193746-75-7
193746-75-7 结构式
基本信息
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
SB242235
SB242235 ≥95%
SB-242235
SB242235
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-
物理化学性质
| 报价日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
| 2024/04/30 | HY-18306 | 4-[4-(4-氟苯基)-1-(4-哌啶基)-1H-咪唑-5-基]-2-甲氧基嘧啶 SB 242235 | 193746-75-7 | 5mg | 850元 |
| 2024/04/30 | HY-18306 | 4-[4-(4-氟苯基)-1-(4-哌啶基)-1H-咪唑-5-基]-2-甲氧基嘧啶 SB 242235 | 193746-75-7 | 10mM * 1mLin DMSO | 935元 |
| 2024/04/30 | HY-18306 | 4-[4-(4-氟苯基)-1-(4-哌啶基)-1H-咪唑-5-基]-2-甲氧基嘧啶 SB 242235 | 193746-75-7 | 10mg | 1450元 |
常见问题列表
IC50: 1.0 μM (p38 MAPK, primary human chondrocytes)
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. |
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. |