1103926-82-4
基本信息
PAI-1抑制剂(TM5275 SODIUM)
TM 5275
TM 5275
TM-5275
TM5275 (sodium)
TM 5275 sodium salt
TM5275 sodium salt >=98% (HPLC)
2-(2-(2-(4-benzhydrylpiperazin-1-yl)-2-oxoethoxy)acetamido)-5-chlorobenzoic acid sodium salt
5-Chloro-2-[[2-[2-[4-(Diphenylmethyl)-1-piperazinyl]-2-oxoethoxy]acetyl]amino]benzoic acid sodium salt
物理化学性质
| 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 | 粉末 |
| 颜色 | 白色至米色 |
安全数据
| 危险性符号(GHS) |   GHS07,GHS09 |
| 警示词 | 警告 |
| 危险性描述 | H302-H400 |
| 防范说明 | P273-P301+P312+P330 |
| 危险品运输编号 | UN 3077 9 / PGIII |
常见问题列表
| Target | Value |
|
PAI-1
(Cell-free assay) | 6.95 μM |
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.
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).