Sacubitril/Valsartan
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.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.96%
- No. CAS: 936623-90-4
- Fòrmula: C48H55N6Na3O8.2.5H2O
- Peso molecular:957.99
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Almacenamiento:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Sacubitril/Valsartan
More- Eur J Med Chem. 2023 Oct 5:258:115602. [Abstract]
- Front Pharmacol. 2021 Sep 2;12:724147. [Abstract]
- Cell Signal. 2026 Aug:144:112536. [Abstract]
- Acta Cardiol. 2024 Sep;79(7):768-777. [Abstract]
- ESC Heart Fail. 2023 Feb;10(1):366-376. [Abstract]
- Exp Biol Med. 2019 Sep;244(12):1028-1039. [Abstract]
- Kaohsiung J Med Sci. 2025 Oct 17:e70127. [Abstract]
- Biochem Biophys Res Commun. 2024 Jan 1:690:149244. [Abstract]
- Clin Exp Pharmacol Physiol. 2022 Aug;49(8):848-857. [Abstract]
- Oxid Med Cell Longev. 2020 Sep 17:2020:9815039. [Abstract]
Customer Validation & Images
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In Vivo Imaging
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In Vivo Efficacy Study
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Histological Imaging/Staining
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WB
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In Vivo Efficacy Study
Ver todos los productos específicos de isoformas Angiotensin Receptor
More
Actividad biológica
Angiotensin receptor-neprilysin[1]
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.
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Cell Line:HG-treated H9C2 cells
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Concentration:1, 10, or 30 µM
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Incubation Time:0.5 hours
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Result:Inhibited HG-treated H9C2 cells apoptosis.
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Cell Line:HG-treated H9C2 cells
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Concentration:1, 10, or 30 µM
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Incubation Time:0.5 hours
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Result:Increased the expression level of cleaved caspase-3 and the ratio of Bax/Bcl-2.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Adult 6- to 8-week-old male Sprague-Dawley rats (220-250 g body weight) [2]
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Dosage:68 mg/kg
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Administration:Perorally; for 4 weeks
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Result:Exhibited small weights and reduced interstitial fibrosis both in the noninfarct zone and peri-infarct zone.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 936623-90-4
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Appearance Solid
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Peso molecular 957.99
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Fòrmula C48H55N6Na3O8.2.5H2O
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Color White to light yellow
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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
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Synonyms
LCZ696
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
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
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Most Recent
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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
Sacubitril/Valsartan purchased from MedChemExpress. Usage Cited in: Eur J Med Chem. 2023 Oct 5:258:115602. [Abstract]
Representative echocardiograms and analyses of LVEF, LVFS and heart rate in DOX-induced heart failure mice administered LCZ696 (Sacubitril/Valsartan; 60 mg/kg; i.g.; once daily for 4 weeks) as a positive control. The cardiac function indexes LVFS, LVEF and heart rate in DOX group were decreased. However, LCZ696 treatment reversed these changes.
Sacubitril/Valsartan purchased from MedChemExpress. Usage Cited in: Eur J Med Chem. 2023 Oct 5:258:115602. [Abstract]
Serum ALP, ALT, CK, LDH and HBDH levels in DOX-induced heart failure mice administered LCZ696 (Sacubitril/Valsartan; 60 mg/kg; i.g.; once daily for 4 weeks) as a positive control. Serum ALP, ALT, CK, LDH and HBDH levels were significantly higher in mice of DOX group than those in Control group, which were largely reduced by LCZ696 treatment.
Sacubitril/Valsartan purchased from MedChemExpress. Usage Cited in: Eur J Med Chem. 2023 Oct 5:258:115602. [Abstract]
Sirius Red staining and quantification of myocardial fibrosis in DOX-induced heart failure mice administered LCZ696 (Sacubitril/Valsartan; 60 mg/kg; i.g.; once daily for 4 weeks) as a positive control. Myocardial fibrosis was markedly enhanced in heart tissues of the DOX group, which was reversed by LCZ696 treatment.
Sacubitril/Valsartan purchased from MedChemExpress. Usage Cited in: Eur J Med Chem. 2023 Oct 5:258:115602. [Abstract]
Myocardial expression of Nrf2, SOD2, SOD1, NQO1, GPX1, CAT, NF-κB, TNF-α, IL-1β and IL-6 in DOX-induced heart failure mice administered LCZ696 (Sacubitril/Valsartan; 60 mg/kg; i.g.; once daily for 4 weeks) as a positive control. DOX-reduced expression of antioxidant enzymes SOD1, SOD2, NQO1, GPX1, CAT, and oxidative stress regulator Nrf2 were enhanced by LCZ696 treatment.
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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
Sacubitril/Valsartan purchased from MedChemExpress. Usage Cited in: Front Pharmacol. 2021 Sep 2;12:724147. [Abstract]
Quantitative analysis of the heart weight-to-body weight (HW/BW) ratio in myocardial infarction mice administered LCZ696 (Sacubitril/Valsartan; 60 mg/kg; p.o.; once daily for 4 weeks). This ratio in the ARNI group was significantly lower than that in the VAL (valsartan) group. ARNI: Sacubitril/valsartan intervention group.
Sacubitril/Valsartan purchased from MedChemExpress. Usage Cited in: Front Pharmacol. 2021 Sep 2;12:724147. [Abstract]
Serum NT-proBNP concentration in myocardial infarction mice administered LCZ696 (Sacubitril/Valsartan; 60 mg/kg; p.o.; once daily for 4 weeks). LCZ696 reduced the elevated serum NT-proBNP level after myocardial infarction. ARNI: Sacubitril/valsartan intervention group.
Sacubitril/Valsartan purchased from MedChemExpress. Usage Cited in: Front Pharmacol. 2021 Sep 2;12:724147. [Abstract]
Representative 2D echocardiograms, M-mode echocardiograms, pulse-wave Doppler echocardiograms of mitral inflow, and tissue Doppler echocardiograms in myocardial infarction mice administered LCZ696 (Sacubitril/Valsartan; 60 mg/kg; p.o.; once daily for 4 weeks). ARNI: Sacubitril/valsartan intervention group.
Sacubitril/Valsartan purchased from MedChemExpress. Usage Cited in: Front Pharmacol. 2021 Sep 2;12:724147. [Abstract]
Sirius Red and Masson’s trichrome staining of myocardial tissues in myocardial infarction mice administered LCZ696 (Sacubitril/Valsartan; 60 mg/kg; p.o.; once daily for 4 weeks). LCZ696 prevented myocardial collagen deposition to a greater extent than valsartan (VAL). ARNI: Sacubitril/valsartan intervention group.
Sacubitril/Valsartan purchased from MedChemExpress. Usage Cited in: Front Pharmacol. 2021 Sep 2;12:724147. [Abstract]
Immunofluorescence images and quantification of the positive area in myocardial tissues from myocardial infarction mice administered LCZ696 (Sacubitril/Valsartan; 60 mg/kg; p.o.; once daily for 4 weeks). LCZ696 significantly decreased α-SMA expression in the infarct area. ARNI: Sacubitril/valsartan intervention group.
Sacubitril/Valsartan purchased from MedChemExpress. Usage Cited in: Front Pharmacol. 2021 Sep 2;12:724147. [Abstract]
Immunohistochemical staining and quantification of collagen I and collagen III in myocardial tissues from myocardial infarction mice administered LCZ696 (Sacubitril/Valsartan; 60 mg/kg; p.o.; once daily for 4 weeks). LCZ696 decreased collagen I and collagen III expression in and around the infarct area to a greater extent than valsartan (VAL). ARNI: Sacubitril/valsartan intervention group.
Sacubitril/Valsartan purchased from MedChemExpress. Usage Cited in: Front Pharmacol. 2021 Sep 2;12:724147. [Abstract]
TUNEL staining in myocardial tissues from myocardial infarction mice administered LCZ696 (Sacubitril/Valsartan; 60 mg/kg; p.o.; once daily for 4 weeks). LCZ696 markedly reduced the elevated apoptosis rate after myocardial infarction. ARNI: Sacubitril/valsartan intervention group.
Sacubitril/Valsartan purchased from MedChemExpress. Usage Cited in: Front Pharmacol. 2021 Sep 2;12:724147. [Abstract]
Relative mRNA expression of β-catenin, sFRP-1 and Dvl-1 in AngII-stimulated primary mouse myocardial fibroblasts exposed to LCZ696 (Sacubitril/Valsartan; 1-30 μM; LCZ696 pretreatment for 1 h followed by co-incubation with Ang II for 2 days). LCZ696 at 30 μM decreased β-catenin and Dvl-1 expression while increasing sFRP-1 expression.
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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;79(7):768-777. 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
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
Solvente y solubilidad
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.
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- 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.
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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.
Add each solvent one by one: PBS
Solubility: 100 mg/mL (104.39 mM); Clear solution; Need ultrasonic
Please enter the basic information of animal experiments:
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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.
Pureza y Documentación
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Ficha de datos (288 KB)
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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)
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Instrucciones de manejo (2659 KB)
Referencias
[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]
Complete Stock Solution Preparation Table
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.
| 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.
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