产品
编 号:F241405
分子式:C19H20FN5O
分子量:353.39
产品类型
结构图
CAS No: 193746-75-7
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产品详情
生物活性:
SB-242235 is a potent and selective p38 MAP kinase inhibitor, with an IC50 of 1.0 μM in primary human chondrocytes.
体内研究:
SB242235 (100 mg/kg; p.o.) abolishes MAP-KAPK-2 activity and HSP27 phosphorylation.SB242235 inhibits expression of the pro-inflammatory cytokines interleukin (IL)-6 and KC (murine IL-8) and COX-2.SB-242235 is demonstrated non-linear elimination kinetics that manifested as a decrease in clearance with increasing dose and apparent oral bioavailability > 100% at high oral doses in rat and monkey.Animal Model:Female SKH-1 hairless mice (4–6 weeks)
Dosage:100 mg/kg
Administration:Oral administered, 30 minutes prior to ultraviolet B (UVB) irradiation
Result:Abolished MAP-KAPK-2 activity and heat shock protein 27 (HSP27) phosphorylation.
体外研究:
SB 242235 (0-10 μM) dose-dependently inhibits the activation of MAPKAP K2 with an IC50 of 1.0 μM in human chondrocytes stimulated with IL-1β.SB 242235 inhibits intracellular p38 activity, MAPKAP K2 was then isolated from these cells and assayed using HSP27 as a substrate.