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Apremilast

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产品名称: Apremilast
产品型号: GOY-Y1907
产品展商: 谷研
产品文档: 无相关文档
发布时间:2023-04-25

简单介绍

Apremilast ≥ 23.05 mg/mL in DMSO


Apremilast  的详细介绍

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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