Table 2.
Modifications to the INF7 portion of the chimeric peptide.
| Number | Sequence | RBC Lysis IC50, pH 5.5 (μM) | RBC Lysis IC50, pH 7.4 (μM) |
|---|---|---|---|
| 12a | CRLFEAIEGFIENGWEGMIDGWYGYGRKKRRQRR | 0.8 | 3.5 |
| 12b | CELFEAIEGFIENGWEGMIDGWYGYGRKKRRQRR | 1.5 | >20 |
| 12c | CGGGLFEAIEGFIENGWEGMIDGWYGYGRKKRRQRR | 1 | 0.9 |
| 12d | C(Nle)LFEAIEGFIENGWEGMIDGWYGYGRKKRRQRR | 0.8 | 2.4 |
| 12e | CVLFEAIEGFIENGWEGMIDGWYGYGRKKRRQRR | 0.72 | >20 |
| 12f | C(b-Ala)LFEAIEGFIENGWEGMIDGWYGYGRKKRRQRR | 0.38 ± 0.17 (n = 5) | >20 (n = 5) |
| 12g | CSLFEAIEGFIENGWEGMIDGWYGYGRKKRRQRR | 0.66 | >20 |
| 13a | CGFFEAIEGFIENGWEGMIDGWYGYGRKKRRQRR | 0.35 | 1.16 |
| 13b | CGKFEAIEGFIENGWEGMIDGWYGYGRKKRRQRR | >20 | >20 |
| 13c | CGEFEAIEGFIENGWEGMIDGWYGYGRKKRRQRR | >20 | >20 |
| 13d | CGGFEAIEGFIENGWEGMIDGWYGYGRKKRRQRR | >10 | >10 |
| 13e | CGNFEAIEGFIENGWEGMIDGWYGYGRKKRRQRR | >10 | >10 |
| 14a | CGLNEAIEGFIENGWEGMIDGWYGYGRKKRRQRR | >100 | >100 |
| 14b | CGLGEAIEGFIENGWEGMIDGWYGYGRKKRRQRR | >20 | >20 |
| 14c | CGLKEAIEGFIENGWEGMIDGWYGYGRKKRRQRR | >10 | >10 |
| 14d | CGLEEAIEGFIENGWEGMIDGWYGYGRKKRRQRR | 2.5 | >10 |
| 14e | CGLAEAIEGFIENGWEGMIDGWYGYGRKKRRQRR | 1.3 (max. 65%) | >10 |
| 14f | CGLLEAIEGFIENGWEGMIDGWYGYGRKKRRQRR | 0.93 | 3.67 |
| 15a | CGLFGAIEGFIENGWEGMIDGWYGYGRKKRRQRR | 0.4 | 1 |
| 15b | CGLFAAIEGFIENGWEGMIDGWYGYGRKKRRQRR | 1.26 | 0.75 |
| 15c | CGLFNAIEGFIENGWEGMIDGWYGYGRKKRRQRR | 1.12 | 1.78 |
| 15d | CGLFLAIEGFIENGWEGMIDGWYGYGRKKRRQRR | >10 | >10 |
| 15e | CGLFKAIEGFIENGWEGMIDGWYGYGRKKRRQRR | 0.71 | 1.27 |
| 16a | CGLFENIEGFIENGWEGMIDGWYGYGRKKRRQRR | >10 | >10 |
| 16b | CGLFELIEGFIENGWEGMIDGWYGYGRKKRRQRR | 0.23 | 1.93 |
| 16c | CGLFEEIEGFIENGWEGMIDGWYGYGRKKRRQRR | 0.26 | >10 |
| 16d | CGLFEKIEGFIENGWEGMIDGWYGYGRKKRRQRR | 0.04 | 1.11 |
| 17a | CGLFEAKEGFIENGWEGMIDGWYGYGRKKRRQRR | >10 | >10 |
| 17b | CGLFEAEEGFIENGWEGMIDGWYGYGRKKRRQRR | 4.74 | >10 |
| 17c | CGLFEALEGFIENGWEGMIDGWYGYGRKKRRQRR | 0.8 | 5 |
| 18a | CGLFEAIWGFIENGWEGMIDGWYGYGRKKRRQRR | 0.9 | 1.2 |
| 18b | CGLFEAIKGFIENGWEGMIDGWYGYGRKKRRQRR | 2.2 | 6.5 |
| 18c | CGLFEAIHGFIENGWEGMIDGWYGYGRKKRRQRR | 7.7 | >80 |
| 18d | CGLFEAIRGFIENGWEGMIDGWYGYGRKKRRQRR | 1.2 | 2.8 |
| 18e | CGLFEAIDGFIENGWEGMIDGWYGYGRKKRRQRR | 3.7 | >100 |
| 18f | CGLFEAIGGFIENGWEGMIDGWYGYGRKKRRQRR | 2.1 | 2.1 |
| 19a | CGLFEAIENFIENGWEGMIDGWYGYGRKKRRQRR | 2.7 | 3.09 |
| 19b | CGLFEAIEKFIENGWEGMIDGWYGYGRKKRRQRR | 2.32 | >10 |
| 19c | CGLFEAIEEFIENGWEGMIDGWYGYGRKKRRQRR | 0.41 | >10 |
| 19d | CGLFEAIEGGIENGWEGMIDGWYGYGRKKRRQRR | 2.52 | >10 |
| 20a | CGLFEAIEGAIENGWEGMIDGWYGYGRKKRRQRR | 0.88 | 4.71 |
| 20b | CGLFEAIEGLIENGWEGMIDGWYGYGRKKRRQRR | 0.24 | 1.97 |
| 20c | CGLFEAIEGGIENGWEGMIDGWYGYGRKKRRQRR | 2.52 | >10 |
| 20d | CGLFEAIEGAIENGWEGMIDGWYGYGRKKRRQRR | 0.88 | 4.71 |
| 20e | CGLFEAIEGLIENGWEGMIDGWYGYGRKKRRQRR | 0.24 | 1.97 |
| 21a | CGLFEAIEGFGENGWEGMIDGWYGYGRKKRRQRR | >10 | >10 |
| 21b | CGLFEAIEGFAENGWEGMIDGWYGYGRKKRRQRR | 1.59 | >10 |
| 21c | CGLFEAIEGFLENGWEGMIDGWYGYGRKKRRQRR | 0.59 | 2.8 |
| 21d | CGLFEAIEGFWENGWEGMIDGWYGYGRKKRRQRR | 0.35 | >10 |
| 21e | CGLFEAIEGFKENGWEGMIDGWYGYGRKKRRQRR | >10 | >10 |
| 21f | CGLFEAIEGFNENGWEGMIDGWYGYGRKKRRQRR | >100 | >100 |
| 22a | CGLFEAIEGFILNGWEGMIDGWYGYGRKKRRQRR | 1.06 | 1.1 |
| 22b | CGLFEAIEGFIWNGWEGMIDGWYGYGRKKRRQRR | 0.44 | 0.95 |
| 22c | CGLFEAIEGFIKNGWEGMIDGWYGYGRKKRRQRR | 4.27 | >10 |
| 22d | CGLFEAIEGFIGNGWEGMIDGWYGYGRKKRRQRR | 6.16 | >10 |
| 23a | CGLFEAIEGFIEPGWEGMIDGWYGYGRKKRRQRR | >10 | >10 |
| 23b | CGLFEAIEGFIEPGWEGMIDGWYGYGRKKRRQRR | >10 | >10 |
| 23c | CGLFEAIEGFIEGGWEGMIDGWYGYGRKKRRQRR | 1.11 | 6.55 |
| 23d | CGLFEAIEGFIELGWEGMIDGWYGYGRKKRRQRR | 1.34 | 1.31 |
| 23e | CGLFEAIEGFIEWGWEGMIDGWYGYGRKKRRQRR | 0.54 | 5.18 |
| 23f | CGLFEAIEGFIEKGWEGMIDGWYGYGRKKRRQRR | 1.52 | >10 |
| 24a | CGLFEAIEGFIENEWEGMIDGWYGYGRKKRRQRR | max. 45% @ 2.0 uM | >100 |
| 24b | CGLFEAIEGFIENKWEGMIDGWYGYGRKKRRQRR | >10 | >10 |
| 24c | CGLFEAIEGFIENNWEGMIDGWYGYGRKKRRQRR | 6.39 | >10 |
| 24d | CGLFEAIEGFIENHWEGMIDGWYGYGRKKRRQRR | 3.06 | 2.9 |
| 24e | CGLFEAIEGFIENPWEGMIDGWYGYGRKKRRQRR | 1.71 | 4.72 |
| 24f | CGLFEAIEGFIENAWEGMIDGWYGYGRKKRRQRR | 1.88 | 1.28 |
| 24g | CGLFEAIEGFIENWWEGMIDGWYGYGRKKRRQRR | 1.1 | >10 |
| 25a | CGLFEAIEGFIENGEEGMIDGWYGYGRKKRRQRR | 1.55 | 0.31 |
| 24b | CGLFEAIEGFIENGKEGMIDGWYGYGRKKRRQRR | >10 | >10 |
| 25c | CGLFEAIEGFIENGLEGMIDGWYGYGRKKRRQRR | 0.66 | 4.43 |
| 26a | CGLFEAIEGFIENGWDGMIDGWYGYGRKKRRQRR | 0.55 | 1.3 |
| 26b | CGLFEAIEGFIENGWRGMIDGWYGYGRKKRRQRR | 0.19 | 3.3 |
| 26c | CGLFEAIEGFIENGWKGMIDGWYGYGRKKRRQRR | 0.34 | >10 |
| 26d | CGLFEAIEGFIENGWHGMIDGWYGYGRKKRRQRR | 2.54 | >10 |
| 26e | CGLFEAIEGFIENGWNGMIDGWYGYGRKKRRQRR | 1.47 | >10 |
| 26f | CGLFEAIEGFIENGWLGMIDGWYGYGRKKRRQRR | 0.84 | 2.03 |
| 26g | CGLFEAIEGFIENGWAGMIDGWYGYGRKKRRQRR | 1.3 | >10 |
| 26h | CGLFEAIEGFIENGWGGMIDGWYGYGRKKRRQRR | 3.1 | >10 |
| 27a | CGLFEAIEGFIENGWEAMIDGWYGYGRKKRRQRR | 0.12(max. 65%) | 0.95 |
| 27b | CGLFEAIEGFIENGWENMIDGWYGYGRKKRRQRR | 0.42 | >10 |
| 27c | CGLFEAIEGFIENGWEKMIDGWYGYGRKKRRQRR | 1.01 | 8.99 |
| 27d | CGLFEAIEGFIENGWEEMIDGWYGYGRKKRRQRR | 3.76 | >10 |
| 28a | CGLFEAIEGFIENGWEG(M sulfoxide)IDGWYGYGRKKRRQRR | >100 | >100 |
| 28b | CGLFEAIEGFIENGWEG(M sulfone)IDGWYGYGRKKRRQRR | >100 | >100 |
| 28c | CGLFEAIEGFIENGWEGNIDGWYGYGRKKRRQRR | >10 | >10 |
| 28d | CGLFEAIEGFIENGWEGQIDGWYGYGRKKRRQRR | >10 | >10 |
| 28e | CGLFEAIEGFIENGWEGTIDGWYGYGRKKRRQRR | >10 | >10 |
| 28f | CGLFEAIEGFIENGWEGSIDGWYGYGRKKRRQRR | >10 | >10 |
| 28g | CGLFEAIEGFIENGWEGLIDGWYGYGRKKRRQRR | 0.71 | 2.9 |
| 28h | CGLFEAIEGFIENGWEG(Nle)IDGWYGYGRKKRRQRR | 0.53 | 3.94 |
| 28i | CGLFEAIEGFIENGWEGYIDGWYGYGRKKRRQRR | 2.56 | >10 |
| 28j | CGLFEAIEGFIENGWEGFIDGWYGYGRKKRRQRR | 0.52 | 9.65 |
| 28k | CGLFEAIEGFIENGWEGIDGWYGYGRKKRRQRR (delete) | 50 | >100 |
| 29a | CGLFEAIEGFIENGWEGMLDGWYGYGRKKRRQRR | 10.2 | >10 |
| 29b | CGLFEAIEGFIENGWEGMADGWYGYGRKKRRQRR | >10 | >10 |
| 29c | CGLFEAIEGFIENGWEGMGDGWYGYGRKKRRQRR | 2.53 | >10 |
| 29d | CGLFEAIEGFIENGWEGMNDGWYGYGRKKRRQRR | 1.04 | >10 |
| 29e | CGLFEAIEGFIENGWEGMKDGWYGYGRKKRRQRR | 1.17 | 9.1 |
| 29f | CGLFEAIEGFIENGWEGMEDGWYGYGRKKRRQRR | >10 | >10 |
| 30a | CGLFEAIEGFIENGWEGMIEGWYGYGRKKRRQRR | 4.4 | >10 |
| 30b | CGLFEAIEGFIENGWEGMIAGWYGYGRKKRRQRR | >10 | 2.83 |
| 30c | CGLFEAIEGFIENGWEGMIWGWYGYGRKKRRQRR | >10 | >10 |
| 30d | CGLFEAIEGFIENGWEGMILGWYGYGRKKRRQRR | >10 | >10 |
| 31a | CGLFEAIEGFIENGWEGMIDAWYGYGRKKRRQRR | 1.4 | >10 |
| 31b | CGLFEAIEGFIENGWEGMIDLWYGYGRKKRRQRR | 0.32 | 0.96 |
| 31c | CGLFEAIEGFIENGWEGMIDIWYGYGRKKRRQRR | 1.68 | >10 |
| 31d | CGLFEAIEGFIENGWEGMIDWWYGYGRKKRRQRR | 0.55 ± 0.25 (n = 8) | 7.14 ± 0.73 (n = 8) |
| 31e | CGLFEAIEGFIENGWEGMIDNWYGYGRKKRRQRR | 6.07 | 7.26 |
| 31f | CGLFEAIEGFIENGWEGMIDKWYGYGRKKRRQRR | 2.86 | >10 |
| 31g | CGLFEAIEGFIENGWEGMIDEWYGYGRKKRRQRR | 1.5 | >10 |
| 32a | CGLFEAIEGFIENGWEGMIDGYGRKKRRQRR | >10 | >10 |
| 32b | CGLFEAIEGFIENGWEGMIDGGGGYGRKKRRQRR | >10 | >10 |
| 33a | CGLFEAIEGFIENGWEGMIDGLYGYGRKKRRQRR | 4.24 | 1.75 |
| 33b | CGLFEAIEGFIENGWEGMIDGAYGYGRKKRRQRR | 4.07 | >10 |
| 33c | CGLFEAIEGFIENGWEGMIDGGYGYGRKKRRQRR | >10 | >10 |
| 33d | CGLFEAIEGFIENGWEGMIDGNYGYGRKKRRQRR | 2.5 | >10 |
| 33e | CGLFEAIEGFIENGWEGMIDGKYGYGRKKRRQRR | 6.6 | >10 |
| 33f | CGLFEAIEGFIENGWEGMIDGEYGYGRKKRRQRR | 4.26 | >10 |
| 34a | CGLFEAIEGFIENGWEGMIDGWAGYGRKKRRQRR | >10 | >10 |
| 34b | CGLFEAIEGFIENGWEGMIDGWHGYGRKKRRQRR | 5.04 | >10 |
| 34c | CGLFEAIEGFIENGWEGMIDGWNGYGRKKRRQRR | 0.13 | 1.72 |
| 34d | CGLFEAIEGFIENGWEGMIDGWEGYGRKKRRQRR | 3.94 | >10 |
| 35a | CGLFEAIEGFIENGWEGMIDGWYAYGRKKRRQRR | 2 | >10 |
| 35b | CGLFEAIEGFIENGWEGMIDGWYWYGRKKRRQRR | 0.17 (max. 70%) | 3.05 |
| 35c | CGLFEAIEGFIENGWEGMIDGWYEYGRKKRRQRR | 1.04 (max. 60%) | >10 |
All peptides were >95% purity by HPLC analysis and demonstrated the correct HRMS profiles. Peptides were tested three times at each pH unless otherwise noted, and the values are reported as the mean. Standard Deviations are reported for peptides with larger n values to provide a reference for the reproducibility of the data. As solubility allowed, testing at pH 7.4 was pushed to the highest possible concentrations to determine as close as possible approximate IC50.