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- 详细信息
- 技术资料
- 保存条件：
Powder:-20℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year
- 保质期：
Powder:-20℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year
- 英文名：
TM5275 Sodium
- 库存：
现询
- 供应商：
北京索莱宝科技有限公司
- CAS号：
1103926-82-4
- 规格：
5mg/10mg/25mg/50mg/100mg/1mg
| 规格： | 5mg | 产品价格： | ￥540.0 |
|---|---|---|---|
| 规格： | 10mg | 产品价格： | ￥900.0 |
| 规格： | 25mg | 产品价格： | ￥1720.0 |
| 规格： | 50mg | 产品价格： | ￥2670.0 |
| 规格： | 100mg | 产品价格： | ￥3956.0 |
| 规格： | 1mg | 产品价格： | ￥320.0 |
| 基本信息 | |
| CAS | No.1103926-82-4 |
| 中文名称 | TM5275钠盐 |
| 英文名称 | TM5275 Sodium |
| 别名 | ;TM5275;2-Deoxycytidine; |
| 分子式 | C28H28ClN3NaO5 |
| 分子量 | 544.98 |
| 溶解性 | Soluble in DMSO |
| 纯度 | ≥98% |
| 外观(性状) | White to off-white Solid |
| 储存条件 | Powder:-20℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year |
| MDL | MFCD28396414 |
| SMILES | C1CN(CCN1C(C2=CC=CC=C2)C3=CC=CC=C3)C(=O)COCC(=O)NC4=C(C=C(C=C4)Cl)C(=O)[O-].[Na+] |
| 靶点 | PAI-1 |
| 通路 | Metabolic Enzyme&Protease |
| 背景说明 | TM5275 Sodium是纤溶酶原激活物抑制剂 (PAI-1)。 |
| 生物活性 | TM5275 sodium is a plasminogen activator inhibitor (PAI-1) with an IC50 of 6.95 μM.[1-3] |
| IC50 | IC50: 6.95 μM (PAI-1)[1] |
| In Vitro | 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[1]. 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[2]. 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[3]. |
| 细胞实验 | 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)[1]. |
| 细胞实验 | ES2 cells are treated with DMSO (control) or 100 μM TM5275 for the indicated periods (24， 48， 72， 96 hour). Cell growth is determined by CellTiter-Glo assay[1]. |
| 动物实验 | Rats: Thrombus formation in arteriovenous shunts is achieved in male CD rats. Either TM5275 (10 and 50?mg/kg， n=9) or ticlopidine (500?mg/kg， n=6)， suspended in 0.5% CMC solution， is administered orally by gavage 90?mins before the study. Control rats are administered only a 0.5% CMC solution (n=10). Blood is allowed to circulate through the shunt for 30?mins. The wet weight of the thrombus covering the silk thread is eventually measured[1]. Mice: TM5275 is administered orally by gavage to male ICR mice (50?mg/kg). Heparinized blood samples are collected from the vein before (0?h) and 1， 2， 6， and 24?h after oral drug administration. Plasma drug concentration is determined on a reverse-phase high-performance liquid chromatography[1]. |
| 激酶实验 | 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)[1]. |
| 数据来源文献 | [1]. Izuhara Y， et al. A novel inhibitor of plasminogen activator inhibitor-1 provides antithrombotic benefits devoid of bleeding effect in nonhuman primates. J Cereb Blood Flow Metab. 2010 May;30(5):904-12. [2]. Yasui H， et al. TM5275 prolongs secreted tissue plasminogen activator retention and enhances fibrinolysis on vascular endothelial cells. Thromb Res. 2013 Jul;132(1):100-5. [3]. Mashiko S， et al. Inhibition of plasminogen activator inhibitor-1 is a potential therapeutic strategy in ovarian cancer. Cancer Biol Ther. 2015;16(2):253-60. |
| 单位 | 瓶 |
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IT2770 TM5275钠盐 代谢酶/蛋白酶 索莱宝
￥320 - 3956
