中文名 | TM5275 (sodium) |
英文名 | TM5275 (sodium) |
别名 | 化合物TM5275 SODIUM PAI-1抑制剂(TM5275 SODIUM) 2-(2-(2-(4-二苯甲基哌嗪-1-基)-2-氧代乙氧基)乙酰氨基)-5-氯苯甲酸钠盐 |
英文别名 | CS-2524 TM-5275 TM 5275 TM5275 (sodium) TM 5275 sodium salt 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 |
CAS | 1103926-82-4 |
化学式 | C28H29ClN3NaO5 |
分子量 | 546 |
溶解度 | DMSO: ≥ 100 mg/mL |
存储条件 | 2-8°C |
外观 | 粉末 |
颜色 | white to beige |
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). |
危险品运输编号 | UN 3077 9 / PGIII |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 1.835 ml | 9.175 ml | 18.349 ml |
5 mM | 0.367 ml | 1.835 ml | 3.67 ml |
10 mM | 0.183 ml | 0.917 ml | 1.835 ml |
5 mM | 0.037 ml | 0.183 ml | 0.367 ml |
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