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Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $51 | In Stock | |
5 mg | $122 | In Stock | |
10 mg | $197 | In Stock | |
25 mg | $397 | In Stock | |
50 mg | $637 | In Stock | |
100 mg | $897 | In Stock | |
500 mg | $1,790 | In Stock | |
1 mL x 10 mM (in DMSO) | $133 | In Stock |
Description | Pamapimod (R1503) (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. |
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[1]. |
In vivo | 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]. |
Alias | R1503, Ro4402257 |
Molecular Weight | 406.38 |
Formula | C19H20F2N4O4 |
Cas No. | 449811-01-2 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | ||||||||||||||||||||||||||||||||||||||||
Solubility Information | H2O: < 1 mg/mL (insoluble or slightly soluble) Ethanol: 27 mg/mL (66.4 mM) DMSO: 45 mg/mL (110.73 mM) | ||||||||||||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||||||||||||
DMSO/Ethanol
DMSO
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