GLPG0492

Melting point: 66 - 71°C

Boiling point: 544.0±60.0 °C(Predicted)

Density: 1.50±0.1 g/cm3(Predicted)

Storage temp.: Hygroscopic, -20°C Freezer, Under inert atmosphere

Solubility: DMSO (Slightly), Ethanol (Slightly, Sonicated)

Form: Solid

Color: White to Off-White

Stability: Hygroscopic

1.Cell Experiment

Solubility in DMSO: ≥ 50 mg/mL (128.43 mM; Hygroscopic DMSO significantly affects the solubility of the product, please use freshly opened DMSO)

* "≥" means soluble, but saturation unknown.

Preparing Stock Solutions:

Please choose a suitable solvent to prepare the stock solution based on the product's solubility in different solvents. Once the solution is prepared, aliquot and store it to avoid product degradation caused by repeated freeze-thaw cycles.

Storage conditions and shelf life of the stock solution: -80°C for 2 years; -20°C for 1 year. When stored at -80°C, use within 2 years; when stored at -20°C, use within 1 year.

2.Animal Experiment

Please choose an appropriate dissolution protocol based on your experimental animals and administration method.  

For all the following dissolution protocols, please first prepare a clear stock solution according to the in vitro method, and then add solubilizing agents sequentially:  

— To ensure the reliability of experimental results, the clear stock solution can be stored appropriately depending on storage conditions; for in vivo experiments, it is recommended to prepare the working solution fresh and use it the same day.  

The percentages shown before each solvent refer to the volume ratio of that solvent in the final solution you prepare; if precipitation or crystallization occurs during preparation, solubilization can be aided by heating and/or ultrasonication.

Protocol 1

Please add each solvent in order: 10% DMSO, 40% PEG300, 5% Tween-80, 45% Saline

Solubility: ≥ 2.5 mg/mL (6.42 mM); clear solution

This protocol can achieve a clear solution of ≥ 2.5 mg/mL (saturation unknown).

For 1 mL of working solution as an example, take 100 μL of a 25.0 mg/mL clear DMSO stock solution and add it to 400 μL of PEG300, then mix well; next, add 50 μL of Tween-80 to the above mixture and mix thoroughly; then continue by adding 450 μL of saline and adjust the volume to 1 mL.

Preparation of saline: Dissolve 0.9 g of sodium chloride in ddH₂O and adjust the volume to 100 mL to obtain a clear, transparent saline solution.

Protocol 2

Please add each solvent in order: 10% DMSO, 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.5 mg/mL (6.42 mM); clear solution

This method can obtain a clear solution with ≥ 2.5 mg/mL (saturation unknown).

For 1 mL of working solution, add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD saline solution and mix well.

Dissolve 2 g of SBE-β-CD (sulfobutyl ether β-cyclodextrin) powder in 10 mL of saline, fully dissolving to a clear and transparent solution.

Protocol 3

Please add each solvent in order: 10% DMSO, 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (6.42 mM); clear solution

This method can achieve a clear solution with ≥ 2.5 mg/mL (saturation unknown). For animal experiments lasting more than half a month, use this method as appropriate.

For 1 mL of working solution, take 100 μL of 25.0 mg/mL clear DMSO stock solution and add it to 900 μL of corn oil, then mix thoroughly.