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Pamapimod(R-1503,Ro4402257)
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。
Pamapimod(R-1503,Ro4402257)图片
CAS NO:449811-01-2
包装与价格：
包装价格(元)
1mg电议
5mg电议

产品介绍
Pamapimod (R-1503, Ro4402257) (Ro4402257) 是一种有效的、选择性的、具有口服活性的 p38 MAPK 抑制剂，对 p38α 的 IC50 为 14 nM 和 480 nM，Kis 分别为 1.3 nM 和 120 nM；和 p38β，分别。
Cas No.449811-01-2
别名Ro4402257; R1503
化学名6-(2,4-difluorophenoxy)-2-((1,5-dihydroxypentan-3-yl)amino)-8-methylpyrido[2,3-d]pyrimidin-7(8H)-one
Canonical SMILESO=C1C(OC2=CC=C(F)C=C2F)=CC3=CN=C(NC(CCO)CCO)N=C3N1C
分子式C19H20F2N4O4
分子量406.38
溶解度DMF: 30 mg/ml,DMSO: 30 mg/ml,DMSO:PBS(pH 7.2) (1:3): 0.25 mg/ml,Ethanol: 0.33 mg/ml
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

IC50: 0.014 and 0.48 μM for p38α and p38β enzymatic activity, respectively.

Pamapimod (R-1503, Ro4402257) is a p38 MAPK inhibitor.

P38alpha, a protein kinase, regulates the inflammatory cytokine expression, indicating a key role in the pathogenesis of diseases such as rheumatoid arthritis and systemic lupus erythematosus.

In vitro: Pamapimod could inhibit p38alpha and p38beta enzymatic activity, and there was no activity against p38delta or p38gamma. When profiled across 350 kinases, pamapimod bound only to four kinases. Moreover, pamapimod was found to inhibit p38, but JNK inhibition was not detected. Pamapimod also inhibited LPS-stimulated TNFα production by monocytes, IL-1β production. In addition, LPS- and TNFα-stimulated production of TNFα and IL-6 in rodent plasma could be also inhibited by pamapimod [1].

In vivo: In murine collagen-induced arthritis, pamapimod was able to reduce the clinical signs of inflammation and bone loss at 50 mg/kg or greater. Moreover, pamapimod dose-dependently increased the tolerance pressure in a rat model of hyperalgesia, indicating the critical role of p38 in pain associated with inflammation. Furthermore, a pamapimod analog had equivalent potency and selectivity in lupus-prone MRL/lpr mice [1].

Clinical trial: Up to now, pamapimod is still in the preclinical development stage.

Reference:
[1] Hill, R.  J. et al. Pamapimod, a novel p38 mitogen-activated protein kinase inhibitor: preclinical analysis of efficacy and selectivity. The Journal of pharmacology and experimental therapeutics 327, 610-619, doi:10.1124/jpet.108.139006 (2008).