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Inhibition of hIDE-mediated catabolism of insulin and glucagon
| Compound | Screening assay IC50a | Glucagon mesoscale IC50b |
|---|---|---|
| nm | nm | |
| 1 | 2000 ± 1000 | 2100 ± 790 |
| 2 | 2000 ± 400 | >100,000 |
| NTE-1 | 4 ± 2 | 3 ± 1 |
| NTE-2 | 4 ± 1 | 150 ± 78 |
a Relative IC50 values. Conditions: insulin = 500 pm, CF-hIDE = 375 pm, 22 °C, 4 h.
b Relative IC50 values. Conditions: glucagon = 1 nm, CF-hIDE = 20 pm, 37 °C, 0.5 h.
