PDE4 inhibitor
CAS：608141-41-9
分子式：C22H24N2O7S
分子量：460.5
纯度：98%
存储：Store at -20°C

Background:

Apremilast, also known as CC-10004, is a novel and potent small-molecule inhibitor of phosphodiesterase 4 (PDE4), a key enzyme involved in cyclic adenosine monophosphate (cAMP) degradation and cytokine production of inflammatory cells. Apremilast binds to the catalytic site of PDE4, with values of inhibition constant IC₅₀and affinity constantK_iof 0.074 μM and 68 nM respectively, consequently leading to the degradation of cAMP. Apremilast exhibits anti-inflammatory activities against inflammatory disease in animal models as well as human chronic inflammatory diseases (such as psoriasis and psoriatic arthritis) by blocking the synthesis of a range of pro-flammatory cytokines and chemokines, including tumor necrosis factor alpha, interleukin 23, CXCL9 and CXCL10.

Reference

[1].Georg Schett, Victor S. Sloan, Randall M. Stevens and Peter Schafer. Apremilast: a novel PDE4 inhibitor in the treatment of autoimmune and inflammatory disease. Ther Adv Musculoskelet Dis. 2010; 2(5): 271-278