PPACK (TFA)

PPACK TFA is a potent and selective irreversible thrombin inhibitor. PPACK TFA serves as an alternative anticoagulant to lithium heparin (LiHep) for blood gas and whole blood electrolyte analyses. PPACK TFA also acts as an inhibitor of plasminogen activator (rt-PA). PPACK TFA inhibits the binding of rt-PA to plasma protease inhibitors. PPACK TFA attenuates the plasmin-induced increase in endothelial permeability and endothelial morphological changes in bovine aortic endothelial cell monolayers, and can be used in thrombosis-related research^[1][2][3]. In Vitro:PPACK (TFA) potently inhibits thrombin with a K_i value of 3.7 × 10^-8 M^[2].
PPACK (TFA) (0.2 mM; 2 h coincubation, 12 h measurement) reduces plasmin-induced permeability increases in confluent bovine aortic endothelial cell monolayers by 59% at 12 hours after initial plasmin exposure, and fully inhibits plasmin activity^[3].
PPACK (TFA) (0.2 mM; 4 h post plasmin treatment) attenuates plasmin-induced morphological damage to confluent bovine aortic endothelial cell monolayers, including reducing intercellular gaps and preserving F-actin stress fiber structure, when assessed 4 hours after initial plasmin treatment^[3]. In Vivo:PPACK (TFA) (0.05-0.5 mg/kg; i.v.; single bolus injection) exerts a significant, dose-dependent antithrombotic effect in He-Ne laser-induced rat mesenteric microthrombosis, with a minimal effective dose of 0.1 mg/kg for both arterioles and venules and maximal activity immediately after a single intravenous bolus injection that persists for 60 minutes^[2].