生物活性 靶点 体外研究 体内研究 CS-2524 试剂级价格
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CS-2524

CS-2524,1103926-82-4,结构式
CS-2524
  • CAS号:1103926-82-4
  • 英文名:TM 5275
  • 中文名:CS-2524
  • CBNumber:CB33146397
  • 分子式:C28H29ClN3NaO5
  • 分子量:546
  • MOL File:1103926-82-4.mol
CS-2524化学性质
  • 储存条件 :2-8°C
  • 溶解度 :DMSO:20.0(Max Conc. mg/mL);36.77(Max Conc. mM)
    DMF:PBS (pH 7.2) (1:8):0.11(Max Conc. mg/mL);0.2(Max Conc. mM)
    DMF:33.0(Max Conc. mg/mL);60.66(Max Conc. mM)
  • 形态 :powder
  • 颜色 :white to beige
安全信息
  • 危险品运输编号 :UN 3077 9 / PGIII

CS-2524性质、用途与生产工艺

  • 生物活性 TM 5275 sodium 是一种口服的、生物活性的 plasminogen activator inhibitor-1 (PAI-1) 抑制剂,其IC50值为6.95 μM。
  • 靶点
    TargetValue
    PAI-1
    (Cell-free assay)
    6.95 μM
  • 体外研究

    Docking studies shows that TM5275 binds to strand 4 of the A β-sheet (s4A) position of PAI-1. TM5275 is a selective PAI-1 and (up to 100 μM) does not interfere with other serpin/serine protease systems. TM5275 at concentrations of 20 and 100 μM significantly prolongs the retention of tPA-GFP on VECs by inhibiting tPA-GFP-PAI-1 high-molecular-weight complex formation. TM5275 enhances the time-dependent accumulation of plasminogen as well as the dissolution of fibrin clots on and around the tPA-GFP-expressing cells. Cell viability at 72 h treatment is decreased with 70-100 μM TM5275 in ES-2 and JHOC-9 cells. From 48 h up to 96 h, cell growth is suppressed with 100 μM TM5275. Active PAI-1 in cell culture media is significantly decreased in cells treated with 100 μM TM5275 compared to control treatment. TM5275 is suggested to exert anti-proliferative effects in ovarian cancer with high PAI-1 expression.

  • 体内研究

    TM5275 exhibits a favorable pharmacokinetics profile and very low toxicity to mice and rats. In rat thrombosis models. Blood clot weights are significantly lower in rats administered 10 and 50 mg/kg of TM5275 (60.9±3.0 and 56.8±2.8 mg, respectively) than in vehicle-treated rats (72.5±2.0 mg). The antithrombotic effectiveness of TM5275 (50 mg/kg) is equivalent to that of ticlopidine (500 mg/kg), a reference antithrombotic compound. Plasma concentration of TM5275 reaches 17.5±5.2 μM after a dose of 10 mg/kg. TM5275 (5 mg/kg) combined with tPA (0.3 mg/kg) significantly enhances the antithrombotic effect of tPA (0.3 mg/kg) alone and provides a benefit similar to that of a high tPA dose (3 mg/kg).

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CS-2524 试剂级价格
  • 更新日期:2024/08/19
  • 产品编号:HY-100447
  • 产品名称:TM5275 sodium
  • CAS编号:
  • 包装:1 mg
  • 价格:500元
  • 更新日期:2024/08/19
  • 产品编号:HY-100447
  • 产品名称:CS-2524 TM5275 sodium
  • CAS编号:1103926-82-4
  • 包装:5mg
  • 价格:998元
CS-2524生产厂家
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