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Chemical Structure| 1450824-22-2 Chemical Structure| 1450824-22-2

Structure of TD139
CAS No.: 1450824-22-2

Chemical Structure| 1450824-22-2

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TD139 is an inhibitor of the galectin-3 carbohydrate binding domain with Kd of 14 nM and shows therapeutic efficacy against idiopathic pulmonary fibrosis (IPF).

Synonyms: Olitigaltin; GB0-139; GB0139

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Product Details of TD139

CAS No. :1450824-22-2
Formula : C28H30F2N6O8S
M.W : 648.64
SMILES Code : 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
Synonyms :
Olitigaltin; GB0-139; GB0139
MDL No. :MFCD29919388
InChI Key :YGIDGBAHDZEYMT-MQFIMZJJSA-N
Pubchem ID :73774610

Safety of TD139

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
Primary mouse alveolar epithelial cells 25 μg/ml 48 hours TD139 blocked TGF-β–induced β-catenin activation. PMC3410728
A549 alveolar epithelial cells 10 µM 48 hours TD139 reduced TGF-β1–induced β-catenin nuclear translocation and blocked TGF-β1–induced β-catenin phosphorylation. PMC3410728
Human neutrophils 250 μM 4 hours PMC5289966
Platelet-rich plasma from healthy subjects 3.1 ± 0.5 μg/L To evaluate the effects of rGalectin-3 on platelet aggregation and ATP release in platelet-rich plasma. Results showed that rGalectin-3 potentiated platelet aggregation and ATP release induced by different agonists. PMC9989600
Washed platelets from healthy subjects 5–20 μg/L 30 minutes To evaluate the effects of recombinant Galectin-3 on platelet function. Results showed that rGalectin-3 concentration-dependently potentiated platelet aggregation induced by collagen, thrombin, or ADP and increased ATP release induced by collagen or thrombin. PMC9989600
PDGFRβ+ fibroblasts 10 µg/ml 24 hours To investigate the ability of PDGFRβ+ fibroblasts to internalize Galectin-3 and its effect on PDGFRβ expression. Results showed that Galectin-3 was internalized by fibroblasts, and inhibition of Galectin-3 led to reduced PDGFRβ expression. PMC11481377
Hippocampal slices of WT mice 1 µM gal3 + 10 µM TD139 15 min To evaluate the preventive effect of TD139 on gal3-induced degradation of gamma oscillations, results showed that 10 µM TD139 effectively prevented the gal3-induced decrease of gamma oscillation power and rhythmicity PMC9901156
Hippocampal slices of WT mice 1 µM 15 min To evaluate the preventive effect of TD139 on gal3-induced degradation of gamma oscillations, results showed that 10 µM TD139 effectively prevented the gal3-induced decrease of gamma oscillation power and rhythmicity PMC9901156

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice Bleomycin-induced lung fibrosis model Intratracheal administration 10 mg Administered on Days 18, 20, 22, and 24, continued until Day 26 TD139 significantly reduced lung fibrosis and β-catenin activation. PMC3410728
ApoE−/− mice Atherosclerosis model Intraperitoneal injection 15 mg/kg Twice, 12 hours apart To evaluate the effects of TD139 on in vivo thrombosis in atherosclerotic ApoE?/? mice. Results showed that TD139 significantly suppressed FeCl3-induced thrombus formation without increasing bleeding risk. PMC9989600
Mice Folic acid-induced acute kidney injury model Intraperitoneal injection 15 mg/kg Single injection, observed for 8 days TD139 significantly improved renal function in AKI mice, reduced platelet and macrophage infiltration, and decreased the expression of inflammatory factors. PMC11927336
C57BL/6J mice Spinal cord injury model (T10 crush injury) Intrathecal injection 3 µg/µl Once daily for 14 days To investigate the effect of TD139 on fibrotic scar formation and functional recovery after spinal cord injury. Results showed that TD139 significantly reduced fibrotic scar formation and promoted neuroprotection and motor function recovery. PMC11481377
Mice Light-induced retinal degeneration model Intraperitoneal injections 15 mg/kg For five consecutive days, starting one day prior to light exposure TD139 reduced microglia reactivity and delayed retinal damage PMC9482176
Mice Systemic Candida infection model Intraperitoneal injection 300 μg Single dose TD139-treated mice have enhanced ability to clear the fungus PMC5289966

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.54mL

0.31mL

0.15mL

7.71mL

1.54mL

0.77mL

15.42mL

3.08mL

1.54mL

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