Thrombin inhibitor
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 constant Kivalue 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
[1].Jun T. Liu, William Paul, Michael Emerson, Carla Cicala and Clive P. Page. Thrombin inhibitors and anti-coagulants on thrombin-induced embolization in rabbit cranial vasculature. European Journal of Pharmacology 264 (1994) 183-190
[2].Ildiko M. Kovach, Paul Kelley, Carol Eddy, Frank Jordan and Ahmet Baykal. Proton bridging in the interactions of thrombin with small inhibitors. Biochemistry. 2009; 48(30): 7296-7304
[3].Martha E. Lyon, James S. Fine, Paul J. Henderson and Andrew W. Lyon. D-Phenylalanyl-L-prolyl-L-arginine chloromethyl ketone (PPACK): alternative anticoagulant to heparin salts for blood gas and electrolyte specimens. CLIN. CHEM. 41/7, 1038-1041 (1995)
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