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TD139

Catalog No.GC19350 Copy One-Click Copy Product Info

TD139 is a high-affinity inhibitor of the galectin-1 and galectin-3 with Kd values of 12nM and 14nM, respectively.

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TD139 Chemical Structure

Cas No.: 1450824-22-2

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1mg
$56.00
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5mg
$112.00
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10mg
$182.00
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Sample solution is provided at 25 µL, 10mM.



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Description of TD139

TD139 is a high-affinity inhibitor of the galectin-1 and galectin-3 with Kd values of 12nM and 14nM, respectively[1]. TD139 selectively targets galectin-3 by disrupting β-galactoside-binding activity and promotes M2-like macrophage polarization[2]. TD139 has been used to suppress Galectin-3-potentiated platelet activation and inhibit occlusive thrombosis[3].

In vitro, TD139 treatment (20μM) for 24 hours significantly inhibited the activation of NLRP3 inflammasome in BV2 cells, and reduced the protein levels of IL-1β, IL-6, IL-18, and TNF-α[4]. Treatment with 100μM TD139 for 72 hours significantly inhibited the growth of FTC-133 and 8505C cells, and reduced the migration of the cells as well as the expressions of β-catenin and MMP2[5]. Treatment with 10μM TD139 for 24 hours the suppressed TNF-α-induced inflammatory response and inhibited the activation of the ERK/JNK/p38 signaling pathway in placental tissues[6].

In vivo, TD139 treatment via intraperitoneal injection at a dose of 15mg/kg, once every 12 hours for 24 hours, alleviated the neuroinflammatory damage after subarachnoid hemorrhage and improved neurological dysfunction in mice[7]. Daily intrathecal injection of TD139 at a dose of 30µg/day for 14 days reduced fibrotic scar formation after spinal cord injury (SCI) and promoted the neurological recovery in mice[8].

References:

[1] Lee L Y G N, Leow S Y, Wen H, et al. An evaluation of the mechanisms of galacto-oligosaccharide (GOS)-Induced IgE cross-linking on basophils in GOS allergy[J]. Frontiers in Allergy, 2022, 3: 840454.

[2] Wang M, Jiang Y, Wan J, et al. Inhibition of Galectin-3 expression could preserve the immunoregulatory function of mesenchymal stem cells during cell passaging[J]. Frontiers in Bioscience-Landmark, 2025, 30(8): 39918.

[3] Chen Y, Fu W, Zheng Y, et al. Galectin 3 enhances platelet aggregation and thrombosis via Dectin-1 activation: a translational study[J]. European Heart Journal, 2022, 43(37): 3556-3574.

[4] Sun W, Hao Y, Li C, et al. Inhibition of Galectin-3 in a rat model of epilepsy and Kainate-Activated BV2 cells limits microglial activation through the NLRP3/Pyroptosis pathway[J]. Neuroimmunomodulation, 2023, 30(1): 325-337.

[5] Lee J J, Hsu Y C, Li Y S, et al. Galectin‐3 inhibitors suppress anoikis resistance and invasive capacity in thyroid cancer cells[J]. International Journal of Endocrinology, 2021, 2021(1): 5583491.

[6] Xia J, Wang Y, Qi B R. In vitro and in vivo effects of Galectin‐3 inhibitor TD139 on inflammation and ERK/JNK/p38 pathway in gestational diabetes mellitus[J]. The Kaohsiung Journal of Medical Sciences, 2024, 40(10): 916-925.

[7] Shen Y, Zhang W, Chang H, et al. Galectin-3 modulates microglial activation and neuroinflammation in early brain injury after subarachnoid hemorrhage[J]. Experimental neurology, 2024, 377: 114777.

[8] Shan F, Ye J, Xu X, et al. Galectin-3 inhibition reduces fibrotic scarring and promotes functional recovery after spinal cord injury in mice[J]. Cell & Bioscience, 2024, 14(1): 128.

Protocol of TD139

Cell experiment [1]:

Cell lines

FTC-133 cells

Preparation Method

FTC-133 cells were cultivated in DMEM/F12 medium supplemented with 10% heat-inactivated fetal bovine serum (FBS), 1% penicillin-streptomycin at 37°C in an incubator with 5% CO2. Cells were seeded in a 96-well plate at a density of 1×104 cells/well for 24h. Cells were treated with TD139 at different concentrations (0, 1, 10, and 100μM). After 72h of treatment, the cell viability was determined.

Reaction Conditions

0, 1, 10, and 100μM; 72h

Applications

TD139 treatment inhibited cell viability of FTC-133 cells in a dose-dependent manner.
Animal experiment [2]:

Animal models

Female C57BL/6J mice

Preparation Method

Female C57BL/6J mice (8 weeks old) were housed in specific pathogen-free facilities under a 12h light-dark cycle at a temperature of 24±1°C with controlled humidity, and had access to food and water. The mice were anesthetized with intraperitoneal injection of sodium pentobarbital (50mg/kg) and placed in the prone position on the operating table. The dorsal surface around the T10 segment was shaved, and the skin was disinfected with iodophor. The T9-T11 dorsal skin was dissected, and the back muscle was sequentially peeled off. Laminectomy was performed to expose the spinal cord at the T10 level, which served as the clamping site. Crush-induced spinal cord injuries were made without spacers, with a tip width of 0.5mm, to completely compress the entire spinal cord laterally from both sides for 5s. Successful SCI induction was confirmed by observing transient spasms in the hind limbs and tail along with a continuous red clamp mark after saline irrigation. The wound was then sutured layer by layer. Postoperatively, the mice were subjected to auxiliary urination twice daily (morning and afternoon) until spontaneous urination was restored after SCI. Prior to injection into the lumbar 5-6 intervertebral space in mice, the dorsal surface was shaved, and the skin was disinfected with iodophor. The successful insertion of the needle into the intradural space was confirmed by sudden tail wagging. 30mg TD139 was dissolved in 10ml PBS containing 3% DMSO and was injected (i.t.) daily at 10µl using a microinjection needle. For the SCI mice, TD139 was injected post-operatively daily for 14 days. The control mice received the same volume of 10µl of PBS containing 3% DMSO. The damaged spinal cords of mice were collected for analysis.

Dosage form

3µg/day; 14 days; i.t.

Applications

TD139 treatment reduced fibrotic scar formation after SCI in mice.

References:

[1] Lee J J, Hsu Y C, Li Y S, et al. Galectin‐3 inhibitors suppress anoikis resistance and invasive capacity in thyroid cancer cells[J]. International Journal of Endocrinology, 2021, 2021(1): 5583491.

[2] Shan F, Ye J, Xu X, et al. Galectin-3 inhibition reduces fibrotic scarring and promotes functional recovery after spinal cord injury in mice[J]. Cell & Bioscience, 2024, 14(1): 128.

Chemical Properties of TD139

Cas No. 1450824-22-2 SDF
Canonical 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
Solubility DMSO : 50 mg/mL (77.08 mM);Ethanol : ≥ 3.33 mg/mL (5.13 mM);Water : < 0.1 mg/mL (insoluble) Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of TD139

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1 mg 5 mg 10 mg
1 mM 1.5417 mL 7.7084 mL 15.4169 mL
5 mM 308.3 μL 1.5417 mL 3.0834 mL
10 mM 154.2 μL 770.8 μL 1.5417 mL
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Average Rating: 5 ★★★★★ (Based on Reviews and 2 reference(s) in Google Scholar.)

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