Home Proteases Neprilysin inhibitor - Apoptosis related activator - Angiotensin Receptor inhibitor Sacubitril/valsartan (LCZ696)

Sacubitril/valsartan (LCZ696)

Catalog No.S7678 Synonyms: Sacubitril, Valsartan

For research use only.

Sacubitril/valsartan (LCZ696, Sacubitril, Valsartan), consisting of valsartan and sacubitril in 1:1 molar ratio, is an orally bioavailable, dual-acting angiotensin receptor-neprilysin inhibitor (ARNi) for hypertension and heart failure. Phase 3.

Sacubitril/valsartan (LCZ696) Chemical Structure

CAS No. 936623-90-4

Selleck's Sacubitril/valsartan (LCZ696) has been cited by 6 Publications

2 Customer Reviews

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Biological Activity

Description Sacubitril/valsartan (LCZ696, Sacubitril, Valsartan), consisting of valsartan and sacubitril in 1:1 molar ratio, is an orally bioavailable, dual-acting angiotensin receptor-neprilysin inhibitor (ARNi) for hypertension and heart failure. Phase 3.
Targets
RAAS [1]
Assay
Methods Test Index PMID
Western blot p-AMPKα / AMPKα / p-AKT / AKT / p-eNOS / eNOS ; p-LKB1 / t-LKB1 / p-AMPK / t-AMPK / p-ACC / t-ACC 28178430 25109475
In vivo In double-transgenic rats overexpressing human renin and angiotensinogen and plasma atrial natriuretic peptide immunoreactivity, LCZ696 (60 mg/kg p.o.) induces a dose-dependent and long-lasting reduction in mean arterial pressure (MAP), and stimulates a rapid and dose-dependent augmentation of plasma ANP immunoreactivity. [1] In rat myocardial infarction (MI) model, LCZ696 (68 mg/kg p.o.) attenuates cardiac remodeling and dysfunction after myocardial infarction by reducing cardiac fibrosis and hypertrophy. [2]

Protocol (from reference)

Animal Research:

[2]
  • Animal Models: Double-transgenic rats overexpressing human renin and angiotensinogen and plasma atrial natriuretic peptide immunoreactivity
  • Dosages: ~60 mg/kg
  • Administration: p.o.

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 915.98
Formula

C24H29N5O3.C24H29NO5.5/2H2O.3Na
CAS No. 936623-90-4
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles [Na+].[Na+].[Na+].CCCCC(=O)N(CC1=CC=C(C=C1)C2=CC=CC=C2C3=NN=N[NH]3)C(C(C)C)C(O)=O.CCOC(=O)C(C)CC(CC4=CC=C(C=C4)C5=CC=CC=C5)NC(=O)CCC(O)=O

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02690974 Completed Drug: LCZ696 (sacubitril/valsartan) Hearth Failure With Reduced Ejection Fraction (HFrEF) Novartis Pharmaceuticals|Novartis March 8 2016 Phase 4
NCT02661217 Completed Drug: LCZ696 Heart Failure With Reduced Ejection Fraction Novartis Pharmaceuticals|Novartis February 12 2016 Phase 4
NCT02226120 Completed Drug: LCZ696 Chronic Heart Failure With Reduced Ejection Fraction Novartis Pharmaceuticals|Novartis October 16 2014 Phase 3

(data from https://clinicaltrials.gov, updated on 2022-08-01)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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