4-[4-(4-氟苯基)-1-(4-哌啶基)-1H-咪唑-5-基]-2-甲氧基嘧啶
| 中文名稱 | 4-[4-(4-氟苯基)-1-(4-哌啶基)-1H-咪唑-5-基]-2-甲氧基嘧啶 |
|---|---|
| 中文同義詞 | 4-[4-(4-氟苯基)-1-(4-哌啶基)-1H-咪唑-5-基]-2-甲氧基嘧啶;P38MAP激酶抑制劑(SB 242235);化合物SB242235;4-(4-(4-氟苯基)-1-(哌啶-4-基)-1H-咪唑-5-基)-2-甲氧基嘧啶 |
| 英文名稱 | SB242235 |
| 英文同義詞 | 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;SB-242235; SB242235;CS-668;SB242235 ≥95%;Pyrimidine, 4-[4-(4-fluorophenyl)-1-(4-piperidinyl)-1H-imidazol-5-yl]-2-methoxy-;inhibit,SB 242235,Autophagy,Inhibitor,p38 MAPK |
| CAS號 | 193746-75-7 |
| 分子式 | C19H20FN5O |
| 分子量 | 353.39 |
| EINECS號 | |
| 相關類別 | 細胞生物學試劑 |
| Mol文件 | 193746-75-7.mol |
| 結構式 | ![4-[4-(4-氟苯基)-1-(4-哌啶基)-1H-咪唑-5-基]-2-甲氧基嘧啶 結構式](CAS/GIF/193746-75-7.gif) |
4-[4-(4-氟苯基)-1-(4-哌啶基)-1H-咪唑-5-基]-2-甲氧基嘧啶 性質
| 沸點 | 568.4±60.0 °C(Predicted) |
|---|---|
| 密度 | 1.34 |
| 儲存條件 | 2-8°C(protect from light) |
| 溶解度 | DMF：25mg/mL； DMSO：20mg/mL；乙醇：30mg/mL |
| 形態(tài) | 粉末 |
| 酸度系數(shù)(pKa) | 9.91±0.10(Predicted) |
| 顏色 | 白色至米白色 |
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. |
安全信息
| 海關編碼 | 2924297099 |
|---|
| 更新日期 | 產(chǎn)品編號 | 產(chǎn)品名稱 | CAS號 | 包裝 | 價格 |
|---|---|---|---|---|---|
| 2024/11/08 | 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 |
| 2024/11/08 | 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 |