It is selective for galectin-3 and galectin-1 over galectin-2, -4N, -4C, -7, -8N, -9N, and -9C (Kds = >5, 0.17, 0.14, 1.9, 86, 0.68, and 0.12 µM, respectively) in a fluorescence anisotropy assay.{45422} TD139 (10 µM) decreases galectin-3 accumulation induced by amitriptyline (Item No. 15881) in MCF-7 cells. It reduces TGF-β1-induced nuclear translocation and phosphorylation of β-catenin in isolated mouse lung alveolar epithelial cells.{45423} TD139 also reduces β-catenin activation in the lung and lung fibrosis in a mouse model of idiopathic pulmonary fibrosis induced by bleomycin (Item No. 13877) when administered via lung instillation at a dose of 10 µg/animal.  

 

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Description

An inhibitor of galectin-3; binds selectively to galectin-3 (Kd = 0.036 µM) over galectin-1 and galectin-7 (Kds = 2.2 and 32 µM, respectively) at 4°C, but it is not selective over galectin-1 in a fluorescence anisotropy assay (Kds = 0.014 and 0.01 µM for galectin-3 and -1, respectively); selective for galectin-3 and galectin-1 over galectin-2, -4N, -4C, -7, -8N, -9N, and -9C (Kds = >5, 0.17, 0.14, 1.9, 86, 0.68, and 0.12 µM, respectively) in a fluorescence anisotropy assay; decreases amitriptyline-induced galectin-3 accumulation in MCF-7 cells; reduces β-catenin activation in the lung and lung fibrosis in a bleomycin-induced mouse model of idiopathic pulmonary fibrosis at 10 µg/animal via lung instillation

Formal name: 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

Synonyms: 

Molecular weight: 648.6

CAS: 1450824-22-2

Purity: ≥98%

Formulation: A crystalline solid

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