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PPACK TFA is a potent, peptidic inhibitor targeting thrombin and granzyme GZMK. PPACK TFA specifically blocks the activities of thrombin and GZMK, thereby inhibiting thrombin-mediated PAR-1 cleavage, as well as downstream inflammatory and procoagulant signaling pathways. Through stabilizing IκB proteins, blocking NF-κB activation and reducing systemic levels of proinflammatory/procoagulant biomarkers, PPACK TFA exerts multiple effects including anti-inflammatory, antithrombotic, barrier repair, and inhibition of atherosclerotic plaque progression. PPACK TFA binds to platelets without interference from kininogen, effectively limiting acute thrombus growth and reducing eosinophil infiltration and goblet cell hyperplasia in asthma models. PPACK TFA is an important tool molecule for investigating the mechanisms of atherosclerosis, asthma and related thromboinflammatory diseases.

PAR1

PPACK TFA nanoparticles can completely inhibit thrombin-induced PAR-1 receptor cleavage on human aortic endothelial cells and the expression of tissue factor on the surface of THP-1 monocytes.
PPACK TFA nanoparticles can inhibit thrombin-induced NF-κB activation in human aortic endothelial cells and THP-1 monocytes.
PPACK TFA (5-fold molar excess; room temperature; 1 h) can inactivate the amide hydrolytic activity of human α-thrombin after 1 h of incubation at room temperature, generating PPACK TFA-thrombin that does not interfere with the enzymatic function of unmodified α-thrombin.
PPACK TFA (200 μM, 100 μM, 10 μM) exhibits anticoagulant effects and demonstrates stronger anticoagulant activity per molar concentration than the factor Xa inhibitor GGACK at the same concentration when used alone.

PPACK TFA nanoparticles (intravenous injection; 3 times per week; for 4 weeks) administered via intravenous injection to high-fat-fed ApoE knockout mice reduced vascular procoagulant activity, restored endothelial barrier integrity, delayed plaque progression, and attenuated inflammatory signaling in atherosclerotic plaques without inducing systemic anticoagulation or altering serum cholesterol levels .
PPACK (62.5 μg; i.p.; once every 2 days; administered within 8-18 days after immunization) significantly alleviated airway eosinophilia, goblet cell hyperplasia, and airway hyperresponsiveness in a mouse model of asthma.

Room temperature in continental US; may vary elsewhere.

2-8°C,Sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (Sealed storage, away from moisture)