Tiplaxtinin (PAI-039; CAS 393105-53-8) is an orally bioavailable small molecule inhibitor targeting plasminogen activator inhibitor-1 (PAI-1), a physiological regulator of the plasminogen activation system. Elevated PAI-1 levels stabilize thrombi by inhibiting tissue- and urokinase-type plasminogen activators. Tiplaxtinin binds selectively to PAI-1 with a Kd of approximately 480 nM and inhibits its activity with an IC50 value around 2.7 μM. In animal models, oral administration of Tiplaxtinin significantly delayed arterial thrombus-induced occlusion, supporting its utility as a research tool for studying fibrinolytic pathways and thrombotic disorders.