PPACK Dihydrochloride
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
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
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
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)
| Storage | Store at -20°C |
| M.Wt | 523.88 |
| Cas No. | 142036-63-3 |
| Formula | C21H31ClN6O3·2HCl |
| Synonyms | PPACK Dihydrochloride |
| Solubility | ≥49.5 mg/mL in DMSO; ≥32.5 mg/mL in EtOH; ≥37.9 mg/mL in H2O |
| Chemical Name | N-(2-amino-3-phenylpropanoyl)-1-[1-chloro-6-(diaminomethylideneamino)-2-oxohexan-3-yl]pyrrolidine-2-carboxamide |
| SDF | Download SDF |
| Canonical SMILES | C1CC(N(C1)C(CCCN=C(N)N)C(=O)CCl)C(=O)NC(=O)C(CC2=CC=CC=C2)N |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
| Description | PPACK Dihydrochloride is a potent, selective and irreversible inhibitor of thrombin with a Ki value of 0.24 nM. | |||||
| Targets | thrombin | |||||
| IC50 | 0.24 nM (Ki) | |||||
Quality Control & MSDS
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Chemical structure
