[CAS NO. 449811-01-2] Pamapimod

Name: Pamapimod
Brand: Arctom Scientific
SKU: SLK-S8125

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PRODUCTS SPECIFICATIONS [449811-01-2]

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Catalog

SLK-S8125

Brand

Selleck

CAS

449811-01-2

DESCRIPTION [449811-01-2]

Overview

MDL	MFCD25976551
Molecular Weight	406.38
Molecular Formula	C19H20F2N4O4
SMILES	CN1C=2C(C=C(OC3=C(F)C=C(F)C=C3)C1=O)=CN=C(NC(CCO)CCO)N2

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Concentration Volume Mass	1 mg	5 mg	10 mg
1 mM	2.4608 mL	12.3038 mL	24.6075 mL
5 mM	0.4922 mL	2.4608 mL	4.9215 mL
10 mM	0.2461 mL	1.2304 mL	2.4608 mL
50 mM	0.0492 mL	0.2461 mL	0.4922 mL

Description

Pamapimod (R-1503, Ro4402257) is a novel, selective inhibitor of . 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 ^[1] (Cell-free assay)	p38β ^[1] (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.

References

[1] Hill RJ, et al. J Pharmacol Exp Ther. 2008, 327(3):610-9.

Synonyms

Pyrido[2,3-d]pyrimidin-7(8H)-one, 6-(2,4-difluorophenoxy)-2-[[3-hydroxy-1-(2-hydroxyethyl)propyl]amino]-8-methyl-

6-(2,4-Difluorophenoxy)-2-[[3-hydroxy-1-(2-hydroxyethyl)propyl]amino]-8-methylpyrido[2,3-d]pyrimidin-7(8H)-one

Pamapimod

R 1503

Ro 4402257