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PH-797804

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Chemical Structure| 586379-66-0 同义名 : -
CAS号 : 586379-66-0
货号 : A369134
分子式 : C22H19BrF2N2O3
纯度 : 98%
分子量 : 477.299
MDL号 : MFCD18251426
存储条件：

粉末 Sealed in dry,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(104.76 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
动物实验配方：
生物活性
靶点

  • p38β

    p38β, IC50:102 nM

  • p38α

    p38α, IC50:26 nM
描述 PH-797804 is a pyridinone inhibitor of p38α with IC50 of 26 nM, being 4-fold selective versus p38β and does not inhibit JNK2.
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
human monocytes Function assay Antiinflammatory activity in human monocytes assessed as inhibition of LPS-induced TNFalpha production, IC50=0.0034 μM 21620699
human PBMC Function assay Antiinflammatory activity in human PBMC assessed as inhibition of LPS-induced TNFalpha release pretreated for 1 hr before LPS treatment measured after 18 hrs, IC50=0.015 μM 21641211
human U937 cells Function assay Inhibition of p38alpha kinase-dependent HSP-27 phosphorylation in human U937 cells, IC50=0.00105 μM 21620699
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
NCT01314885 Chronic Obstructive Pulmonary ... 展开 >>Disease (COPD) 收起 << Phase 1 Completed - United Kingdom ... 展开 >> Pfizer Investigational Site London, United Kingdom, SE1 1YR Pfizer Investigational Site Manchester, United Kingdom, M23 9QZ 收起 <<
NCT00827515 Pain Phase 1 Withdrawn May 2009 -
NCT00383188 Arthritis, Rheumatoid Phase 2 Completed - -
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.10mL

0.42mL

0.21mL

10.48mL

2.10mL

1.05mL

20.95mL

4.19mL

2.10mL
参考文献

[1]Hope HR, Anderson GD, et al. Anti-inflammatory properties of a novel N-phenyl pyridinone inhibitor of p38 mitogen-activated protein kinase: preclinical-to-clinical translation. J Pharmacol Exp Ther. 2009 Dec;331(3):882-95.

[2]Xing L, Shieh HS, et al. Structural bioinformatics-based prediction of exceptional selectivity of p38 MAP kinase inhibitor PH-797804. Biochemistry. 2009 Jul 14;48(27):6402-11.