產(chǎn)品目錄

規(guī)格	1mg 5mg
CAS	449811-01-2
別名
化學(xué)名	6-(2,4-difluorophenoxy)-2-((1,5-dihydroxypentan-3-yl)amino)-8-methylpyrido[2,3-d]pyrimidin-7(8H)-one
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
儲(chǔ)存條件	Store at -20°C
General tips	For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition	Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request

產(chǎn)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.

特別提醒：

1. 本產(chǎn)品僅供科研使用。請(qǐng)勿用于醫(yī)藥、臨床診斷或治療，食品及化妝品等用途。請(qǐng)勿存放于普通住宅區(qū)。

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原創(chuàng)作者：上海莼試生物技術(shù)有限公司

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