| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
Purity: ≥98%
| Targets |
TD-139 targets galectin-3 (Gal-3), a protein involved in the progression of fibrosis, including the excessive accumulation of scar tissue in the lungs seen in IPF. By inhibiting galectin-3, TD-139 blocks galectin-3-mediated pathways that contribute to fibrosis, inflammation, and tissue remodeling. The compound has potential anti-fibrotic activity.
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| ln Vitro |
In vitro, TD-139 is a potent galectin-3 inhibitor. Its activity is assessed by measuring galectin-3 binding inhibition in biochemical assays and by assessing its effects on galectin-3-mediated cellular functions such as cell adhesion, migration, and fibrosis-related signaling.
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| ln Vivo |
In vivo, TD-139 is an inhaled galectin-3 inhibitor investigated for the treatment of idiopathic pulmonary fibrosis (IPF). The compound has potential anti-fibrotic activity and has been studied in clinical trials for IPF. By inhibiting galectin-3 in the lungs, TD-139 may reduce fibrosis and improve lung function.
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| Enzyme Assay |
In vitro enzyme/receptor binding assays for TD-139 measure its binding affinity to galectin-3 using surface plasmon resonance or fluorescence polarization. The compound's ability to inhibit galectin-3-mediated lectin activity is assessed using carbohydrate-binding assays. Selectivity over other galectins is determined in parallel assays.
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| Cell Assay |
In vitro cell-based assays for TD-139 use lung fibroblasts or epithelial cells to assess its effects on galectin-3-mediated cellular functions. Cells are treated with serial dilutions of the compound, and galectin-3-mediated cell adhesion, migration, proliferation, and fibrosis-related signaling (e.g., TGF-β signaling) are measured.
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| Animal Protocol |
In vivo animal models for TD-139 include mouse models of pulmonary fibrosis such as bleomycin-induced lung fibrosis. The compound is administered via inhalation, and its effects on lung fibrosis, collagen deposition, inflammatory cell infiltration, and lung function are evaluated. Pharmacodynamic studies measure galectin-3 inhibition in lung tissues.
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| ADME/Pharmacokinetics |
TD-139 has a molecular formula of C28H30F2N6O8S and a molecular weight of 648.64 g/mol. It is also known as Orlitigaltin, GB0139, and TD139. The compound has an FDA UNII code of 60Y0GUO72B and is an inhaled formulation. It is stored under appropriate conditions for research use.
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| Toxicity/Toxicokinetics |
The toxicity profile of TD-139 is characterized in preclinical and clinical studies. As an inhaled galectin-3 inhibitor, the compound is administered locally to the lungs, which may reduce systemic toxicity. The compound is for research use only and is not approved for clinical use. Appropriate safety precautions should be taken during handling.
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| References |
: Cell Intrinsic Galectin-3 Attenuates Neutrophil ROS-Dependent Killing of Candida by Modulating CR3 Downstream Syk Activation. Front Immunol. 2017 Feb 3;8:48.
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| Additional Infomation |
Orlitigaltine has been investigated for the treatment of idiopathic pulmonary fibrosis. Orlitigaltine is an inhaled, small-molecule galactolectin-3 (Gal-3) inhibitor with potential anti-fibrotic activity. After administration, orlitigaltine inhibits the activity of Gal-3. This may prevent the activation of alveolar macrophages and fibroblasts, thereby reducing pulmonary fibrosis. Gal-3 is a β-galactosidase-binding lectin expressed in multiple cell types, including macrophages, fibroblasts, activated T lymphocytes, and epithelial cells. Gal-3 expression is upregulated in fibrotic lung diseases, including idiopathic pulmonary fibrosis (IPF) and collagen vascular disease-associated interstitial pneumonia (CVD-IP), and it plays an important role in the fibrotic process of multiple organs. It is also frequently dysregulated in cancer and may play a role in angiogenesis, cell proliferation, and cell survival.
TD-139 (Orlitigaltin, GB0139) is a novel and potent galectin-3 inhibitor with potential for the treatment of idiopathic pulmonary fibrosis (IPF). Galectin-3 is a protein involved in the progression of fibrosis, including the excessive accumulation of scar tissue in the lungs seen in IPF. TD-139 is an inhaled, small-molecule galectin-3 inhibitor with potential anti-fibrotic activity. It has been investigated in clinical trials for IPF and is intended for laboratory research use only. |
| Molecular Formula |
C28H30F2N6O8S
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|---|---|
| Molecular Weight |
648.6350
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| Exact Mass |
648.181
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| CAS # |
1450824-22-2
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| Related CAS # |
1450824-22-2;
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| PubChem CID |
73774610
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| Appearance |
White to off-white solid powder
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| Density |
1.8±0.1 g/cm3
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| Boiling Point |
1017.2±75.0 °C at 760 mmHg
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| Flash Point |
569.0±37.1 °C
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| Vapour Pressure |
0.0±0.3 mmHg at 25°C
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| Index of Refraction |
1.761
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| LogP |
2.19
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| Hydrogen Bond Donor Count |
6
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| Hydrogen Bond Acceptor Count |
15
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
45
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| Complexity |
903
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| Defined Atom Stereocenter Count |
10
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| SMILES |
S([C@@]1([H])[C@@]([H])([C@]([H])([C@]([H])([C@@]([H])(C([H])([H])O[H])O1)O[H])N1C([H])=C(C2C([H])=C([H])C([H])=C(C=2[H])F)N=N1)O[H])[C@@]1([H])[C@@]([H])([C@]([H])([C@]([H])([C@@]([H])(C([H])([H])O[H])O1)O[H])N1C([H])=C(C2C([H])=C([H])C([H])=C(C=2[H])F)N=N1)O[H]
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| InChi Key |
YGIDGBAHDZEYMT-MQFIMZJJSA-N
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| InChi Code |
InChI=1S/C28H30F2N6O8S/c29-15-5-1-3-13(7-15)17-9-35(33-31-17)21-23(39)19(11-37)43-27(25(21)41)45-28-26(42)22(24(40)20(12-38)44-28)36-10-18(32-34-36)14-4-2-6-16(30)8-14/h1-10,19-28,37-42H,11-12H2/t19-,20-,21+,22+,23+,24+,25-,26-,27+,28+/m1/s1
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| Chemical Name |
(2R,2'R,3R,3'R,4S,4'S,5R,5'R,6S,6'S)-6,6'-thiobis(4-(4-(3-fluorophenyl)-1H-1,2,3-triazol-1-yl)-2-(hydroxymethyl)tetrahydro-2H-pyran-3,5-diol)
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| Synonyms |
TD-139 TD139 TD 139
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.5417 mL | 7.7084 mL | 15.4169 mL | |
| 5 mM | 0.3083 mL | 1.5417 mL | 3.0834 mL | |
| 10 mM | 0.1542 mL | 0.7708 mL | 1.5417 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Products are for research use only; We do not sell to patients
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