您好,欢迎来到化工原料网! [登录] [免费注册]
化工原料网
位置:首页 > 产品库 > Pamapimod(R-1503,Ro4402257)
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
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
规格:98%
分子量:406.38
包装与价格:
包装价格(元)
1mg电议
5mg电议

产品介绍
p38 MAPK inhibitor
CAS:449811-01-2
分子式:C19H20F2N4O4
分子量:406.38
纯度:98%
存储:Store at -20°C

Background:

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).