Neprilysin Inhibitor

Sacubitril/Valsartan (LCZ696), comprised Valsartan and Sacubitril (AHU377) in 1:1 molar ratio, is a first-in-class, orally bioavailable, and dual-acting angiotensin receptor-neprilysin (ARN) inhibitor for hypertension and heart failure. Sacubitril/Valsartan ameliorates diabetic cardiomyopathy by inhibiting inflammation, oxidative stress and apoptosis.

Sacubitril (AHU-377) is a potent and orally active NEP (neprilysin) inhibitor with an IC₅₀ of 5 nM. Sacubitril is a component of the heart failure medicine LCZ696. Sacubitril can be used for the research of heart failure, hypertension and COVID-19.

Sacubitrilat (Desethyl Sacubitril) is an active neprilysin (NEP) inhibitor.

Thiorphan is a selective neprilysin (NEP) inhibitor with an IC₅₀ of 6.9 nM. Thiorphan competitively binds to NEP and blocks its activity, preventing the degradation of neuropeptides such as substance P (SP) and neurokinin NKA. In the field of neonatal brain injury research, Thiorphan can increase the levels of SP and NKA, activate NK1 and NK2 receptors and downstream transduction pathways, and inhibit excessive activation of NMDA receptors. Thus, Thiorphan can protect neocortical neurons from excitotoxic cell death. Thiorphan may also inhibit NEP from enhancing bronchoconstriction and can be used in the study of respiratory diseases.

Phosphoramidon disodium, a microbial metabolite, is a specific metalloprotease thermolysin inhibitor with an IC₅₀ of 0.4 μg/mL. Phosphoramidon disodium also inhibits endothelin-converting enzyme (ECE), neutral endopeptidase (NEP), and angiotensin-converting enzyme (ACE) with IC₅₀ values of 3.5, 0.034, and 78 μM, respectively.

Racecadotril (Acetorphan) is a neutral endopeptidase (NEP) inhibitor. Racecadotril and its active metabolite Thiorphan inhibits purified NEP activity from mouse brain with K_is of 4500 and 6.1 nM, , respectively. Antidiarrheal agent.

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.

Sacubitril sodium is a potent and orally active NEP (neprilysin) inhibitor, with an IC₅₀ of 5 nM. Sacubitril sodium enhances the tone of the natriuretic peptide (NP) system and exerts significant antihypertensive effects. Sacubitril sodium is a component of the heart failure medicine LCZ696. Sacubitril sodium can be used for the research of heart failure, hypertension and COVID-19.

Met-Arg-Phe-Ala is a peptide. Met-Arg-Phe-Ala also is a potent competitive inhibitor for enkephalin-generating endopeptidase (EGE). Met-Arg-Phe-Ala can be used for the research of neurological disease.

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

Phenylalanylalanine (H-Phe-Ala-OH) is a dipeptide composed of phenylalanine and alanine. Phenylalanylalanine is an incomplete breakdown product of protein digestion or protein catabolism.

Candoxatril is a neutral endopeptidase (NEP) inhibitor.

Sampatrilat (UK-81252) is a potent and orally active vasopeptidase inhibitor of ACE and neutral endopeptidase (NEP). Sampatrilat inhibits C-domain ACE (K_i=13.8 nM) 12.4-fold more potent than that for the N-domain (K_i=171.9 nM). Sampatrilat (UK-81252) can be used for the study of chronic heart failure and blood pressure regulation.

Sacubitril-d₄ is the deuterium labeled Sacubitril. Sacubitril (AHU-377) is a potent NEP inhibitor with an IC50 of 5 nM. Sacubitril (AHU-377) is a component of the heart failure medicine LCZ696.

JA2 is an inhibitor of metalloendopeptidase 24.15 that can potentiate the hypotensive response to bradykinin in rat.

Sacubitrilat-d₄ is the deuterium labeled Sacubitrilat. Sacubitrilat (Desethyl Sacubitril) is an active neprilysin (NEP) inhibitor.

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

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

Kelatorphan is a full inhibitor of enkephalin degrading enzymes.

Sacubitril-d₄ hemicalcium salt is the deuterium labeled Sacubitril hemicalcium salt (HY-15407A). Sacubitril hemicalcium salt is a potent NEP inhibitor with an IC₅₀ of 5 nM.