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首页-小分子抑制剂&激动剂-Ras-Raf-MAPK-ERK Pathway-p38 MAPK-PH-797804
PH-797804

Chemical Structure : PH-797804

CAS No.: 586379-66-0

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PH-797804 (PH797804)

货号: PC-21598Not For Human Use, Lab Use Only.

PH-797804 is a potent, highly selective and ATP-competitive p38α/p38β MAPK inhibitor with IC50 of 2.3 nM (p38α).

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5 mg ￥880 In stock
10 mg ￥1280 In stock
25 mg ￥2180 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

PH-797804 is a potent, highly selective and ATP-competitive p38α/p38β MAPK inhibitor with IC50 of 2.3 nM (p38α).
PH-797804 exhibits significant inhibition of TNFα release in hPBMC with IC50 of 3.4 nM.
PH-797804 is a readily reversible inhibitor of the alpha isoform of human p38 MAP kinase with Ki of 5.8 nM.
PH-797804 blocks inflammation-induced production of cytokines and proinflammatory mediators, such as prostaglandin E(2) in human monocyte and synovial fibroblast cell systems.
PH-797804 effectively inhibits acute inflammatory responses induced by systemically administered endotoxin in both rat and cynomolgus monkeys.
PH-797804 demonstrates robust anti-inflammatory activity in chronic disease models, significantly reducing both joint inflammation and associated bone loss in streptococcal cell wall-induced arthritis in rats and mouse collagen-induced arthritis.

物理化学性质&存储条件

分子量 477.31
分子式 C22H19BrF2N2O3
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

3-[3-bromo-4-[(2,4-difluorophenyl)methoxy]-6-methyl-2-oxopyridin-1-yl]-N,4-dimethylbenzamide

参考文献

1. Selness SR, et al. Bioorg Med Chem Lett. 2011 Jul 1;21(13):4066-71.

2. Hope HR, et al. J Pharmacol Exp Ther. 2009 Dec;331(3):882-95.

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