neutral endopeptidase

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

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.

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

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

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

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

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

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

(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.

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.

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).

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).

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.

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.