中文名称:

4-[4-(4-氟苯基)-1-(4-哌啶基)-1H-咪唑-5-基]-2-甲氧基嘧啶

中文同义词:

4-[4-(4-氟苯基)-1-(4-哌啶基)-1H-咪唑-5-基]-2-甲氧基嘧啶;P38MAP激酶抑制剂(SB 242235);化合物SB242235

英文名称:

SB242235

英文同义词:

SB-242235; SB242235;CS-668;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;SB242235 ≥95%;Pyrimidine, 4-[4-(4-fluorophenyl)-1-(4-piperidinyl)-1H-imidazol-5-yl]-2-methoxy-

CAS号:

193746-75-7

分子式:

C19H20FN5O

分子量:

353.39

EINECS号:

相关类别:

细胞生物学试剂

Mol文件:

193746-75-7.mol

沸点 

568.4±60.0 °C(Predicted)

密度 

1.34

储存条件 

Keep in dark place,Sealed in dry,2-8°C

酸度系数(pKa)

9.91±0.10(Predicted)

生物活性

SB-242235　是一种有效、选择性的　p38 MAP 激酶抑制剂，在人的软骨细胞中　IC50　值为 1.0 μM。

靶点

IC50: 1.0　μM (p38 MAPK, primary human chondrocytes)

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.

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.

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.