Inhibition constants (IC50 values), relative inhibitory potencies (RIP), RIP per glycan and inhibitory potencies (IP) for Lac and glycomacromolecules 4–15.
| Glyco-conjugate | No. of carbohydrate | IC50 ± SDa [μM] | RIPb | RIP/Lac | IPc [%] |
|---|---|---|---|---|---|
| Lactose | 1 | 159 ± 13 | 1.0 | 1.0 | — |
| Lac(1)-2, 4 | 1 | 123 ± 3 | 1.3 | 1.3 | 31 |
| Lac(2)-3, 5 | 1 | 111 ± 4 | 1.4 | 1.4 | 46 |
| Lac(1,5)-5, 6 | 2 | 55 ± 5 | 2.9 | 1.5 | 61 |
| Lac(1,5,9)-9, 7 | 3 | 36 ± 3 | 4.4 | 1.5 | 66 |
| Lac(1,4,7)-8, 8 | 3 | 42 ± 3 | 3.8 | 1.3 | 65 |
| Lac(1,3,5)-6, 9 | 3 | 38 ± 2 | 4.2 | 1.4 | 68 |
| Lac(1,2,3)-4, 10 | 3 | 37 ± 1 | 4.3 | 1.4 | 72 |
| Lac3-TPD, 11 | 3 | 29 ± 1 | 5.5 | 1.8 | 77 |
| Lac(1,2,3,4,5,6)-7, 12 | 6 | 16 ± 4 | 9.8 | 1.6 | 78 |
| Lac(2)-3 L, 13 | 1 | 133 ± 8 | 1.2 (0.8*) | 1.2 | 36 |
| Lac(1,5)-5 L, 14 | 2 | 87 ± 3 | 1.8 (0.6*) | 0.9 | 50 |
| Lac(1,5,9)-9 L, 15 | 3 | 50 ± 2 | 3.2 (0.7*) | 1.1 | 55 |
a
Determined by ELISA-inspired inhibition studies on ASF coated plates. Measurements were performed two times in triplicates.
b
Relative inhibitory potency normalized to IC50 value of Lac (159 μM).
c
Reduced IC50 experiment determined by SPR inhibition studies with 100 μg mL−1 Gal-3 in PBS and 50 μM ligand. Binding signal of blank Gal-3 was set to 100% binding and 0% inhibition, inhibition values reported are referred to Gal-3. *RIP in brackets are the result of a direct comparison of the IC50 value of compound 5 to 13, 6 to 14 and 7 to 15.