Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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.
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
1 mg | In stock | $ 51.00 | |
5 mg | In stock | $ 122.00 | |
10 mg | In stock | $ 197.00 | |
25 mg | In stock | $ 397.00 | |
50 mg | In stock | $ 637.00 | |
100 mg | In stock | $ 897.00 | |
500 mg | In stock | $ 1,790.00 | |
1 mL * 10 mM (in DMSO) | In stock | $ 133.00 |
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. |
Targets&IC50 | p38β:0.48±0.04 μM, p38α:0.014 ±0.002μM |
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]. |
Synonyms | R1503, Ro4402257 |
Molecular Weight | 406.38 |
Formula | C19H20F2N4O4 |
CAS No. | 449811-01-2 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: < 1 mg/mL (insoluble or slightly soluble)
Ethanol: 27 mg/mL (66.4 mM)
DMSO: 75 mg/mL (184.6 mM)
You can also refer to dose conversion for different animals. More
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Pamapimod 449811-01-2 Autophagy MAPK p38 MAPK Ro-4402257 Inhibitor R1503 IL-6 TNF-α inhibit IL-1β JNK R-1503 p38β Ro 4402257 Ro4402257 p38α anti-inflammation LPS R 1503 inhibitor