PPACK Dihydrochloride is the dihydrochloride form of its active component PPACK (_D-Phenylalanyl-_L-prolyl-_L-arginine chloromethyl ketone), a potent, selective and irreversible inhibitor of thrombin that inhibits human α-thrombin with inhibition constantK_ivalue of 0.24 nM. PPACK covalently binds to the specific active-site Ser of thrombin and cross links with His57 at the binding site forming a tetrahedral PPACK-thrombin complex. The complex further binds to and saturates the high-affinity functional thrombin receptors eventually leading to the inhibition of thrombin activation. PPACK is currently being investigated as an anti-coagulant to prevent blood coagulation. Study results show that PPACK is able to dose-dependently inhibit thrombin-induced platelet accumulation.

Reference

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