性能参数
产品名称
Apremilast
规格
10mM (in 1mL DMSO) 5mg 10mg 25mg 50mg
货号
GOY-Y1907
含量
>98.00%
CAS
608141-41-9
别名
N/A
化学名
N-[2-[(1S)-1-(3-ethoxy-4-methoxyphenyl)-2-methylsulfonylethyl]-1,3-dioxoisoindol-4-yl]acetamide
分子式
C22H24N2O7S
分子量
分子 460.5
溶解度
≥ 23.05 mg/mL in DMSO
储存条件
Store at -20°C
General tips
用途
仅供科研
价格
电询
详细内容
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
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