产品
编 号:F273731
分子式:C27H24FN3O
分子量:425.5
产品类型
结构图
CAS No: 215303-72-3
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产品详情
生物活性:
RWJ-67657 (JNJ 3026582) is an orally active and selective p38α and p38β MAPK inhibitor with IC50s of 1 and 11 μM, respectively. RWJ-67657 displays no activity at p38γ and p38δ, and exhibits cardio protective effect. Anti-inflammatory and anti-tumor activity.
体内研究:
RWJ-67657 inhibits 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. RWJ-67657 (50 mg/kg; administered orally; once per day for 7 consecutive days) displays a potent anti-inflammatory effect. By both improving the functioning of endothelial progenitor cells (EPCs) and reducing inflammation, EPC transplantation plus RWJ-67657 administration synergistically promotes angiogenesis and neurogenesis after diabetic stroke.Animal Model:The db/db mice (male, 8 weeks old) with EPCs
Dosage:50 mg/kg
Administration:Administered orally; once per day for 7 consecutive days
Result:Increased angiogenesis and neurogenesis of diabetic mice after cotreatment with EPCs transplantation.
体外研究:
RWJ-67657 inhibits the release of TNF-α by lipopolysaccharide (LPS)-treated human peripheral blood mononuclear cells with an IC50 of 3 nM, as well as the release of TNF-α from peripheral blood mononuclear cells treated with the superantigen staphylococcal enterotoxin B, with an IC50 value of 13 nM. RWJ67657 (10 μM; 24 hours) decreases colony formation in MCF-7 cells.