neutral endopeptidase (nep)

Candoxatril (UK 79300) is a small-molecule inhibitor and a neutral endopeptidase (NEP) inhibitor with oral activity and cell permeability, used for the treatment of chronic heart failure and capable of improving exercise capacity in patients receiving angiotensin-converting enzyme inhibitor therapy.

NEP-IN-1 is an inhibitor of neutral endopeptidase (NEP, IC₅₀ = 2 nM) and can be used in studies about female sexual arousal disorders.

Sacubitril hemicalcium salt (AHU377 calcium salt) is a potent NEP inhibitor with an IC₅₀ of 5 nM. Sacubitril hemicalcium salt is a component of the heart failure medicine LCZ696. Sacubitril hemicalcium salt is a prodrug of LBQ657, which is an inhibitor of the zinc metallopeptidase neprilysin. Neprilysin degrades a variety of vasoactive peptides such as atrial and brain natriuretic peptide, bradykinin, adrenomedullin, and endothelin-1. Inhibition of neprilysin leads to an increased level of these peptides and, thus, antihypertensive effects. Formulations containing AHU377 in combination with the angiotensin II receptor antagonist valsartan are used to treat hypertension and heart failure.

Sacubitril (AHU-377) is a potent NEP inhibitor with an IC₅₀ of 5 nM and is a component of the heart failure medicine LCZ696.

LHW090-A7 is an neutral endopeptidase (NEP) inhibitor, and an enzyme responsible for the metabolic inactivation of enkephalins.

Racecadotril (Acetorphan) has been investigated for the basic science and treatment of Diarrhea, Acute Diarrhea, and Acute Gastroenteritis.

Ilepatril TFA is a dual inhibitor of angiotensin-converting enzyme (ACE) and neutral endopeptidase (NEP), exhibiting physiological effects such as enhanced natriuresis and vasodilation. In animal studies and early clinical trials, Ilepatril TFA has demonstrated the ability to improve insulin sensitivity and metabolic abnormalities, suggesting its potential value in the treatment of cardiovascular and metabolic diseases.

SQ28603 is a potent and selective inhibitor of neutral endopeptidase 3.4.24.11 (NEP).

NEP-IN-2 is a neutral endopeptidase inhibitor used in the research of proliferation in atherosclerosis and restenosis.

CGS-24592 is an orally active, selective, and potent inhibitor of neutral endopeptidase 24.11 (NEP), with an IC₅₀ value of 1.6 nmol/L. It reduces the degradation of atrial natriuretic peptide (ANP), thereby increasing plasma ANP concentration and lowering blood pressure. CGS-24592 shows potential for research in cardiovascular diseases such as hypertension and congestive heart failure.

CGS-30440 is a potent, orally active dual inhibitor of neutral endopeptidase (NEP) and angiotensin-converting enzyme (ACE). It exhibits antihypertensive and natriuretic effects while also providing protective benefits in chronic renal failure. CGS-30440 is applicable in cardiovascular disease research, such as hypertension.

UK-447841, a neutral endopeptidase (NEP) inhibitor, is used potentially for the treatment of female sexual dysfunction.

Ecadotril is a neutral endopeptidase (NEP) inhibitor, which plays an anti hypertensive role.

Aminopeptidase N (AP-N) inhibitor is a reversible inhibitor of AP-N/CD13 (IC₅₀ = 25 μM). It is selective for AP-N/CD13 over matrix metalloproteinase-9 (MMP-9), angiotensin converting enzyme (ACE), neutral endopeptidase (NEP), γ-glutamyl transpeptidase, and the serine proteases dipeptidyl peptidase 4 (DPP-4) and cathepsin G at a concentration of 1 mM. AP-N inhibitor is non-cytotoxic to U937 cells at a concentration of 100 μM.

GLP-1(28-36)amide, a C-terminal nonapeptide derived from the cleavage of GLP-1 by neutral endopeptidase (NEP), is an important compound that functions as an antioxidant primarily targeting the mitochondrion to inhibit mitochondrial permeability transition (MPT), displaying anti-diabetic properties and cardioprotection effects[1].

SCH-42354 is a potent, orally active inhibitor of neutral endopeptidase (NEP), serving as the active form of the prodrug SCH-42495. By inhibiting NEP hydrolysis, SCH-42354 enhances the activity of atrial natriuretic peptide (ANP) and prevents the hydrolysis of leu-enkephalin and ANF with IC₅₀ values of 8.3 nM and 10.0 nM, respectively. Furthermore, SCH-42354 exhibits antihypertensive activity [1] [2].

Phosphoramidon Disodium (Phosphoramidon Disodium Salt) Salt is a metalloendopeptidase inhibitor, widely used as a biochemical tool.

CGS 25462 is a neutral endopeptidase (NEP) inhibitor.

MDL-100173 is a dual angiotensin-converting enzyme (ACE)/neutral endopeptidase (NEP) inhibitor.

GLP-1(28-36)amide TFA, a C-terminal nonapeptide derived from GLP-1 cleavage by neutral endopeptidase (NEP), is an antioxidant that targets mitochondria and inhibits mitochondrial permeability transition (MPT), demonstrating anti-diabetic and cardioprotective effects [1].

Thiorphan is an neprilysin inhibitor (NEP; IC₅₀ : 0.007 μM).

Sialorphin TFA is an inhibitor of neutral endopeptidase (NEP) and aminopeptidase N (APN), which is responsive to androgen signaling. It inhibits the degradation of endogenous opioid peptides, interacting with μ-, δ-, and κ-opioid receptors. Sialorphin TFA modulates the ERK/mTOR signaling pathway by inducing cell cycle arrest, enhancing ERK1/2 activity, and reducing phosphorylation levels of mTOR, 4E-BP1, and p70S6K, thereby exhibiting antiproliferative activity against colorectal cancer, glioma, and prostate cancer cells without cytotoxicity. Additionally, it possesses anti-nociceptive properties, regulates sexual behavior, relaxes penile corpus cavernosum smooth muscle, and alleviates experimental colitis. Moreover, Sialorphin TFA serves as a copper (II) ion-binding ligand and has been utilized in mechanistic studies related to cancer, pain management, and inflammatory bowel disease.

Sacubitrilat (LBQ-657) (LBQ657) is an effective inhibitor of active neprilysin (NEP).