PPACK, DIHYDROCHLORIDE

What are the applications of Application

PPACK dihydrochloride is an irreversible, potent, selective inhibitor of thrombin and its downstream effects.

Biological Activity

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.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) 183-190ildiko 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): 7296-7304martha 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)