IC50-values of glycoclusters (given in mM based on GalNAc) and the cognate monosaccharide in lectin histochemical assays with biotinylated lectins applied to sections of fixed murine jejunum.
| Compound/cell type | DBA | SBA | HPA | MGL | |
|---|---|---|---|---|---|
| CRD | CRD + stalk | ||||
| 1 | |||||
| Surface enterocytes | n.i.a | 10.0 (0.05)b | >10.0 (<0.5) | >20.0 (<1.25) | >20.0 (<1.25) |
| Crypt-associated cells | n.i.a | 20.0 (0.1) | >20.0 (<0.25) | >20.0 (<2.5) | >20.0 (<2.5) |
| 2 | |||||
| Surface enterocytes | 1.0 (25) | 0.02/0.01 (50/100) | 5.0 (1.0) | 1.0 (25) | 1.0 (25) |
| Crypt-associated cells | 2.0 (25) | 0.01 (200) | 5.0 (1.0) | 1.0 (50) | 2.0 (25) |
| 3 | |||||
| Surface enterocytes | 2.0 (12.5) | 0.005/0.002 (200/500) | 0.1/0.05 (50/100) | 0.05 (500) | 0.1 (250) |
| Crypt-associated cells | 5.0 (10) | 0.005/0.002 (200/500) | 0.5/0.2 (10/25) | 0.05 (1000) | 0.1 (500) |
| 4 | |||||
| Surface enterocytes | 1.0 (25) | 0.005 (200) | 1.0 (5.0) | 0.05/0.02 (500/1250) | 0.1/0.05 (250/500) |
| Crypt-associated cells | 5.0 (5) | 0.01 (200) | 5.0 (1.0) | 0.05/0.02 (1000/2500) | 0.1/0.05 (500/1000) |
| 5 | |||||
| Surface enterocytes | 2.0 (12.5) | 0.001/0.0005 (1000/2000) | 0.05/0.02 (100/250) | 0.01/0.005 (2500/5000) | 0.005 (5000) |
| Crypt-associated cells | 5.0 (10) | 0.001 (2000) | 0.02 (250) | 0.01/0.005 (5000/10 000) | 0.005/0.002 (10 000/25 000) |
| 6 | |||||
| Surface enterocytes | 20 (1.4) | 0.1 (10) | 0.1 (50) | 0.2 (125) | 0.1 (250) |
| Crypt-associated cells | >20 (<2.5) | 0.2 (10) | 0.2 (25) | 0.2 (250) | 0.2/0.1 (250/500) |
| 7 | |||||
| Surface enterocytes | 20 (1.25) | 0.02 (50) | 0.5 (10.0) | 5.0 (5) | 10.0 (2.5) |
| Crypt-associated cells | >20 (<2.5) | 0.05 (40) | 2.0 (2.5) | 1.0 (50) | 2.0 (25) |
| d-GalNAc | |||||
| Surface enterocytes | 25.0 | 1.0 | 5.0 | 25.0 | 25.0 |
| Crypt-associated cells | 50.0 | 2.0 | 5.0 | 50.0 | 50.0 |
n.i.: not inhibitory; tested up to 20 mM.
Numbers in parentheses denote relative inhibitory potency using activitiy of free GalNAc as standard set to 1.