中文名 | SB 242235 |
英文名 | SB 242235 |
别名 | 化合物SB242235 P38MAP激酶抑制剂(SB 242235) 4-[4-(4-氟苯基)-1-(4-哌啶基)-1H-咪唑-5-基]-2-甲氧基嘧啶 4-(4-(4-氟苯基)-1-(哌啶-4-基)-1H-咪唑-5-基)-2-甲氧基嘧啶 |
英文别名 | CS-668 SB242235 SB242235 SB-242235 SB 242235 4-[4-(4-Fluorophenyl)-1-(4-piperidinyl)-1H-imidazol-5-yl]-2-methoxypyrimidine 4-(4-(4-Fluorophenyl)-1-(piperidin-4-yl)-1H-iMidazol-5-yl)-2-MethoxypyriMidine Pyrimidine, 4-[4-(4-fluorophenyl)-1-(4-piperidinyl)-1H-imidazol-5-yl]-2-methoxy- |
CAS | 193746-75-7 |
化学式 | C19H20FN5O |
分子量 | 353.39 |
密度 | 1.34 |
沸点 | 568.4±60.0 °C(Predicted) |
溶解度 | DMSO: ≥ 48 mg/mL |
酸度系数 | 9.91±0.10(Predicted) |
存储条件 | 2-8°C(protect from light) |
体外研究 | SB 242235 (0-10 μM) dose-dependently inhibits the activation of MAPKAP K2 with an IC 50 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. Western Blot Analysis Cell Line: Human chondrocytes Concentration: 0 μM,0.01 μM,0.1 μM,1 μM,10 μM Incubation Time: 15 minutes Result: Dose-dependently inhibited the activation of MAPKAP K2 with an IC 50 of 1.0 μM. |
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. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.83 ml | 14.149 ml | 28.297 ml |
5 mM | 0.566 ml | 2.83 ml | 5.659 ml |
10 mM | 0.283 ml | 1.415 ml | 2.83 ml |
5 mM | 0.057 ml | 0.283 ml | 0.566 ml |
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