| Size | Price | |
|---|---|---|
| 25mg |
TD-139 is an inhaled galectin-3 inhibitor with a Kd of 14 nM.
| References | |
|---|---|
| Additional Infomation |
Olitigaltin has been investigated for the treatment of idiopathic pulmonary fibrosis. Olitigaltin is an inhaled, small-molecule galactolectin-3 (Gal-3) inhibitor with potential anti-fibrotic activity. After administration, Olitigaltin 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.
|
| Molecular Formula |
C28H30F2N6O8S
|
|---|---|
| Molecular Weight |
648.6350
|
| Exact Mass |
648.181
|
| CAS # |
1450824-22-2
|
| PubChem CID |
73774610
|
| Appearance |
White to off-white solid powder
|
| Density |
1.8±0.1 g/cm3
|
| Boiling Point |
1017.2±75.0 °C at 760 mmHg
|
| Flash Point |
569.0±37.1 °C
|
| Vapour Pressure |
0.0±0.3 mmHg at 25°C
|
| Index of Refraction |
1.761
|
| LogP |
2.19
|
| Hydrogen Bond Donor Count |
6
|
| Hydrogen Bond Acceptor Count |
15
|
| Rotatable Bond Count |
8
|
| Heavy Atom Count |
45
|
| Complexity |
903
|
| Defined Atom Stereocenter Count |
10
|
| 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]
|
| 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 |
| 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) |
DMSO: ~50 mg/mL (~77.1 mM; with ultrasonication)
H2O: < 0.1 mg/mL (insoluble) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (3.85 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), Clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 400 μL of PEG300 and mix well; then add 50 μL of Tween-80 and mix well; finally add 450 μL of physiological saline and adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (3.85 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), Clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 900 μL of 20% SBE-β-CD saline and mix well. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 3: ≥ 2.5 mg/mL (3.85 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), Clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 900 μL of corn oil and mix well. View More
Solubility in Formulation 4: 3.33 mg/mL (5.13 mM) in 10% HP-β-CD in Saline water (add these co-solvents sequentially from left to right, and one by one), Clear solution; with ultrasonication. Solubility in Formulation 5: 10 mg/mL (15.42 mM) in 45% PEG300 + 5% Tween-80 + 50% Saline (add these co-solvents sequentially from left to right, and one by one), Clear solution; with ultrasonication. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 6: 2 mg/mL (3.08 mM) in 15% Cremophor EL + 85% Saline (add these co-solvents sequentially from left to right, and one by one), Clear solution; with ultrasonication. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. (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
Copyright 2020 InvivoChem LLC | All Rights Reserved
