DC Chemicals Supply: RWJ67657, Cas: 215303-72-3 ,Cat No. DC7491, Purity>98%, In stock.
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RWJ67657|cas 215303-72-3, Synonym name: RWJ-67657; RWJ-67657; RWJ-67657, Chemical name: 4-[4-(4-Fluorophenyl)-1-(3-phenylpr?opyl)-5-(4-pyridinyl)-1H-imidazol-2-yl]-3-butyn-1-?ol, Molecule weight: 425.49736, Molecule Formula: C27H24FN3O
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. RWJ 67657 inhibited the enzymatic activity of recombinant p38alpha and beta, but not gamma or delta, in vitro and had no significant activity against a variety of other enzymes. In contrast, SB 203580 significantly inhibited the tyrosine kinases p56 lck and c-src (IC(50) = 5 microM). RWJ 67657 did not inhibit T cell production of interleukin-2 or interferon-gamma and did not inhibit T cell proliferation in response to mitogens. RWJ 67657 inhibited TNF-alpha production in lipopolysaccharide-injected mice (87% inhibition at 50 mg/kg) and in rats (91% inhibition at 25 mg/kg) after oral administration. Based on these favorable biological properties, RWJ 67657 may have use as a treatment for inflammatory diseases. (copied from J Pharmacol Exp Ther. 1999 Nov;291(2):680-7.) (12/2/2013).
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