neutral endopeptidase

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

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

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

Candoxatril (UK 79300) is an orally active neutral peptide endonuclease (NEP, EC 3.4.24.11) inhibitor that improves exercise capacity in patients with chronic heart failure undergoing angiotensin-converting enzyme inhibition.

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

(Rac)-Daglutril (SLV 306 acetic acid) is the racemate form of Daglutril. Daglutril is an orally active, mixed neutral endopeptidase endothelin converting enzyme inhibitor under development for the treatment of essential hypertension and congestive heart failure.

Desonide (Prednacinolone) is a synthetic glucocorticosteroid for topical use, with anti-inflammatory activity. Desonide binds to glucocorticoid receptors in the cytoplasm, and the ligand-receptor complex is translocated as a homodimer into the nucleus, where transcription activation via glucocorticoid response elements within glucocorticoid-responsive genes occur. This agent induces transcription of genes coding for anti-inflammatory proteins, including lipocortin-1, interleukin-10, interleukin-1 receptor antagonist and neutral endopeptidase. Increased synthesis of lipocortin-1 has an inhibitory effect on phospholipase A2, which in turn inhibits the release of arachidonic acid, thereby controlling the biosynthesis of potent mediators of inflammation such as prostaglandins and leukotrienes.

Sacubitril Valsartan (LCZ696) is an orally bioavailable, dual angiotensin II receptor and neprilysin inhibitor for the treatment of hypertension and heart failure.

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.

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

Sar-[D-Phe8]-des-Arg9-Bradykinin acetate is a potent and selective bradykinin B1 receptor agonist (EC50 = 9.02 nM in rabbit aorta) that is resistant to aminopeptidase, kininase I and II (ACE) and neutral endopeptidase cleavage. Exhibits hypotensive and angiogenic activity in vivo.

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.

Sampatrilat is an effecive and orally active vasopeptidase inhibitor of ACE and neutral endopeptidase. Sampatrilat inhibits C-domain ACE (Ki=13.8 nM) 12.4-fold more potent than that for the N-domain (Ki=171.9 nM).

Aladotril is an inhibitor of neutral endopeptidase. Its prodrug is aladotrilat.

Aladotrilat is an inhibitor of neutral endopeptidase. Its prodrug is aladrotril.

RB 101 suppresses enkephalinase and aminopeptidases; biologically cleaved at disulfide to produce inhibitors of both aminopeptidase N and neutral endopeptidase.

Sch 34826 is a potent, selective neutral endopeptidase inhibitor.

UK-414,495 is a potent, selective inhibitor of the neutral endopeptidase, the enzyme normally serves to break down the neuropeptide VIP.

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

Candoxatrilat (U 73967, UK69578) is an active neutral endopeptidase inhibitor that reduces atrial natriuretic peptide degradation.

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].