生物活性 靶点 体外研究 体内研究 4-(3-苄基-4-((5-(2-氟苯基)呋喃-2-基)亚甲基)-5-氧代-4,5-二氢-1H-吡唑-1-基)苯甲酸 试剂级价格
ChemicalBook  CAS数据库列表  4-(3-苄基-4-((5-(2-氟苯基)呋喃-2-基)亚甲基)-5-氧代-4,5-二氢-1H-吡唑-1-基)苯甲酸

4-(3-苄基-4-((5-(2-氟苯基)呋喃-2-基)亚甲基)-5-氧代-4,5-二氢-1H-吡唑-1-基)苯甲酸

4-(3-苄基-4-((5-(2-氟苯基)呋喃-2-基)亚甲基)-5-氧代-4,5-二氢-1H-吡唑-1-基)苯甲酸,916232-21-8,结构式
4-(3-苄基-4-((5-(2-氟苯基)呋喃-2-基)亚甲基)-5-氧代-4,5-二氢-1H-吡唑-1-基)苯甲酸
  • CAS号:916232-21-8
  • 英文名:GS 143
  • 中文名:4-(3-苄基-4-((5-(2-氟苯基)呋喃-2-基)亚甲基)-5-氧代-4,5-二氢-1H-吡唑-1-基)苯甲酸
  • CBNumber:CB64721604
  • 分子式:C28H19FN2O4
  • 分子量:466.46
  • MOL File:916232-21-8.mol
4-(3-苄基-4-((5-(2-氟苯基)呋喃-2-基)亚甲基)-5-氧代-4,5-二氢-1H-吡唑-1-基)苯甲酸化学性质
  • 沸点 :667.9±65.0 °C(Predicted)
  • 密度 :1.30±0.1 g/cm3(Predicted)
  • 储存条件 :2-8°C
  • 溶解度 :DMF:25.0(Max Conc. mg/mL);53.59(Max Conc. mM)
    DMF:PBS (pH 7.2) (1:4):0.2(Max Conc. mg/mL);0.43(Max Conc. mM)
    DMSO:31.38(Max Conc. mg/mL);67.28(Max Conc. mM)
  • 形态 :A crystalline solid
  • 酸度系数(pKa) :4.20±0.10(Predicted)
  • 颜色 :Pink to red

4-(3-苄基-4-((5-(2-氟苯基)呋喃-2-基)亚甲基)-5-氧代-4,5-二氢-1H-吡唑-1-基)苯甲酸性质、用途与生产工艺

  • 生物活性 GS143 是一种选择性的 IκBα 泛素化抑制剂,对于 SCFβTrCP1 介导的 IκBα 泛素化作用的 IC50 为 5.2 μM。GS143 抑制靶基因的 NF-κB 活化和转录,并且不抑制蛋白酶体的活性,并具有抗哮喘作用。
  • 靶点

    IC50: 5.2 μM (SCF βTrCP1 -mediated IκBα ubiquitylation)

  • 体外研究

    GS143 (10 μM or 20 μM) inhibits antigen-induced differentiation of Th2 cells but not of Th1 cells in vitro. The IL-4 pro­duc­tion in Th2-polar­iz­ing con­di­tion is mark­edly sup­pressed by GS143 in a dose-depen­dent man­ner.
    GS143 suppresses the transcription of TNFα-induced NF-κB with a mean IC 50 value of 10.5 μM. GS143 also inhibits TNFα-induced expression of ICAM-1 in HT-29 colon cancer cells with an IC 50 value of 6.1 μM. The production levels of TNFα and IL-1β in LPS-activated THP-1 cells are inhibited with IC 50 values of 5.3 μM and 2.1 μM, respectively. GS143 does not inhibit p53 and β-catenin.

  • 体内研究

    GS143 (16-32 μg/body; intranasal administration; once; BALB/c mice) treatment suppresses antigen-induced NF-κB activation in the lung of sensitized mice. GS143 treatment also inhibits antigen-induced eosinophil and lymphocyte recruitment into the airways and the expression of Th2 cytokines and eotaxin in the airways.

    Animal Model: BALB/c mice (age 7-8weeks) injected with oval­bu­min
    Dosage: 16 μg/body or 32 μg/body
    Administration: Intranasal administration; once
    Result: Suppressed antigen-induced NF-κB activation in the lung of sensitized mice.
4-(3-苄基-4-((5-(2-氟苯基)呋喃-2-基)亚甲基)-5-氧代-4,5-二氢-1H-吡唑-1-基)苯甲酸上下游产品信息
上游原料
下游产品
4-(3-苄基-4-((5-(2-氟苯基)呋喃-2-基)亚甲基)-5-氧代-4,5-二氢-1H-吡唑-1-基)苯甲酸 试剂级价格
  • 更新日期:2024/08/19
  • 产品编号:HY-110261
  • 产品名称:GS143
  • CAS编号:
  • 包装:1 mg
  • 价格:400元
  • 更新日期:2024/08/19
  • 产品编号:HY-110261
  • 产品名称:4-(3-苄基-4-((5-(2-氟苯基)呋喃-2-基)亚甲基)-5-氧代-4,5-二氢-1H-吡唑-1-基)苯甲酸 GS143
  • CAS编号:916232-21-8
  • 包装:5mg
  • 价格:1000元
4-(3-苄基-4-((5-(2-氟苯基)呋喃-2-基)亚甲基)-5-氧代-4,5-二氢-1H-吡唑-1-基)苯甲酸生产厂家
  • 公司名称:TOCRIS-US
  • 联系电话:--
  • 电子邮件:customerservice@tocris.co.uk
  • 国家:英国
  • 产品数:5729
  • 优势度:77
916232-21-8, 4-(3-苄基-4-((5-(2-氟苯基)呋喃-2-基)亚甲基)-5-氧代-4,5-二氢-1H-吡唑-1-基)苯甲酸相关搜索: