Art. -Nr.: HY-18204A

Sacubitril/Valsartan

(Synonyms: LCZ696)

10 Cited Publications

Kundenbewertung

Based on 10 publication(s) in Google Scholar

Sacubitril/Valsartan (LCZ696), comprised Valsartan and Sacubitril (AHU377) in 1:1 molar ratio, is a first-in-class, orally bioavailable, and dual-acting angiotensin receptor-neprilysin (ARN) inhibitor for hypertension and heart failure. Sacubitril/Valsartan ameliorates diabetic cardiomyopathy by inhibiting inflammation, oxidative stress and apoptosis.

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Reinheit: 99.96%
CAS. Nr.: 936623-90-4
Formel: C₄₈H₅₅N₆Na₃O₈.2.5H₂O
Molecular Weight:957.99

Speicherung:

4°C, sealed storage, away from moisture

* In solvent : -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture)

Sacubitril/Valsartan Chemical Structure

CAS. Nr.: 936623-90-4

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (10)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Sacubitril/Valsartan (LCZ696), comprised Valsartan and Sacubitril (AHU377) in 1:1 molar ratio, is a first-in-class, orally bioavailable, and dual-acting angiotensin receptor-neprilysin (ARN) inhibitor for hypertension and heart failure^[1]^[2]^[3]. Sacubitril/Valsartan ameliorates diabetic cardiomyopathy by inhibiting inflammation, oxidative stress and apoptosis^[4].

IC₅₀ & Target

Angiotensin receptor-neprilysin^[1]

Alle Angiotensin Receptor Isoform-spezifische Produkte anzeigen :

In Vitro

Sacubitril/Valsartan (LCZ696; 1-30 μM; 0.5 hours) inhibits HG-treated H9C2 cells apoptosis in an experimental model of Diabetic cardiomyopathy (DCM)^[4].
Sacubitril/Valsartan (1-30 μM; 0.5 hours) increases the expression level of cleaved caspase-3 and the ratio of Bax/Bcl-2 in HG-treated H9C2 cells^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Apoptosis Analysis^[4]

Cell Line:

HG-treated H9C2 cells
Concentration:

1, 10, or 30 µM
Incubation Time:

0.5 hours
Result:

Inhibited HG-treated H9C2 cells apoptosis.

Western Blot Analysis^[4]

Cell Line:

HG-treated H9C2 cells
Concentration:

1, 10, or 30 µM
Incubation Time:

0.5 hours
Result:

Increased the expression level of cleaved caspase-3 and the ratio of Bax/Bcl-2.

In Vivo

Sacubitril/Valsartan (LCZ696; perorally; 68 mg/kg for 4 weeks) significantly exhibits small weights and reduces interstitial fibrosis both in the noninfarct zone and peri-infarct zone^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Adult 6- to 8-week-old male Sprague-Dawley rats (220-250 g body weight) ^[2]
Dosage:

68 mg/kg
Administration:

Perorally; for 4 weeks
Result:

Exhibited small weights and reduced interstitial fibrosis both in the noninfarct zone and peri-infarct zone.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 936623-90-4
Appearance Solid
Molecular Weight 957.99
Formel C₄₈H₅₅N₆Na₃O₈.2.5H₂O
Color White to light yellow
SMILES

O=C(CCC(O[Na])=O)N([C@H](CC(C=C1)=CC=C1C2=CC=CC=C2)C[C@@H](C)C(OCC)=O)[H].O=C(O[Na])[C@@H](N(C(CCCC)=O)CC3=CC=C(C4=CC=CC=C4C5=NN=NN5[Na])C=C3)C(C)C.O
Synonyms

LCZ696
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, sealed storage, away from moisture

* In solvent : -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture)

Publications (10)

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Journal Impact Factor

Eur J Med Chem

Novel pterostilbene derivatives ameliorate heart failure by reducing oxidative stress and inflammation through regulating Nrf2/NF-κB signaling pathway. [Abstract]

2023 Oct 5:258:115602. PMID: 37406380
Front Pharmacol

Lcz696 Alleviates Myocardial Fibrosis After Myocardial Infarction Through the sFRP-1/Wnt/β-Catenin Signaling Pathway. [Abstract]

2021 Sep 2;12:724147. PMID: 34539406
Cell Signal

LCZ696 (Sac/Val) protects against high-fat diet-induced kidney injury in mice by targeting ROCK2 to suppress ROCK2/NF-κB signaling. [Abstract]

2026 Aug:144:112536. PMID: 41967621
Acta Cardiol

Sacubitril/valsartan alleviates myocardial infarction-induced inflammation in mice by promoting M2 macrophage polarisation via regulation of PI3K/Akt pathway. [Abstract]

2024 Sep 11:1-10. PMID: 39257342
ESC Heart Fail

The protective effect of LCZ696 in coxsackievirus B3-induced acute viral myocarditis mice. [Abstract]

2023 Feb;10(1):366-376. PMID: 36245336
Exp Biol Med (Maywood)

LCZ696, an angiotensin receptor-neprilysin inhibitor, ameliorates diabetic cardiomyopathy by inhibiting inflammation, oxidative stress and apoptosis. [Abstract]

2019 Sep;244(12):1028-1039. PMID: 31262190
Kaohsiung J Med Sci

Sacubitril/Valsartan Ameliorates Inflammation and Oxidative Stress in Hypertensive Heart Disease by Upregulating CAMKK2 Protein and Modulating the AMPK/AKT/GSK-3β Axis. [Abstract]

2025 Oct 17:e70127. PMID: 41104684
Biochem Biophys Res Commun

Bioinformatics and experimental studies jointly reveal that Sacubitril Valsartan improves myocardial oxidative stress and inflammation by regulating the MAPK signaling pathway to treat chemotherapy related cardiotoxicity. [Abstract]

2024 Jan 1:690:149244. PMID: 38029488
Clin Exp Pharmacol Physiol

Angiotensin receptor-neprilysin inhibitor attenuates cardiac hypertrophy and improves diastolic dysfunction in a mouse model of heart failure with preserved ejection fraction. [Abstract]

2022 Aug;49(8):848-857. PMID: 35596518
Oxid Med Cell Longev

LCZ696 Ameliorates Oxidative Stress and Pressure Overload-Induced Pathological Cardiac Remodeling by Regulating the Sirt3/MnSOD Pathway. [Abstract]

2020 Sep 17;2020:9815039. PMID: 33014281

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : ≥ 100 mg/mL (104.39 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : ≥ 50 mg/mL (52.19 mM)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.0439 mL

5.2193 mL

10.4385 mL

5 mM

0.2088 mL

1.0439 mL

2.0877 mL

10 mM

0.1044 mL

0.5219 mL

1.0439 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (2.61 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (2.61 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (2.61 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

Working Solution

For the following dissolution methods, please prepare the working solution directly:

It is recommended to prepare fresh solutions and use them promptly within a short period of time.

The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: PBS

Solubility: 100 mg/mL (104.39 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Working solution concentration: 0.22 mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact

MedChemExpress (MCE) .

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (288 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Gu J, et al. Pharmacokinetics and pharmacodynamics of LCZ696, a novel dual-acting angiotensin receptor-neprilysin inhibitor (ARNi). J Clin Pharmacol. 2010 Apr;50(4):401-14. [Content Brief]

[2]. von Lueder TG, et al. Angiotensin receptor neprilysin inhibitor LCZ696 attenuates cardiac remodeling and dysfunction after myocardial infarction by reducing cardiac fibrosis and hypertrophy. Circ Heart Fail. 2015 Jan;8(1):71-8. [Content Brief]

[3]. Huo H, et al. Erastin Disrupts Mitochondrial Permeability Transition Pore (mPTP) and Induces Apoptotic Death of Colorectal Cancer Cells. PLoS One. 2016 May 12;11(5):e0154605. [Content Brief]

[4]. Ge Q, et al. Feature article: LCZ696, an angiotensin receptor-neprilysin inhibitor, ameliorates diabeticcardiomyopathy by inhibiting inflammation, oxidative stress and apoptosis. Exp Biol Med (Maywood). 2019 Sep;244(12):1028-1039. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
H₂O / DMSO	1 mM	1.0439 mL	5.2193 mL	10.4385 mL	26.0963 mL
	5 mM	0.2088 mL	1.0439 mL	2.0877 mL	5.2193 mL
	10 mM	0.1044 mL	0.5219 mL	1.0439 mL	2.6096 mL
	15 mM	0.0696 mL	0.3480 mL	0.6959 mL	1.7398 mL
	20 mM	0.0522 mL	0.2610 mL	0.5219 mL	1.3048 mL
	25 mM	0.0418 mL	0.2088 mL	0.4175 mL	1.0439 mL
	30 mM	0.0348 mL	0.1740 mL	0.3480 mL	0.8699 mL
	40 mM	0.0261 mL	0.1305 mL	0.2610 mL	0.6524 mL
	50 mM	0.0209 mL	0.1044 mL	0.2088 mL	0.5219 mL
DMSO	60 mM	0.0174 mL	0.0870 mL	0.1740 mL	0.4349 mL
	80 mM	0.0130 mL	0.0652 mL	0.1305 mL	0.3262 mL
	100 mM	0.0104 mL	0.0522 mL	0.1044 mL	0.2610 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Keywords

Sacubitril/Valsartan

10 Cited Publications

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Publications Citing Use of MedChemExpress (MCE) Sacubitril/Valsartan

Alle Angiotensin Receptor Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (10)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Sacubitril/Valsartan Related Classifications

HY-18204A Related Classifications