Neprilysin

Neprilysin inhibitors block a zinc endopeptidase that inactivates natriuretic and opioid peptides. Neprilysin (NEP), also called neutral endopeptidase, was purified in 1974 from rabbit kidney brush border membranes. In 1978 a high-affinity enkephalin-degrading peptidase was described in brain, and the activity became known as enkephalinase. Further NEP substrates include atrial natriuretic peptide, bradykinin, substance P and amyloid-β peptides. Sacubitril calcium and candoxatril are prodrugs, and sacubitrilat is the active form of sacubitril. Racecadotril is a prodrug of an enkephalinase inhibitor, and phosphoramidon disodium salt is a microbial metalloendopeptidase inhibitor. Omapatrilat blocks both NEP and angiotensin-converting enzyme (ACE), while Sacubitril/Valsartan combines NEP inhibition with angiotensin receptor blockade.

Items 1-25 of 44

  • TD-0212
    Cat. No.
    A13715

    TD-0212

    TD-0212 (compound 35) is an orally active dual pharmacology angiotensin II type 1 receptor (AT1) antagonist and neprilysin (NEP) inhibitor, with a pKi of 8.9 for AT1 and a pIC50 of 9.2 for NEP.

    1 mg
    $355.00
    5 mg
    $1,075.00
    All 6 sizes
  • LHW090-A7
    Cat. No.
    A13885

    LHW090-A7

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

    2 mg
    $25.00
    5 mg
    $45.00
    All 4 sizes
  • Sacubitril hemicalcium salt
    Cat. No.
    A18053

    Sacubitril hemicalcium salt

    Synonyms: AHU-377 hemicalcium salt

    Sacubitril hemicalcium salt is a potent neprilysin (NEP) inhibitor, demonstrating an IC50 of 5 nM. This compound plays a critical role in heart failure research and is a key component of the therapeutic agent LCZ696. Its mechanism of action involves the elevation of natriuretic peptides, contributing to improved cardiovascular function and offering insights into novel heart failure treatments.

    2 mg
    $25.00
    5 mg
    $40.00
    All 8 sizes
  • Omapatrilat
    Cat. No.
    A21059

    Omapatrilat

    Synonyms: BMS-186716

    Omapatrilat is a dual inhibitor of the metalloproteases ACE and NEP with Ki values of 0.64 and 0.45 nM, respectively.

    2 mg
    $55.00
    5 mg
    $75.00
    All 6 sizes
  • Sch-42495 racemate
    Cat. No.
    A21408

    Sch-42495 racemate

    Synonyms: Sch42495

    Sch-42495 racemate is the racemate of Sch-42495. Sch-42495 is a novel neutral metalloendopeptidase (NEP) inhibitor. Sch-42495 is the orally active ethylester prodrug of SCH 42354.

    1 mg
    $200.00
    5 mg
    $500.00
    All 6 sizes
  • Opiorphin
    Cat. No.
    A23064

    Opiorphin

    Opiorphin, an opioid peptide, is a potent enkephalin-inactivating zinc ectopeptidases in human inhibitor. Opiorphin inhibits two enkephalin-catabolizing ectoenzymes, human neutral ecto-endopeptidase, hNEP (EC 3.4.24.11) with an IC50 value of 11 μM, and human ecto-aminopeptidase, hAP-N (EC 3.4.11.2). Opiorphin displays potent analgesic activity by activating endogenous opioid-dependent transmission.

    10 mg
    $45.00
    25 mg
    $95.00
    All 3 sizes
  • Fasidotril
    Cat. No.
    A42310

    Fasidotril

    Synonyms: Alatriopril

    Fasidotril is a dual inhibitor of neprilysin and angiotensin-converting enzyme (ACE). It demonstrates significant biological activity in the modulation of blood pressure and fluid balance, making it a valuable tool in hypertension and congestive heart failure (CHF) research. The compound's ability to inhibit both pathways provides insight into the therapeutic potential for cardiovascular disease management.

    25 mg
    $1,530.00
    50 mg
    $1,950.00
    All 3 sizes
  • AD015
    Cat. No.
    A42313

    AD015

    AD015 is a dual inhibitor of angiotensin-converting enzyme (ACE) and neprilysin (NEP). It exhibits potent inhibitory activity against NEP, with an IC50 of 0.009 µM, and shows strong inhibition of both nephron ACE (nACE) and cardiac ACE (cACE), with IC50 values of 0.019 µM and 0.0008 µM, respectively. This compound is valuable for research in cardiovascular and renal physiology, particularly in studies related to hypertension and heart failure, where modulation of the renin-angiotensin system is critical.

    Out of stock

    All 3 sizes
  • Z-13752A
    Cat. No.
    A42351

    Z-13752A

    Z-13752A is a mercaptopropanoyl amino acid that functions as an inhibitor of neprilysin (NEP) and angiotensin-converting enzyme (ACE) with Ki values of 1.8 nM and 3.2 nM, respectively. This compound has been shown to effectively reduce arterial blood pressure while enhancing coronary blood flow. Z-13752A is valuable for research focused on coronary artery occlusion and related cardiovascular conditions.

    Out of stock

    All 3 sizes
  • AD011
    Cat. No.
    A42360

    AD011

    AD011 is a dual inhibitor of carboxypeptidase angiotensin-converting enzyme (cACE) and neprilysin (NEP). This compound is derived from the C-domain selective ACE inhibitor lisinopril-tryptophan and demonstrates significant antihypertensive and cardioprotective effects. AD011 is suitable for research applications focused on cardiovascular health and the modulation of renin-angiotensin system pathways.

    Out of stock

    All 3 sizes
  • AD013
    Cat. No.
    A42365

    AD013

    AD013 is a dual inhibitor of the enzymes cACE (constitutive Angiotensin-Converting Enzyme) and NEP (Neutral Endopeptidase). This compound is derived from a C-domain selective ACE inhibitor and has demonstrated significant potential in providing antihypertensive and cardioprotective effects. AD013 serves as a valuable reagent for research focused on cardiovascular diseases and hypertension therapies.

    Out of stock

    All 3 sizes
  • AD012
    Cat. No.
    A42370

    AD012

    AD012 is a dual inhibitor of the enzymes neprilysin (NEP) and angiotensin-converting enzyme (cACE). Designed from the C-domain selective ACE inhibitor, lisinopril-tryptophan, AD012 demonstrates significant antihypertensive and cardioprotective properties. This compound is valuable for research in cardiovascular health and the treatment of hypertension.

    Out of stock

    All 3 sizes
  • GW 796406
    Cat. No.
    A42373

    GW 796406

    GW 796406 is a potent neprilysin (NEP) inhibitor with an IC50 value of approximately 1.1-2.5 nM, exhibiting a higher selectivity compared to ACE, which has an IC50 of around 1.6-4.7 nM. This compound is valuable for exploring mechanisms involved in cardiovascular diseases and may aid in the development of therapeutics targeting NEP-related pathways. GW 796406's specificity and efficacy make it a useful tool for researchers studying cardiovascular health and related disorders.

    Out of stock

    All 3 sizes
  • RB-105
    Cat. No.
    A42382

    RB-105

    RB-105 is a potent dual inhibitor of angiotensin-converting enzyme (ACE) and neutral endopeptidase (NEP), with Ki values of 4.2 nM and 1.7 nM, respectively. By inhibiting ACE, RB-105 decreases angiotensin II production and enhances bradykinin levels, while NEP inhibition further elevates natriuretic peptide levels, resulting in a synergistic increase in bradykinin. This compound exhibits significant antihypertensive and natriuretic effects in both spontaneously hypertensive and normotensive rat models, making RB-105 a valuable reagent for studies on hypertension and related cardiovascular conditions.

    Out of stock

    All 3 sizes
  • Aladotril
    Cat. No.
    A42399

    Aladotril

    Synonyms: BP1137

    Aladotril, a dual inhibitor of neutral endopeptidase (NEP) and angiotensin-converting enzyme (ACE), exhibits potential in ameliorating cardiac hypertrophy without reducing blood pressure. This compound is valuable for research focused on heart failure and the mechanisms of cardiac remodeling following myocardial infarction. Its unique properties make it an important tool for studying cardiovascular health and therapeutic interventions.

    25 mg
    $1,655.00
    50 mg
    $2,115.00
    All 3 sizes
  • CGS 35601
    Cat. No.
    A42408

    CGS 35601

    CGS 35601 is a potent inhibitor of endothelin-converting enzyme-1 (ECE-1), neutral endopeptidase 24.11 (NEP), and angiotensin-converting enzyme (ACE), exhibiting IC50 values of 55 nM, 2 nM, and 22 nM, respectively. This compound effectively suppresses pressor responses induced by big endothelin-1 and angiotensin I, while simultaneously enhancing the circulation of atrial natriuretic peptide (ANP). CGS 35601 serves as a valuable tool in cardiovascular research, particularly in delineating the regulatory mechanisms of cardiovascular function in animal models.

    25 mg
    $1,275.00
    50 mg
    $1,625.00
    All 3 sizes
  • Alatrioprilat
    Cat. No.
    A42422

    Alatrioprilat

    Alatrioprilat is an orally active inhibitor of angiotensin-converting enzyme (ACE) and neprilysin, with an IC50 of 19.6 nM for ACE and 6.1 nM for neprilysin. This compound is significant in the metabolism of hormonal peptides, particularly in the degradation of nitric oxide and atrial natriuretic factor (ANF). Alatrioprilat is applicable in cardiovascular disease research, offering insights into therapeutic strategies for conditions influenced by these pathways.

    25 mg
    $1,655.00
    50 mg
    $2,115.00
    All 3 sizes
  • Sialorphin
    Cat. No.
    A53765

    Sialorphin

    Sialorphin targets neprilysin (NEP) and aminopeptidase N (APN) as a potent inhibitor, effectively preventing the degradation of key neuropeptides like Substance P and methionine enkephalin. This compound demonstrates significant biological activity, including analgesic effects, modulation of sexual behavior in male rats, and the alleviation of colitis. Additionally, Sialorphin exhibits low toxicity against specific tumor cells, making it a valuable tool for research into pain management, inflammatory bowel disease, and oncology.

    Out of stock

    All 3 sizes
  • TD-0212 TFA
    Cat. No.
    A58926

    TD-0212 TFA

    TD-0212 TFA is an orally active dual pharmacology inhibitor targeting the angiotensin II type 1 receptor (AT1) and neprilysin (NEP). With a pKi of 8.9 for AT1 and a pIC50 of 9.2 for NEP, this compound exhibits significant biological activity in modulating cardiovascular and neuroprotective pathways. TD-0212 TFA is suitable for research applications exploring the roles of AT1 antagonism and neprilysin inhibition in various disease models.

    1 mg
    $145.00
    5 mg
    $375.00
    All 6 sizes

Items 1-25 of 44

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