Oglemilast

产品说明书

Print
Chemical Structure| 778576-62-8 同义名 : GRC 3886
CAS号 : 778576-62-8
货号 : A613618
分子式 : C20H13Cl2F2N3O5S
纯度 : 99%+
分子量 : 516.3
MDL号 : MFCD18633298
存储条件：

Pure form Inert atmosphere, store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 : -
动物实验配方：
生物活性
描述 Oglemilast, identified as GRC 3886, is a highly effective and orally available inhibitor of phosphodiesterase-4 (PDE4), with an IC50 value of 0.5 nM for PDE4D3. It is effective in reducing pulmonary cell infiltration, such as eosinophilia and neutrophilia, both in vitro and in vivo, showing potential as a treatment for inflammatory airway conditions[1][2][3].
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
NCT00671073 Pulmonary Disease, Chronic Obs... 展开 >>tructive 收起 << Phase 2 Completed - -
NCT00859404 Asthma Phase 2 Unknown January 2010 India ... 展开 >> Glenmark investigational sites (28) Mumbai, Bangalore etc, India 收起 <<
NCT00322686 Asthma Phase 2 Completed - United States, California ... 展开 >> Forest Investigative Site Los Angeles, California, United States, 90025 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.94mL

0.39mL

0.19mL

9.68mL

1.94mL

0.97mL

19.37mL

3.87mL

1.94mL
参考文献

[1]Giembycz MA. Can the anti-inflammatory potential of PDE4 inhibitors be realized: guarded optimism or wishful thinking? Br J Pharmacol. 2008 Oct;155(3):288-90.

[2]Rabe KF, et al. Update on roflumilast, a phosphodiesterase 4 inhibitor for the treatment of chronic obstructive pulmonary disease. Br J Pharmacol. 2011 May;163(1):53-67.

[3]Moruno-Manchon JF, Koellhoffer EC, Gopakumar J, et al. The G-quadruplex DNA stabilizing drug pyridostatin promotes DNA damage and downregulates transcription of Brca1 in neurons. Aging (Albany NY). 2017;9(9):1957-1970.