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编 号:F052264
分子式:C16H14Cl2FN3S
分子量:370.27
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生物活性:
SKF-86002 dihydrochloride is an orally active p38 MAPK inhibitor, with anti-inflammatory, anti-arthritic and analgesic activities. SKF-86002 dihydrochloride inhibits lipopolysaccharide (LPS)-stimulate human monocyte IL-1 and TNF-α production (IC50 = 1 μM). SKF-86002 dihydrochloride inhibits lipoxygenase- and cyclooxygenase-mediated metabolism of arachidonic acid.

体内研究:
SKF-86002 dihydrochloride (10-90 mg/kg; p.o.; daily; for 22 days) has antiarthritic activity.Animal Model:Lewis rats, with adjuvant-induced arthritis (AA)
Dosage:10 mg/kg, 30 mg/kg, 90 mg/kg
Administration:Oral administration, daily, for 22 days
Result:Significantly decreased hindleg volumes after injection of adjuvant.

体外研究:
SKF-86002 dihydrochloride (10 μM; 1 hour) inhibits apoptosis induced by stress stimulation with UV irradiation (UV).SKF-86002 dihydrochloride does not inhibit UV-induced apoptosis in undifferentiated HL-60 cells.SKF-86002 dihydrochloride (10 μM; 72 hours) prevent IL-4-induced monocyte or U937 cell CD23 surface expression and protein formation with no effect on CD23 mRNA levels.
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