Apremilast

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Chemical Structure| 608141-41-9 同义名 : 阿普斯特 ;CC-10004; APR
CAS号 : 608141-41-9
货号 : A227494
分子式 : C22H24N2O7S
纯度 : 98%
分子量 : 460.5
MDL号 : MFCD18782607
存储条件：

Pure form Inert atmosphere, room temperature

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 45 mg/mL(97.72 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
生物活性
靶点

  • TNF-α

    TNF-α, IC50:77 nM

  • PDE4

    PDE4, IC50:74 nM
描述 Apremilast is a small molecule inhibitor of PDE4 with an IC50 value of 74 nM.
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.17mL

0.43mL

0.22mL

10.86mL

2.17mL

1.09mL

21.72mL

4.34mL

2.17mL
参考文献

[1]Chen LG, Wang Z, et al. Determination of Apremilast in Rat Plasma by UPLC-MS-MS and Its Application to a Pharmacokinetic Study. J Chromatogr Sci. 2016 Sep;54(8):1336-40.

[2]Perez-Aso M, Montesinos MC, et al. Apremilast, a novel phosphodiesterase 4 (PDE4) inhibitor, regulates inflammation through multiple cAMP downstream effectors. Arthritis Res Ther. 2015 Sep 15;17:249.