CS-2524

CS-2524

中文名称CS-2524
中文同义词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;化合物TM5275 SODIUM;PAI-1抑制剂(TM5275 SODIUM);TM5275钠盐
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C28H29ClN3NaO5
分子量546
EINECS号
相关类别细胞生物学试剂
Mol文件1103926-82-4.mol
结构式CS-2524 结构式

CS-2524 性质

储存条件2-8°C
溶解度DMSO:20.0(最大浓度 mg/mL);36.77(最大浓度 mM)
DMF:PBS (pH 7.2) (1:8):0.11(最大浓度 mg/mL);0.2(最大浓度.mM)
DMF:33.0(最大浓度 mg/mL);60.66(最大浓度 mM)
形态粉末
颜色白色至米色

CS-2524 用途与合成方法

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。
TargetValue
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).

安全信息

危险品运输编号UN 3077 9 / PGIII

MSDS信息

更新日期产品编号产品名称CAS号包装价格
2024/08/19HY-100447TM5275 sodium1 mg500元
2024/08/19HY-100447CS-2524
TM5275 sodium
1103926-82-45mg998元

CS-2524 上下游产品信息

"CS-2524"相关产品信息
CS-2510
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