Table 1.
Specificity of neprilysin inhibitors (Ki or IC50).
| Inhibitor (units for Ki or IC50) | Neprilysin | NEP2 | ACE | ECE-1 | ECE-2 | APP | References |
|---|---|---|---|---|---|---|---|
| Thiorphan (nmol/L) | 4, 4.7 | 120, 129, 250 | 150 | No | >10 μmol/L# | >100 μmol/L | (2–6) |
| Phosphoramidon (nmol/L) | 1.5, 2 | 0.8, 1.0 | 2 | 680*, 675* | 1.2#, 4# | >10 μmol/L | (2, 3, 5–9) |
| Candoxatrilat (nmol/L) | 3.2, 9.5 | 44 | >10 μmol/L | 6.5† | >10 μmol/L | (10, 11) | |
| Omapatrilat (nmol/L) | 0.45, ~2, 3, 5–8 | 8, 17, 25 | 0.64, 0.98, 5 | 10 μmol/L† | 194, 250, 260 | (3, 10–13) | |
| LBQ657 (nmol/L) | 2.3, 5 | Yes | Yes, >10 μmol/L | No | Yes | No | (14–16) |
Inhibitor concentrations are shown as nmol/L, except where indicated to be μmol/L.
*
pH: 7.2;
†
pH 6.5;
#
pH 5.5.
ACE, angiotensin converting enzyme; APP, aminopeptidase P; ECE-1, endothelin converting enzyme 1; ECE-2, endothelin converting enzyme 2; NEP2, neprilysin homolog membrane metalloendopeptidase-like 1.