Cilomilast

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Chemical Structure| 153259-65-5 同义名 : SB-207499
CAS号 : 153259-65-5
货号 : A292821
分子式 : C20H25NO4
纯度 : 99%
分子量 : 343.42
MDL号 : MFCD00924373
存储条件：

Pure form Sealed in dry, 2-8°C

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

DMSO: 105 mg/mL(305.75 mM)，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

  • PDE4

    LPDE4, IC50:100 nM

    HPDE4, IC50:120 nM
描述 Cilomilast is a potent PDE4 inhibitor with IC50 of about 110 nM, has anti-inflammatory activity and low central nervous system activity.
细胞研究
细胞系 浓度 检测类型 检测时间 活性说明 数据源
human peripheral blood mononuclear cells Function assay Inhibition of TNF-alpha release from human peripheral blood mononuclear cells, IC50=3.467 μM 11755362
sf21 cells Function assay Inhibition of human full length PDE4A4 expressed in baculovirus infected sf21 cells, IC50=0.062 μM 23806553
Sf9 cells Function assay Inhibition of human Phosphodiesterase 4A isoform using construct representing the common region of spliced variants expressed as GST-fusion proteins in Sf9 cells, IC50=0.038 μM 12270195
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00103922 Pulmonary Disease, Chronic Obs... 展开 >>tructive 收起 << Phase 3 Completed - -
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.91mL

0.58mL

0.29mL

14.56mL

2.91mL

1.46mL

29.12mL

5.82mL

2.91mL
参考文献

[1]Griswold DE, Webb EF, et al. SB 207499 (Ariflo), a second generation phosphodiesterase 4 inhibitor, reduces tumor necrosis factor alpha and interleukin-4 production in vivo. J Pharmacol Exp Ther. 1998 Nov;287(2):705-11.

[2]Barnette MS, Christensen SB, et al. SB 207499 (Ariflo), a potent and selective second-generation phosphodiesterase 4 inhibitor: in vitro anti-inflammatory actions. J Pharmacol Exp Ther. 1998 Jan;284(1):420-6.