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PH-797804
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
PH-797804图片
CAS NO:586379-66-0
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
5mg电议
25mg电议

产品介绍
PH-797804 是一种 ATP 竞争性的选择性 p38α/p38β 抑制剂(p38α 的 IC50=26 nM 和 Ki=5.8 nM;p38β 的 Ki=40 nM)并且不抑制 JNK2。
Cas No.586379-66-0
别名PH797804;PH 797804
化学名3-[3-bromo-4-[(2,4-difluorophenyl)methoxy]-6-methyl-2-oxopyridin-1-yl]-N,4-dimethylbenzamide
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
分子式C22H19BrF2N2O3
分子量477.3
溶解度≥ 23.85mg/mL in DMSO
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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.