Apremilast (CC-10004)

Cell lines

U937 human monocytic cells

Preparation method

The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months.

Reaction Conditions

18h; IC50=74 nM

Applications

Apremilast was initially screened for PDE4 inhibition using a partially purified enzyme preparation from U937 human monocytic cells and which has been shown previously to contain predominantly PDE4B and PDE4D activities. Apremilast was also found to exhibit an IC50 of around 74 nM using 1 mM cAMP as substrate.

Animal models

SCID mice

Dosage form

5 mg·kg-1·day-1 ; oral taken

Applications

The pharmacological activity of apremilast (5 mg·kg-1·day-1 total divided into 2 daily doses) was tested in comparison with cyclosporine (5 mg·kg-1·day-1 total divided into 2 daily doses) and vehicle control (0.1 mL·day-1 divided into twice daily doses) in a mouse xenograft model of psoriasis. Epidermal thickness and proliferation index correlated with histological findings and demonstrated significant differences between treatment groups. Notably, apremilast caused statistically significant reductions in epidermal thickness (P < 0.001) and proliferation index (P < 0.001).

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1] Schafer P H, Parton A, Gandhi A K, et al. Apremilast, a cAMP phosphodiesterase‐4 inhibitor, demonstrates anti‐inflammatory activity in vitro and in a model of psoriasis[J]. British journal of pharmacology, 2010, 159(4): 842-855.