CGS-30440 is a potent and orally active dual inhibitor of neutral endopeptidase (NEP) and angiotensin-converting enzyme (ACE). CGS-30440 exhibit antihypertensive and natriuretic effects. CGS-30440 also shows protective effect for chronic renal failure. CGS-30440 can be used for the research of cardiovascular disease, such as hypertension.

BL-2401 is an orally active enkephalinase inhibitor. BL-2401 exhibit antinociceptive and antidepressant-like activitiesin association with endogenous opioid systems. BL-2401 can be used for the research of neurological disease.

GW 796406 is a novel vascular peptidase inhibitor. GW 796406’s inhibitory activity against NEP (IC50 ≈ 1.1-2.5 nM) is about three times that of ACE (IC50 ≈ 1.6-4.7 nM). GW 796406 can be used for research on cardiovascular conditions.

SDUY817 is a dual APN/NEP inhibitor, with IC50 values of 0.29 μM for APN and 7.4 μM for NEP. SDUY817 exerts analgesic effects in a concentration- and time-dependent manner, and can be used for research in the field of neuropathic pain disorders.

Thiorphan (DL-3-Mercapto-2-benzylpropanoylglycine) is a selective NEP (neprilysin) inhibitor with an IC50 of 6.9 nM. It is also a potent inhibitor of enkephalinase, with antinociceptive activity.

LCZ696 is a first-in-class dual inhibitor of the angiotensin II receptor(AT II receptor) and neprilysin; a novel single molecule comprising molecular moieties of valsartan and NEP inhibitor prodrug AHU377 (1:1 ratio).

SCH-42354 is a potent, orally active neutral endopeptidase (NEP) inhibitor, is the pharmacologically active form of the prodrug SCH-42495. SCH-42354 inhibits the hydrolysis of NEP to enhance the activity of atrial natriuretic peptide (ANP). SCH-42354 inhibits hydrolysis of leu-enkephalin and ANF with IC50 values of 8.3 nM and 10.0 nM, respectively. SCH-42354 has antihypertensive activity.

Racecadotril (acetorphan), a potent enkephalinase inhibitor (IC50= 4.5 uM), protects endogenous enkephalins from degradation.