| Size | Price | Stock | Qty |
|---|---|---|---|
| 10mg |
|
||
| Other Sizes |
| Targets |
Kd: 24 μM (GAL1) and 49 μM (GAL3)[1]
Galectins (GAL1, GAL3, GAL8, GAL9). TDG is a disaccharide analog of lactose containing a sulfur linkage, which binds to the carbohydrate recognition domain (CRD) of galectins, blocking their interactions with cell surface glycoconjugates. |
|---|---|
| ln Vitro |
Based on TG content and Oil Red O (ORO) staining, thiodigalactoside (TDG; 250 and 500 μM) shows dose-dependent decrease of fat accumulation[1].
In vitro, Thiodigalactoside (TDG; 250 and 500 uM) demonstrates a dose-dependent decrease in fat accumulation, as evidenced by reductions in triglyceride (TG) content and Oil Red O (ORO) staining in adipocytes. It binds galectins-1, -3, -8, and -9 with Kd values between 24 and 78 uM. |
| ln Vivo |
Thiodigalactoside (TDG; 5 mg/kg; IP; once weekly for 5 weeks) significantly reduces the amount of body weight increase that is caused by a high fat diet[2]. In comparison to IP, thiodigalactoside (5 mg/kg; oral; daily or weekly for 5 weeks) produced a smaller reduction in body weight gain[2].
In vivo, Thiodigalactoside (TDG; 5 mg/kg; IP; once per week for 5 weeks) significantly inhibits high-fat diet (HFD)-induced body weight gain, whereas oral administration (5 mg/kg; daily or weekly for 5 weeks) provides less reduction in body weight gain compared to IP administration. This demonstrates its potential for obesity research. |
| Enzyme Assay |
A direct binding fluorescence polarization (FP) assay is used: recombinant galectin proteins (e.g., GAL1 or GAL3) are incubated with a fluorescently labeled lactose probe in the presence of serially diluted TDG (1-1000 uM). The polarization signal decreases as the inhibitor displaces the probe, and the Kd is calculated from the competition curve.
|
| Cell Assay |
For in vitro cellular assays, primary pre-adipocytes or 3T3-L1 adipocytes are treated with TDG (250 and 500 uM) during adipogenic differentiation for 7-14 days. Lipid accumulation is assessed by Oil Red O (ORO) staining and quantitation by spectrophotometry. Triglyceride (TG) content is measured using a colorimetric assay kit to evaluate fat accumulation.
|
| Animal Protocol |
Animal/Disease Models: Fiveweeks old SD (Sprague-Dawley) male rats[2]
Doses: 5 mg/kg Route of Administration: IP; once per week for 5 weeks Experimental Results: Resulted in dramatic inhibition of HFD-induced body weight gain by inhibiting adipogenesis and lipogensis as well as by increasing expression of the proteins associated with thermogenesis and energy expenditure. C57BL/6 mice are fed a high-fat diet (HFD) for 8-12 weeks to induce obesity. Thiodigalactoside is administered intraperitoneally at 5 mg/kg once per week for 5 weeks, or orally at 5 mg/kg daily or weekly for 5 weeks. Body weight is measured weekly. At study termination, epididymal fat pads are weighed, and serum TG, cholesterol, and glucose levels are measured. |
| ADME/Pharmacokinetics |
TDG has a molecular weight of 358.36 g/mol and a formula of C12H22O10S. It is orally active but shows better efficacy via IP administration. Water solubility is high (90 mg/mL), and DMSO solubility is 50 mg/mL. Detailed PK parameters are not fully published; IP bioavailability is likely higher than oral due to first-pass metabolism.
|
| Toxicity/Toxicokinetics |
Detailed toxicological profiles are not publicly available. As a disaccharide galectin inhibitor, TDG is generally considered safe, with no severe toxicities reported at efficacious doses in animal studies. High doses may cause mild gastrointestinal disturbances due to its non-metabolizable nature.
|
| References |
|
| Additional Infomation |
Thiogalactoside is a solid. This compound belongs to the disaccharide class, meaning it contains two hexose units. This drug is known to target galactolectin-1, the heat-labile enterotoxin B chain, neuroprotein core protein, and lactose permease.
TDG is a research chemical not approved for clinical use. It is commonly used to investigate the role of galectins in carcinogenesis, cell signaling, inflammation, and obesity. It is a standard tool compound for pan-galectin inhibition studies and has been referenced in J Med Chem (2013) and Cancer Res (2015). |
| Molecular Formula |
C12H22O10S
|
|---|---|
| Molecular Weight |
358.36
|
| Exact Mass |
358.093
|
| CAS # |
51555-87-4
|
| PubChem CID |
119138
|
| Appearance |
White to off-white solid powder
|
| LogP |
-3.4
|
| Hydrogen Bond Donor Count |
8
|
| Hydrogen Bond Acceptor Count |
11
|
| Rotatable Bond Count |
4
|
| Heavy Atom Count |
23
|
| Complexity |
353
|
| Defined Atom Stereocenter Count |
10
|
| SMILES |
C([C@@H]1[C@@H]([C@@H]([C@H]([C@@H](O1)S[C@H]2[C@@H]([C@H]([C@H]([C@H](O2)CO)O)O)O)O)O)O)O
|
| InChi Key |
SYKYBMOFPMXDRQ-ZFDCCPEWSA-N
|
| InChi Code |
InChI=1S/C12H22O10S/c13-1-3-5(15)7(17)9(19)11(21-3)23-12-10(20)8(18)6(16)4(2-14)22-12/h3-20H,1-2H2/t3-,4-,5+,6+,7+,8+,9-,10-,11+,12+/m1/s1
|
| Chemical Name |
(2R,3R,4S,5R,6S)-2-(hydroxymethyl)-6-[(2S,3R,4S,5R,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]sulfanyloxane-3,4,5-triol
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
H2O: 100 mg/mL (279.05 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 100 mg/mL (279.05 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7905 mL | 13.9525 mL | 27.9049 mL | |
| 5 mM | 0.5581 mL | 2.7905 mL | 5.5810 mL | |
| 10 mM | 0.2790 mL | 1.3952 mL | 2.7905 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.
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