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PH-797804

现货
Catalog No.
A8308
P38 MAP激酶抑制剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 2,240.00
现货
5mg
¥ 1,200.00
现货
25mg
¥ 3,800.00
Ship with 10-15 days

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Background

PH-797804 is a novel, potent, ATP-competitive and reversible inhibitor of human p38 MAP kinase. It specifically inhibits p38α with IC50 value of 26 nM and K(i) value of 5.8 nM.

PH-797804 inhibits LPS induced TNF-α and IL-1β production in monocytes with a concentration-dependently manner. PH-797804 blocks RANKL and M-CSF induced osteoclast formation in primary rat bone marrow cells.

Orally administered PH-797804 suppresses TNF-α level in a dose-dependent manner in LPS induced Lewis rats and also in cynomolgus monkeys. Additionally, PH-797804 has been shown to inhibit chronic inflammation in arthritis models induced by mouse collagen-induced or rat streptococcal cell wall (SCW) extract.

References:
[1] Hope HR1, Anderson GD, Burnette BL, Compton RP, Devraj RV, Hirsch JL, Keith RH, Li X, Mbalaviele G, Messing DM, Saabye MJ,Schindler JF, Selness SR, Stillwell LI, Webb EG, Zhang J, Monahan JB. 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.

文献引用

1. Zheng, Lufeng, et al. "The 3′ UTR of the pseudogene CYP4Z2P promotes tumor angiogenesis in breast cancer by acting as a ceRNA for CYP4Z1." Breast cancer research and treatment (2015): 1-14. PMID:25701119

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt477.3
Cas No.586379-66-0
FormulaC22H19BrF2N2O3
SynonymsPH797804;PH 797804
Solubility≥23.85mg/mL in DMSO, <2.51 mg/mL in EtOH, <2.22 mg/mL in H2O
Chemical Name3-[3-bromo-4-[(2,4-difluorophenyl)methoxy]-6-methyl-2-oxopyridin-1-yl]-N,4-dimethylbenzamide
SDFDownload SDF
Canonical SMILESCC1=C(C=C(C=C1)C(=O)NC)N2C(=CC(=C(C2=O)Br)OCC3=C(C=C(C=C3)F)F)C
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

生物活性

描述 PH-797804是p38α的新型吡啶酮抑制剂,IC50值为26 nM,比对p38β的选择性高4倍。
靶点 p38α          
IC50 26 nM          

质量控制

化学结构

PH-797804

相关生物数据

PH-797804

相关生物数据

PH-797804

相关生物数据

PH-797804