生物活性 靶点 体外研究 体内研究 4-[4-(4-氟苯基)-1-(4-哌啶基)-1H-咪唑-5-基]-2-甲氧基嘧啶 试剂级价格
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ChemicalBook  CAS数据库列表  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-(4-哌啶基)-1H-咪唑-5-基]-2-甲氧基嘧啶

生物活性 靶点 体外研究 体内研究 4-[4-(4-氟苯基)-1-(4-哌啶基)-1H-咪唑-5-基]-2-甲氧基嘧啶 试剂级价格
4-[4-(4-氟苯基)-1-(4-哌啶基)-1H-咪唑-5-基]-2-甲氧基嘧啶,193746-75-7,结构式
4-[4-(4-氟苯基)-1-(4-哌啶基)-1H-咪唑-5-基]-2-甲氧基嘧啶
  • CAS号:193746-75-7
  • 英文名:SB242235
  • 中文名:4-[4-(4-氟苯基)-1-(4-哌啶基)-1H-咪唑-5-基]-2-甲氧基嘧啶
  • CBNumber:CB12621150
  • 分子式:C19H20FN5O
  • 分子量:353.39
  • MOL File:193746-75-7.mol
4-[4-(4-氟苯基)-1-(4-哌啶基)-1H-咪唑-5-基]-2-甲氧基嘧啶化学性质
  • 沸点 :568.4±60.0 °C(Predicted)
  • 密度 :1.34
  • 储存条件 :2-8°C(protect from light)
  • 溶解度 :DMF: 25 mg/ml; DMSO: 20 mg/ml; Ethanol: 30 mg/ml
  • 形态 :Powder
  • 酸度系数(pKa) :9.91±0.10(Predicted)
  • 颜色 :White to off-white
安全信息
  • 海关编码 :2924297099

4-[4-(4-氟苯基)-1-(4-哌啶基)-1H-咪唑-5-基]-2-甲氧基嘧啶性质、用途与生产工艺

  • 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.
  • 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.
4-[4-(4-氟苯基)-1-(4-哌啶基)-1H-咪唑-5-基]-2-甲氧基嘧啶上下游产品信息
上游原料
下游产品
4-[4-(4-氟苯基)-1-(4-哌啶基)-1H-咪唑-5-基]-2-甲氧基嘧啶 试剂级价格
  • 更新日期：2024/11/08
  • 产品编号：HY-18306
  • 产品名称：4-[4-(4-氟苯基)-1-(4-哌啶基)-1H-咪唑-5-基]-2-甲氧基嘧啶 SB 242235
  • CAS编号：193746-75-7
  • 包装：5mg
  • 价格：850元
  • 更新日期：2024/11/08
  • 产品编号：HY-18306
  • 产品名称：4-[4-(4-氟苯基)-1-(4-哌啶基)-1H-咪唑-5-基]-2-甲氧基嘧啶 SB 242235
  • CAS编号：193746-75-7
  • 包装：10mM * 1mLin DMSO
  • 价格：935元
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