Additional Information s4

ADDITIONAL INFORMATION

The data for APTT in the tables for peptides with Val115 refer to values above Ref.t. 29.7 sec. Table 1. Data for anticoagulant activity of the compound H-Arg-Pro-Lys-

Arg-Lys-Leu-Val-Pro-NH2 Concentration (mol.10-9) APTT (sec) 200,50 10,0 260,70 29,9 300,80 45,0

Table 2. Data for anticoagulant activity of the compound H-Lys-Pro-Lys-

Arg-Lys-Leu-Val-Pro-NH2

Concentration (mol.10-9) APTT (sec) 211,00 8,9 646,61 28,9 1077,70 57,9

Table 3. Data for anticoagulant activity of the compound H-Orn-Pro-Lys-

Arg-Lys-Leu-Val-Pro-NH2

Table 4. Data for anticoagulant activity of the compound H-Pro-Lys-Arg-

Lys-Leu-Val-Pro-NH2 Concentration (mol.10-9) APTT (sec) 906,80 8,8 1813,59 18,6 2266,99 18,8 2720,39 25,5 2901,75 29,8 2992,43 32,4

Table 5. Data for anticoagulant activity of the compound H-Arg-Pro-Lys- Arg-Lys-Leu-Val-Pro-OH

Concentration (mol.10-9) APTT (sec) 41,89 NA 272,29 3,8 418,91 5,5 523,64 15,6 802,24 62,4 NA-no activity Table 6. Data for anticoagulant activity of the compound H-Lys-Pro-Lys- Arg-Lys-Leu-Val-Pro-OH

Concentration (mol.10-9) APTT (sec) 290,00 6,7 894,00 21,6 1043,42 24,1 1117,95 30,0 1192,00 50,9 2235,90 122,8

Table 7. Data for anticoagulant activity of the compound H-Orn-Pro-Lys- Arg-Lys-Leu-Val-Pro-OH Concentration (mol.10-9) APTT (sec) 771,00 22,2 1156,56 28,5

Table 8. Data for anticoagulant activity of the compound H-Pro-Lys-Arg- Lys-Leu-Val-Pro-OH

The data for APTT in the tables for peptides with Ile115 refer to values above Ref.t. 28.8 sec. Table 9. Anticoagulant activity of the compound H-Arg-Pro-Lys-Arg-Lys-

Leu-Ile-Pro-OH

Concentration (mol.10-9) APTT (sec.) 19,88 NA 835,00 NA 1252,49 NA 1550,70 NA 1600,00 28,9±0,4

Table 10. Anticoagulant activity of the compound H-Lys-Pro-Lys-Arg-

Lys-Leu-Ile-Pro-OH

Concentration (mol.10-9) APTT (sec.) 73,24 3,1±0,1 476,06 8,8±0,1 1025,36 16,6±0,4 1464,8 29,5±0,3

Table 11. Anticoagulant activity of the compound H-Orn-Pro-Lys-Arg-

Lys-Leu-Ile-Pro-OH

Concentration (mol.10-9) APTT (sec.) 790,90 14,8±0,4 1224,30 28,5±0,4 2902,61 Out of range

Table 12. Anticoagulant activity of the compound H-Pro-Lys-Arg-Lys-

Leu-Ile-Pro-OH

Concentration (mol.10-9) APTT (sec.) 1134,52 24,0±0,4 3857,40 29,1±0,2 6807,12 Out of range

Table 13. Anticoagulant activity of the compound H-Arg-Pro-Lys-Arg-

Lys-Leu-Ile-Pro-NH2

Concentration (mol.10-9) APTT (sec.) 2535,60 27,9±0,3 3480,19 30,6±0,5

Table 14. Anticoagulant activity of the compound H-Lys-Pro-Lys-Arg-

Lys-Leu-Ile-Pro-NH2

Concentration (mol.10-9) APTT (sec.) 413,33 19,1±0,4 448,57 27,9±0,2 516,67 54,0±0,2

Table 15. Anticoagulant activity of the compound H-Orn-Pro-Lys-Arg-

Lys-Leu-Ile-Pro-NH2

Concentration (mol.10-9) APTT (sec.) 3748,3 28,8±0,5 4150.40 33.2±0,5 4669.2 35.7±0,5

Table 16. Anticoagulant activity of the compound H-Pro-Lys-Arg-Lys-

Leu-Ile-Pro-NH2

Concentration (mol.10-9) APTT (sec.) 4708.00 20.8±0,2 5002.30 29.2±0,2 7062.00 Out of range

Table 17. ESI-MS data for newly synthesized compounds Compound MS data Mass exact [M+H] found calculated Arg-Pro-Lys-Arg-Lys-Leu-Val-Pro-OH 992,6607 993,84

Arg-Pro-Lys-Arg-Lys-Leu-Val-Pro-NH2 991,6767 992,80 Lys-Pro-Lys-Arg-Lys-Leu-Val-Pro-OH 964,6546 965,44

Lys-Pro-Lys-Arg-Lys-Leu-Val-Pro-NH2 963,6706 964,68 Orn-Pro-Lys-Arg-Lys-Leu-Val-Pro-OH 950,6389 951,80

Orn-Pro-Lys-Arg-Lys-Leu-Val-Pro-NH2 949,6549 950,80 Pro-Lys-Arg-Lys-Leu-Val-Pro-OH 836,5596 837,66

Pro-Lys-Arg-Lys-Leu-Val-Pro-NH2 835,5756 836,60 Arg-Pro-Lys-Arg-Lys-Leu-Ile-Pro-OH 1006,6764 1007,40 Arg-Pro-Lys-Arg-Lys-Leu-Ile-Pro-NH2 1005,6924 1006,44 Lys-Pro-Lys-Arg-Lys-Leu-Ile-Pro-OH 978,6702 979,40

Lys-Pro-Lys-Arg-Lys-Leu-Ile-Pro-NH2 977,6862 978,40 Orn-Pro-Lys-Arg-Lys-Leu-Ile-Pro-OH 964,6546 965,37

Orn-Pro-Lys-Arg-Lys-Leu-Ile-Pro-NH2 963,6706 964,40 Pro-Lys-Arg-Lys-Leu-Ile-Pro-OH 850,5753 851,30

Pro-Lys-Arg-Lys-Leu-Ile-Pro-NH2 849,5912 850,31