Apremilast (CC-10004) (Synonyms: APR, CC-10004) |
| カタログ番号GC10420 |
経口投与可能なPDE4阻害剤
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 608141-41-9
Sample solution is provided at 25 µL, 10mM.
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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 IC50 and affinity constant Kiof 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
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
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