CS-2524
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- CAS号:
- 1103926-82-4
- 英文名:
- TM 5275
- 英文别名:
- CS-2524;TM 5275;TM5275 Na;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;Plasminogen activator inhibitor-1,PAI-1,TM5275,TM5275 sodium,TM-5275 sodium,TM-5275,inhibit,TM 5275,Inhibitor
- 中文名:
- CS-2524
- 中文别名:
- TM5275钠盐;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
- CBNumber:
- CB33146397
- 分子式:
- C28H29ClN3NaO5
- 分子量:
- 546
- MOL File:
- 1103926-82-4.mol
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CS-2524化学性质
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储存条件:
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2-8°C
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溶解度:
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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)-
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形态:
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powder
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颜色:
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white to beige
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CS-2524性质、用途与生产工艺
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。
| Target | Value |
PAI-1
(Cell-free assay)
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6.95 μM
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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).
CS-2524
上下游产品信息
上游原料
下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
|---|
| 2024/04/30 | HY-100447 | TM5275 sodium | | 1 mg | 500元 |
| 2024/04/30 | HY-100447 | CS-2524
TM5275 sodium | 1103926-82-4 | 5mg | 998元 |
1103926-82-4, CS-2524 相关搜索:
- 药靶配体
- 生物试剂
- 细胞生物学试剂
- C28H27ClN3O5Na
- TM5275钠盐
- PAI-1抑制剂(TM5275 SODIUM)
- 化合物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
- 1103926-82-4
- Plasminogen activator inhibitor-1,PAI-1,TM5275,TM5275 sodium,TM-5275 sodium,TM-5275,inhibit,TM 5275,Inhibitor
- TM5275 Na
- TM5275 sodium salt >=98% (HPLC)
- 5-Chloro-2-[[2-[2-[4-(Diphenylmethyl)-1-piperazinyl]-2-oxoethoxy]acetyl]amino]benzoic acid sodium salt
- 2-(2-(2-(4-benzhydrylpiperazin-1-yl)-2-oxoethoxy)acetamido)-5-chlorobenzoic acid sodium salt
- TM 5275;TM-5275
- CS-2524
- TM5275 (sodium)
- TM 5275 sodium salt
- TM 5275