中文名：帕马皮莫德
英文名：Pamapimod
纯度：Moligand™，≥99%
货号：P413914
Cas号：449811-01-2
存储温度：-20°C储存
运输条件：超低温运输
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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关键字： 帕吡莫德;AC-33182 ; DEGARELIX [USAN] ; DTXSID6040244
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