Apremilast (CC-10004)
Catalog #
27735-1
$260
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Description
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.
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Synonyms
Apremilast; CC-10004; N-[2-[(1S)-1-(3-ethoxy-4-methoxyphenyl)-2-methylsulfonylethyl]-1,3-dioxoisoindol-4-yl]acetamide
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Product Data Gallery
Product Info
Storage and Usage
Citations
Purity
≥98%
Target(s)
PDE4
Formula
C22H24N2O7S
MW
460.5 Da
Solubility
≥23.05 mg/mL in DMSO; insoluble in H2O; insoluble in EtOH. For obtaining a higher solubility, please warn the tube at 37°C and shake in the ultrasonic bath for a while.
Biological Activity
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.
CAS Registry #
608141-41-9
References
Schett, G., et al. Ther Adv Musculoskelet Dis. 2010; 2(5): 271-278.
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