帕马皮莫德，449811-01-2，10mM in DMSO

中文名：帕马皮莫德

英文名：Pamapimod

英文别名：Pamapimod|449811-01-2|RO 4402257|R1503|PamapimodR-1503|Ro4402257|Ro-4402257|CHEMBL1090089|CHEBI:90685|R-1503|8S2C9V11K4|6-(2,4-Difluorophenoxy)-2-{[3-Hydroxy-1-(2-Hydroxyethyl)propyl]amino}-8-Methylpyrido[2,3-D]pyrimidin-7(8h)-One|Pamapimod (R-1503, Ro440

纯度：10mM in DMSO

货号：P424045

Cas号：449811-01-2

存储温度：-80℃储存

产品介绍：

Information

Pamapimod (R-1503, Ro4402257) is a novel, selective inhibitor ofp38 mitogen-activated protein kinase. It inhibits p38α and p38β enzymatic activity with IC50 values of 0.014±0.002 and 0.48± 0.04 microM, respectively with no activity against p38delta or p38gamma isoforms.

Targets

p38α (Cell-free assay); p38β (Cell-free assay) 0.014 μM; 0.48 μM

In vitro

Pamapimod inhibited p38, but inhibition of JNK was not detected. Pamapimod also inhibited lipopolysaccharide (LPS)-stimulated tumor necrosis factor (TNF) α production by monocytes, interleukin (IL)-1β production in human whole blood, and spontaneous TNFα production by synovial explants from RA patients.

In vivo

In murine collagen-induced arthritis, pamapimod reduced clinical signs of inflammation and bone loss at 50 mg/kg or greater. In a rat model of hyperalgesia, pamapimod increased tolerance to pressure in a dose-dependent manner, suggesting an important role of p38 in pain associated with inflammation. Pamapimod suppresses spontaneous production of TNFα by synovial explants from RA patients. LPS- and TNFα-stimulated production of TNFα and IL-6 in rodents also was inhibited by pamapimod.

Cell Research(from reference)

Cell lines：Human Monocytic Cell Line, THP-1 

Concentrations：15 μM 

Incubation Time：150 min 

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