Description: Tiplaxtinin sodium (PAI-039) is an orally bioactive and selective plasminogen activator inhibitor-1 (PAI-1) inhibitor with IC50 of 2.7 μM. 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. In a rat carotid thrombosis model, Tiplaxtinin (1 mg/kg, p.o.) increases time to occlusion and prevents the carotid blood flow reduction. In C57BL/6J mice, (1 mg/g chow) attenuates Ang II-induced aortic remodeling.

References: J Med Chem. 2004 Jul 1;47(14):3491-4; Arterioscler Thromb Vasc Biol. 2005 Feb;25(2):365-71; Mol Cancer Ther. 2013 Dec;12(12):2697-708.

纯度：≥98%