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

Sacubitril/Valsartan (Synonyms: LCZ696)

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

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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10 mM * 1 mL in DMSO USD 105 In-stock
Estimated Time of Arrival: December 31
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10 mg USD 100 In-stock
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50 mg USD 190 In-stock
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Customer Review

Based on 2 publication(s) in Google Scholar

Other Forms of Sacubitril/Valsartan:

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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].

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].

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

C₄₈H₆₀N₆Na₃O₁₀.₅

CAS No.
SMILES

O=C(CCC(O[Na])=O)N([[email protected]](CC(C=C1)=CC=C1C2=CC=CC=C2)C[[email protected]@H](C)C(OCC)=O)[H].O=C(O[Na])[[email protected]@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
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (104.39 mM)

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
10 mM 0.1044 mL 0.5219 mL 1.0439 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 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

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

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

*All of the co-solvents are provided by MCE.
References

Purity: 99.99% ee.: 99.99%

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Keywords:

Sacubitril/ValsartanLCZ696LCZ 696LCZ-696Angiotensin ReceptorNeprilysinApoptosisNeutral endopeptidaseNEPCluster of differentiation 10CD10 orallyangiotensinreceptor-neprilysinARNhypertensionheartInhibitorinhibitorinhibit

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