Sacubitril/valsartan (LCZ696)

Name: Sacubitril/valsartan (LCZ696)
Brand: Selleck Chemicals
SKU: S7678
Rating: 5 (2 reviews)

For research use only.

Catalog No.S7678 Synonyms: Sacubitril, Valsartan

2 publications

Sacubitril/valsartan (LCZ696) Chemical Structure

CAS No. 936623-90-4

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.

Selleck's Sacubitril/valsartan (LCZ696) has been cited by 2 publications

J Mol Cell Cardiol, 2017, 108:138-148

PubMed: 28623750 ( click the link to review the publication )

RSC Adv, 2017, 10.1039/C7RA01404J

PubMed: ( click the link to review the publication )

2 Customer Reviews

Histological analysis staining of three groups. (a) Representative H&E-staining micrographs displaying transverse myocardial section (original magnification ×200). (b) Masson staining of three groups (original magnification ×200). Collagen content (%) of heart tissues were presented as fibrosis (***P < 0.001, n = 7 per group). (c) Cardiac section of three group mice hearts stained with WGA (original magnification ×400) (*P < 0.05, n = 7 per group). (d) The expression of Drp1 significantly increased in DOX group (***P < 0.001, n = 7 per group) and it decreased in DOX + LCZ696 group (**P < 0.01, n = 7 per group).

J Mol Cell Cardiol, 2017, 108:138-148. Sacubitril/valsartan (LCZ696) purchased from Selleck.

Representative H&E stain of heart sections from (A) sham-operated group, (B) model group, (C) LCZ696-treated group. Representative H&E-staining micrographs displaying transverse myocardial section (original magnification ×100).

RSC Adv, 2017, doi:10.1039/C7RA01404J. Sacubitril/valsartan (LCZ696) purchased from Selleck.

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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 ; PubMed: 28178430 Bosn J Basic Med Sci Effects of valsartan (10 µmol/L) on Akt, adenosine monophosphate-activated protein kinase (AMPK) and endothelial nitric oxide synthase (eNOS) phosphorylation and expression in human umbilical vein endothelial cells. Ctrl: control; Antibodies: p-AMPKα (Thr172) - phospho-AMPKα (Thr172), AMPKα, p-Akt (Ser473) - phospho-Akt (Ser473), Akt, p-eNOS (Ser1177) - phospho-eNOS (Ser1177), eNOS, and beta-actin. p-LKB1 / t-LKB1 / p-AMPK / t-AMPK / p-ACC / t-ACC ; PubMed: 25109475 J Cell Mol Med To confirm that valsartan activates AMPK through LKB1, THP-1 cells were transfected with LKB1 siRNA or scrambled siRNA and incubated with valsartan for 24 hrs. The proteins were quantified and Western blot analysis was performed with corresponding antibodies (P-AMPK, AMPK, p-LKB1, LKB1, p-ACC and ACC). The relative intensity of each protein is depicted as bar graphs on the right side	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

Animal Research: ^[2]	- Collapse Animal Models: Double-transgenic rats overexpressing human renin and angiotensinogen and plasma atrial natriuretic peptide immunoreactivity Dosages: ~60 mg/kg Administration: p.o. (Only for Reference)

References

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

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information Download Sacubitril/valsartan (LCZ696) SDF

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
Synonyms	Sacubitril, Valsartan
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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Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2020-01-06)

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

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Sacubitril/valsartan (LCZ696)