PPACK is a synthetic peptide derivative that irreversibly and specifically inhibits thrombin-mediated platelet activation by binding with high affinity to the active site of thrombin (Ki = 0.24 nM).
CAS：71142-71-7
分子式：C21H31ClN6O3
分子量：451
纯度：98%
存储：Store at -20°C

Background:

PPACK is a synthetic peptide derivative that irreversibly and specifically inhibits thrombin-mediated platelet activation by binding with high affinity to the active site of thrombin (Ki = 0.24 nM).[1][2][3] It has been used as an anticoagulant (100 μM) and to study thrombin-mediated fibrin deposition, angiogenesis, and proinflammatory processes.[4][5]

Reference:
[1]. Kovach, I.M., Kelley, P., Eddy, C., et al. Proton bridging in the interactions of thrombin with small inhibitors. Biochemistry 48(30), 7296-7304 (2009).
[2]. Bode, W., Turk, D., and Karshikov, A. The refined 1.9-? x-ray crystal structure of D-Phe-Pro-Arg chloromethylketone-inhibited human α-thrombin: Structure analysis, overall structure, electrostatic properties, detailed active-site geometry, and structure-function relationships. Protein Science 1(4), 426-471 (1992).
[3]. Hanson, S.R., and Harker, L.A. Interruption of acute platelet-dependent thrombosis by the synthetic antithrombin D-phenylalanyl-L-prolyl-L-arginyl chloromethyl ketone. Proceedings of the National Academy of Sciences of the United States of America 85(9), 3184-3488 (1988).
[4]. Lyon, M.E., Fine, J.S., Henderson, P.J., et al. D-phenylalanyl-L-prolyl-L-arginine chloromethyl ketone (PPACK): Alternative anticoagulant to heparin salts for blood gas and electrolyte specimens. Clinical Chemistry 41(7), 1038-1041 (1995).
[5]. Liu, J.F., Hou, S.M., Tsai, C.H., et al. Thrombin induces heme oxygenase-1 expression in human synovial fibroblasts through protease-activated receptor signaling pathways. Arthritis Research & Therapy 14(2), R91 (2012).