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

Purity & Quality Control

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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

 Water 100 mg/mL warmed
(109.17 mM)
DMSO 30 mg/mL warmed
(32.75 mM)
Ethanol ''9 mg/mL warmed

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

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

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

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
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Molarity Calculator

Mass Concentration Volume Molecular Weight

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 2022-01-17)

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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