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Tiplaxtinin(PAI-039)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Tiplaxtinin(PAI-039)图片
CAS NO:393105-53-8
规格:98%
分子量:439.38
包装与价格:
包装价格(元)
5mg电议
10mg电议
50mg电议

产品介绍
Orally efficacious inhibitor of PAI-1
CAS:393105-53-8
分子式:C24H16F3NO4
分子量:439.38
纯度:98%
存储:Store at -20°C

Background:

Description:


IC50: 2.7 μM


Plasminogen activator inhibitor-1 (PAI-1) is the most important physiologic regulator of the plasminogen activation system through its inhibition of its target serine proteases, tissue plasminogen activator, and urokinase plasminogen activator. Significant elevations of PAI-1 lead to stabilization of arterial and venous thrombi, which contribute respectively to coronary arterial occlusion in postmyocardial infarction and venous thrombosis following postoperative recovery from orthopedic surgery. Tiplaxtinin (PAI-039) is a novel, orally efficacious inhibitor of PAI-1.


In vitro: Tiplaxtinin inhibited PAI-1 as determined by the antibody method. By use of fluorescent spectroscopy, tiplaxtinin bound to the PAI-1 mutant selectively with a Kd of 480 nM. This binding event was saturable and associated with inhibition of the protein [1].


In vivo: In the rat model of carotid thrombosis, oral administration of tiplaxtinin at 1 mg/kg increased time to occlusion and prevented the carotid blood flow reduction when compared to the vehicle group. All of the vehicle control rats exhibited thrombosis with an average time to occlusion of 11 min and a complete reduction of 100% carotid flow. Conversely, those rats receiving tiplaxtinin at 1 mg/kg po exhibited an average time to occlusion of >50 min and a carotid blood flow reduction of approximately 50% [1].


Clinical trial: Up to now, tiplaxtinin is still in the preclinical development stage.


Reference:
[1] Elokdah H, Abou-Gharbia M, Hennan JK, McFarlane G, Mugford CP, Krishnamurthy G, Crandall DL.  Tiplaxtinin, a novel, orally efficacious inhibitor of plasminogen activator inhibitor-1: design, synthesis, and preclinical characterization. J Med Chem. 2004 Jul 1;47(14):3491-4.
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