Sacubitril sodium

Names

[ Name ]:
Sacubitril sodium

[Synonym ]:
AHU-377 sodium salt
UNII-MOP72GEP8Z

Biological Activity

[Description]:

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[1][2][3].

[Related Catalog]:

Research Areas >> Cardiovascular Disease

Research Areas >> Infection

Signaling Pathways >> Metabolic Enzyme/Protease >> Neprilysin

[In Vitro]

Sacubitril sodium increases neprylisin-degraded peptides, such as natriuretic peptides (NPs), peptide natriuretic atrial (ANP) and peptide natriuretic brain (BNP)[2].

[In Vivo]

In normotensive rats, pretreatment with Sacubitril sodium (3, 10 and 30 mg/kg, PO.) augments ANP-evoked plasma cGMP levels by 2.4, 3.3 and 4.0 fold, respectively (4h AUC compared to vehicle)[1]. Sacubitril sodium (30 and 100 mg/kg, PO) produces a dose-dependent antihypertensive effect in Dahl-SS rats[1].

[References]

[1]. Hegde, L.G., et al. Comparative efficacy of AHU-377, a potent neprilysin inhibitor, in two rat models of volume-dependent hypertension. BMC Pharmacol 11, P33 (2011).

[2]. Vitiello A, et al. Sacubitril, valsartan and SARS-CoV-2. BMJ Evid Based Med. 2020 Jul 27:bmjebm-2020-111497.

[3]. Chrysant SG. Pharmacokinetic, pharmacodynamic, and antihypertensive effects of the neprilysin inhibitor LCZ-696: sacubitril/valsartan. J Am Soc Hypertens. 2017 Jul;11(7):461-468.

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₄H₂₈NNaO₅

[ Molecular Weight ]:
433.47300

[ Exact Mass ]:
433.18700

[ PSA ]:
99.02000

[ LogP ]:
4.54780

[ Storage condition ]:
2-8°C

Safety Information

[ Hazard Codes ]:
Xi

Precursor & DownStream

Precursor

DownStream

Related Compounds

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