nep-in-1

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.

Daglutril, a NEP/ECE inhibitor, is potentially used for the treatment of hypertension, heart failure andpulmonary. Daglutril inhibits systemic conversion of big endothelin-1 in humans.

NEP(1-40) TFA is a peptide antagonist of the Nogo-66 receptor (NgR), which attenuates myelin-derived inhibition and mitigates injury-induced shifts in microglial morphology distributions [1].