2. GPCR/G Protein Metabolic Enzyme/Protease Apoptosis
  3. Angiotensin Receptor Neprilysin Apoptosis
  4. Sacubitril/Valsartan

Sacubitril/Valsartan  (Synonyms: LCZ696)

Cat. No.: HY-18204A Purity: 99.99%
COA Handling Instructions

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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.

For research use only. We do not sell to patients.

Sacubitril/Valsartan Chemical Structure

Sacubitril/Valsartan Chemical Structure

CAS No. : 936623-90-4

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Based on 8 publication(s) in Google Scholar

Other Forms of Sacubitril/Valsartan:

Sacubitril/Valsartan Related Antibodies

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Description

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]
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.

Sacubitril/Valsartan Related Antibodies

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
Molecular Weight

957.99

Formula

C48H55N6Na3O8.2.5H2O
CAS No.
Appearance

Solid

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.[2.5H2O]
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

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

Solvent & Solubility
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.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.0439 mL 5.2193 mL 10.4385 mL
5 mM 0.2088 mL 1.0439 mL 2.0877 mL
View the 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.

* 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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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.

  • 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.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • 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.

    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.

  • 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

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: 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).
Purity & Documentation

Purity: 99.99%

COA (265 KB) RP-HPLC (270 KB)

Handling Instructions (2659 KB)
References

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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Sacubitril/Valsartan Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Sacubitril/Valsartan936623-90-4LCZ696LCZ 696LCZ-696Angiotensin ReceptorNeprilysinApoptosisNeutral endopeptidaseNEPCluster of differentiation 10CD10 orallyangiotensinreceptor-neprilysinARNhypertensionheartInhibitorinhibitorinhibit

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