RWJ-67657

    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 510234

CAS#: 215303-72-3

Description: RWJ-67657 is a potent p38 MAPK inhibitor, which inhibited the release of TNF-alpha by lipopolysaccharide (a monocyte stimulus)-treated human peripheral blood mononuclear cells with an IC(50) of 3 nM, as well as the release of TNF-alpha from peripheral blood mononuclear cells treated with the superantigen staphylococcal enterotoxin B (a T cell stimulus), with an IC(50) value of 13 nM. This compound was approximately 10-fold more potent than the literature standard p38 kinase inhibitor SB 203580 in all p38 dependent in vitro systems tested.


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This agent is available through custom synthesis (minimum order requested).


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 510234
Name: RWJ-67657
CAS#: 215303-72-3
Chemical Formula: C27H24FN3O
Exact Mass: 425.19034
Molecular Weight: 425.49736
Elemental Analysis: C, 76.21; H, 5.69; F, 4.46; N, 9.88; O, 3.76


Synonym: RWJ67657; RWJ-67657; RWJ 67657

IUPAC/Chemical Name: 4-(4-(4-fluorophenyl)-1-(3-phenylpropyl)-5-(pyridin-4-yl)-1H-imidazol-2-yl)but-3-yn-1-ol

SMILES Code: OCCC#CC1=NC(C2=CC=C(F)C=C2)=C(C3=CC=NC=C3)N1CCCC4=CC=CC=C4


Technical Data

Appearance:
white solid powder

Purity:
>98% (or refer to the Certificate of Analysis)

Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition:
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility:
Soluble in DMSO, not in water

Shelf Life:
>2 years if stored properly

Drug Formulation:
This drug may be formulated in DMSO

Stock Solution Storage:
0 - 4 C for short term (days to weeks), or -20 C for long term (months).

Harmonized System Code:
293490


Additional Information

  
  
 
 


References

1: Westra J, Kułdo JM, van Rijswijk MH, Molema G, Limburg PC. Chemokine production and E-selectin expression in activated endothelial cells are inhibited by p38 MAPK (mitogen activated protein kinase) inhibitor RWJ 67657. Int Immunopharmacol. 2005 Jul;5(7-8):1259-69. Epub 2005 Apr 26. PubMed PMID: 15914330.

2: Westra J, Limburg PC, de Boer P, van Rijswijk MH. Effects of RWJ 67657, a p38 mitogen activated protein kinase (MAPK) inhibitor, on the production of inflammatory mediators by rheumatoid synovial fibroblasts. Ann Rheum Dis. 2004 Nov;63(11):1453-9. PubMed PMID: 15479895; PubMed Central PMCID: PMC1754789.

3: Westra J, Doornbos-van der Meer B, de Boer P, van Leeuwen MA, van Rijswijk MH, Limburg PC. Strong inhibition of TNF-alpha production and inhibition of IL-8 and COX-2 mRNA expression in monocyte-derived macrophages by RWJ 67657, a p38 mitogen-activated protein kinase (MAPK) inhibitor. Arthritis Res Ther. 2004;6(4):R384-92. Epub 2004 Jun 21. PubMed PMID: 15225374; PubMed Central PMCID: PMC464924.

4: Parasrampuria DA, de Boer P, Desai-Krieger D, Chow AT, Jones CR. Single-dose pharmacokinetics and pharmacodynamics of RWJ 67657, a specific p38 mitogen-activated protein kinase inhibitor: a first-in-human study. J Clin Pharmacol. 2003 Apr;43(4):406-13. PubMed PMID: 12723461.

5: Faas MM, Moes H, Fijen JW, Muller Kobold AC, Tulleken JE, Zijlstra JG. Monocyte intracellular cytokine production during human endotoxaemia with or without a second in vitro LPS challenge: effect of RWJ-67657, a p38 MAP-kinase inhibitor, on LPS-hyporesponsiveness. Clin Exp Immunol. 2002 Feb;127(2):337-43. PubMed PMID: 11876759; PubMed Central PMCID: PMC1906333.

6: Fijen JW, Zijlstra JG, De Boer P, Spanjersberg R, Tervaert JW, Van Der Werf TS, Ligtenberg JJ, Tulleken JE. Suppression of the clinical and cytokine response to endotoxin by RWJ-67657, a p38 mitogen-activated protein-kinase inhibitor, in healthy human volunteers. Clin Exp Immunol. 2001 Apr;124(1):16-20. PubMed PMID: 11359438; PubMed Central PMCID: PMC1906020.

7: Wadsworth SA, Cavender DE, Beers SA, Lalan P, Schafer PH, Malloy EA, Wu W, Fahmy B, Olini GC, Davis JE, Pellegrino-Gensey JL, Wachter MP, Siekierka JJ. RWJ 67657, a potent, orally active inhibitor of p38 mitogen-activated protein kinase. J Pharmacol Exp Ther. 1999 Nov;291(2):680-7. PubMed PMID: 10525088.