Diaplasinin (PAI-749) is a plasminogen activator inhibitor-1 (PAI-1) inhibitor with IC50 of 295 nm. Antithrombotic efficacy[1].
PAI-749 is a potent and selective synthetic antagonist of plasminogen activator inhibitor 1 (PAI-1) that preserved tissue-type plasminogen activator (tPA) and urokinase-type plasminogen activator (uPA) activities in the presence of PAI-1 (IC50 values, 157 and 87 nM, respectively)[2].
PAI-749 quenches the fluorescence (Fl) of fluorophore-tagged PAI-1 (PAI-NBD119) with the apparent Kd of 254 nM) and the IC50 of 140 nM[2].
[1]. A J Lucking, et al. Effect of the small molecule plasminogen activator inhibitor-1 (PAI-1) inhibitor, PAI-749, in clinical models of fibrinolysis. J Thromb Haemost. 2010 Jun;8(6):1333-9.
[2]. Stephen J Gardell, et al. Neutralization of plasminogen activator inhibitor I (PAI-1) by the synthetic antagonist PAI-749 via a dual mechanism of action. Mol Pharmacol. 2007 Oct;72(4):897-906.