PamaPimod 是一种新型的选择性 p38 丝裂原活化蛋白激酶抑制剂，对于p38α和p38β的IC50分别为 14 nM 和 480 nM，Ki分别为 1.3 nM 和 120 nM，对 p38δ 或 p38γ 亚型没有活性，可研究类风湿关节炎和其他自身免疫性疾病。

Pamapimod (R-1503, Ro4402257) is a novel, selective inhibitor of p38 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 p38 gamma isoforms.

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[1].

In murine collagen-induced arthritis, pamapimod reduced Clinicalal 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[1].

449811-01-2

C19H20F2N4O4

406.38

帕吡莫德;R1503;Ro4402257

H2O:<1 mgml
Ethanol:27 mg/mL (66.4 mM)
DMSO:75 mg/mL (184.6 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years