CS-2524

中文名称:

CS-2524

中文同义词:

PAI-1抑制剂(TM5275 SODIUM);化合物TM5275 SODIUM

英文名称:

TM 5275

英文同义词:

TM 5275;TM 5275 sodium salt;TM5275 (sodium);CS-2524;TM 5275;TM-5275;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;TM5275 sodium salt >=98% (HPLC)

CAS号:

1103926-82-4

分子式:

C28H27ClN3O5*Na

分子量:

0

EINECS号:

相关类别:

细胞生物学试剂

Mol文件:

Mol File

储存条件 

2-8°C

形态

powder

颜色

white to beige

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

Target Value PAI-1 (Cell-free assay) 6.95 μM

Target

Value

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).

危险品运输编号 

UN 3077 9 / PGIII