Pamapimod
作者：齐岳
发布时间：2023-09-13
17:11:44
点击数：
产品名称：Pamapimod
产品描述：
| 产品描述 | 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. |
| 靶点活性 | p38β:0.48±0.04 μM, p38α:0.014 ±0.002μM |
| 体外活性 | 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]. |
| 体内活性 | 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]. |
| 别名 | 帕吡莫德, R1503, Ro4402257 |
| 分子量 | 406.38 |
| 分子式 | C19H20F2N4O4 |
| CAS No. | 449811-01-2 |
存储
| Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
H2O: <1 mg/mL
Ethanol: 27 mg/mL (66.4 mM)
DMSO: 75 mg/mL (184.6 mM)
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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