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- 2025年07月23日
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- 详细信息
- 技术资料
- 保存条件：
Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year
- 保质期：
Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year
- 英文名：
Tiplaxtinin
- 库存：
现询
- 供应商：
北京索莱宝科技有限公司
- CAS号：
393105-53-8
- 规格：
100mg/50mg/20mg/2mg/5mg
| 规格： | 100mg | 产品价格： | ￥5478.0 |
|---|---|---|---|
| 规格： | 50mg | 产品价格： | ￥3640.0 |
| 规格： | 20mg | 产品价格： | ￥1980.0 |
| 规格： | 2mg | 产品价格： | ￥520.0 |
| 规格： | 5mg | 产品价格： | ￥670.0 |
| 基本信息 | |
| CAS | No.393105-53-8 |
| 英文名称 | Tiplaxtinin |
| 别名 | PAI-039 |
| 分子式 | C24H16F3NO4 |
| 分子量 | 439.38 |
| 溶解性 | Soluble in DMSO(Need ultrasonic) |
| 纯度 | ≥98% |
| 外观(性状) | Solid |
| 储存条件 | Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year |
| MDL | MFCD09475615 |
| SMILES | C1=CC=C(C=C1)CN2C=C(C3=C2C=CC(=C3)C4=CC=C(C=C4)OC(F)(F)F)C(=O)C(=O)O |
| InChIKey | ODXQFEWQSHNQNI-UHFFFAOYSA-N |
| InChI | InChI=1S/C24H16F3NO4/c25-24(26，27)32-18-9-6-16(7-10-18)17-8-11-21-19(12-17)20(22(29)23(30)31)14-28(21)13-15-4-2-1-3-5-15/h1-12，14H，13H2，(H，30，31) |
| PubChem CID | 6450819 |
| 靶点 | PAI-1 |
| 通路 | Metabolic Enzyme&Protease |
| 背景说明 | Tiplaxtinin 是一种有效的选择性的纤溶酶原激活物抑制剂-1 (PAI-1) 抑制剂。 |
| 生物活性 | Tiplaxtinin is a selective and orally efficacious inhibitor of plasminogen activator inhibitor-1 (PAI-1) with IC50 of 2.7 μM[1]. |
| IC50 | IC50: 2.7 μM (PAI-1)[1] |
| In Vitro | PAI-1 expression was manipulated in a panel of cell lines and functional inhibition was achieved using the small molecule tiplaxtinin. Reduction or inhibition of PAI-1 resulted in the reduction of cellular proliferation， cell adhesion， and colony formation， and the induction of Apoptosis and anoikis in vitro.Treatment of T24 xenografts with tiplaxtinin resulted in inhibition of angiogenesis and induction of Apoptosis， leading to a significant reduction in tumor growth. Similar results were obtained through evaluation of the human cervical Cancer HeLa cell line， showing that PAI-1-mediated effects are not restricted to tumor cells of bladder origin.[2] |
| 细胞实验 | Carotid artery and vena cava vascular injury was produced by application of FeCl3 and blood flow was monitored using ultrasonic technology. To assess efficacy in a thrombosis prevention paradigm， PAI-039 was administered orally 90 min before injury (1-30 mg kg(-1)). To assess efficacy in a thrombosis treatment paradigm， vascular injury and stable thrombus formation were followed 4 h later by recovery and PAI-039 administration. PAI-039 prevented carotid artery occlusion in 20， 68 and 60% of Animals pretreated with 0.3， 1.0 and 3.0 mg kg(-1)， respectively. Time to occlusive thrombosis was increased from 18.2 +/- 4.6 min in controls to 32.5 +/- 8.7 (P = ns)， 46.1 +/- 7.0 (P < 0.05)， and 41.6 +/- 11.3 min (P < 0.05) in the respective PAI-039 treatment groups. In the vena cava protocol， PAI-039 pretreatment significantly reduced thrombus weight at PAI-039 doses of 3， 10 and 30 mg kg(-1). When PAI-039 was dosed in a treatment paradigm 4 h after stable arterial and venous thrombosis， a significant reduction in thrombus weight was observed 24 h later at PAI-039 doses of 3， 10 and 30 mg kg(-1). PAI-039 (10， 30 and 100 mg kg(-1)) had no effect on platelet aggregation in response to ADP or collagen and was not associated with increased bleeding or prolonged prothrombin time. In Animals bearing no vascular injury， PAI-039 had no effect on circulating， low-levels of PAI-1 activity. In contrast， circulating PAI-1 activity increased 5-fold following the induction of vascular injury， which was completely neutralized by PAI-039.[1]。 |
| 细胞实验 | PAI-1 expression was manipulated in a panel of cell lines and functional inhibition was achieved using the small molecule tiplaxtinin. Reduction or inhibition of PAI-1 resulted in the reduction of cellular proliferation， cell adhesion， and colony formation， and the induction of Apoptosis and anoikis in vitro. Treatment of T24 xenografts with tiplaxtinin resulted in inhibition of angiogenesis and induction of Apoptosis， leading to a significant reduction in tumor growth. Similar results were obtained through evaluation of the human cervical Cancer HeLa cell line， showing that PAI-1-mediated effects are not restricted to tumor cells of bladder origin. Collectively， these data show that targeting PAI-1 may be beneficial and support the notion that novel drugs such as tiplaxtinin could be investigated as Anticancer agents.[1]。 |
| 动物实验 | Rats[1]:Male Sprague-Dawley rats (250-350 g) are dosed orally with either vehicle or Tiplaxtinin (0.3-3 mg/kg) on the morning of the experiment， then anesthetized with sodium-pentobarbital (50 mg/kg， i.p.). A midline incision is made along the neck， and the right and left carotid arteries and jugular veins are exposed. The left jugular vein is catheterized for tPA delivery and blood sampling. The right carotid artery is cannulated with PE-60 tubing filled with 3.8% sodium citrate solution， and interfaced to a saline-filled pressure transducer for monitoring of heart rate and blood pressure. The left carotid artery is used for vascular injury induction and thrombosis. An ultrasonic flow probe is placed on the left carotid artery， and baseline blood flow is recorded. A 3-mm section of PE-60 tubing is sectioned longitudinally， and a piece of filter paper saturated with 25% FeCl3 is inserted into the tubing. Flow is monitored in the damaged vessel during tPA infusion and for an additional 20 min afterwards. At the end of the experiment， the arterial thrombus is excised and weighed.Mice[2]:Mice bearing bladder xenografts and mice bearing cervical xenografts are divided randomly into three groups (control， 5 mg/kg of Tiplaxtinin， and 20 mg/kg of Tiplaxtinin) and treatment is initiated. Each group is composed of at least 10 mice. No toxicity or weight loss is noted in any of the treatment groups. Tiplaxtinin (100 μL diluted in corn oil) is administered via oral gavage daily (Monday-Friday) for 5 weeks. Control mice received vehicle alone on the same schedule. Tumor volumes are measured weekly with digital calipers and calculated. After 5 weeks， the mice are sacrificed， tumors resected， and analyzed by immunohistochemical staining. |
| 数据来源文献 | [1]. Hennan JK， et al. Effect of Tiplaxtinin (PAI-039)， an orally bioavailable PAI-1 antagonist， in a rat model of thrombosis. J Thromb Haemost. 2008 Sep;6(9):1558-64. [2]. Gomes-Giacoia E， et al. Targeting plasminogen activator inhibitor-1 inhibits angiogenesis and tumor growth in a human cancer xenograft model. Mol Cancer Ther. 2013 Dec;12(12):2697-708. [3]. Hennan JK， et al. Evaluation of PAI-039 [{1-benzyl-5-[4-(trifluoromethoxy)phenyl]-1H-indol-3-yl}(oxo)acetic acid]， a novel plasminogen activator inhibitor-1 inhibitor， in a canine model of coronary artery thrombosis. J Pharmacol Exp Ther. 2005 Aug;314(2): |
| 单位 | 瓶 |
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IT3830 Tiplaxtinin 代谢酶/蛋白酶 索莱宝
￥520 - 5478
