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[CAS NO. 936623-90-4] Sacubitril/Valsartan

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Catalog:	HY-18204A
Brand:	MCE
CAS:	936623-90-4

Overview

MDL	-
Molecular Weight	957.99
Molecular Formula	C48H55N6Na3O8.2.5H2O
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]

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

5 Publications Citing Use of MCE

[1]Oxid Med Cell Longev. 2020 Sep 17;2020:9815039.
[2]ESC Heart Fail. 2022 Oct 17.
[3]Front Pharmacol. 2021 Sep 2;12:724147.
[4]Exp Biol Med (Maywood). 2019 Sep;244(12):1028-1039.
[5]Clin Exp Pharmacol Physiol. 2022 May 20.

Summary

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

NCT Number	Sponsor	Condition	Start Date	Phase
NCT01621633	Novartis Pharmaceuticals\|Novartis	Hepatic Impairment	September 2012	Phase 2
NCT04637555	Novartis Pharmaceuticals\|Novartis	Post Myocardial Infarction	May 26, 2021	Phase 3
NCT03785405	Novartis Pharmaceuticals\|Novartis	Heart Failure	May 2, 2019	Phase 3
NCT03832660	Newcastle University\|Azienda Ospedaliero-Universitaria Careggi\|University Hospital Regensburg\|Institute for Cardiovascular Diseases of Vojvodina\|University of Belgrade	Hypertrophic Cardiomyopathy	May 3, 2019	Phase 2
NCT04023227	Novartis Pharmaceuticals\|Novartis	Chagas Disease\|Heart Failure	December 10, 2019	Phase 4
NCT03119623	Brigham and Women´s Hospital\|Novartis Pharmaceuticals	Heart Failure With Reduced Ejection Fraction	June 1, 2017	Phase 4
NCT02957409	Novartis Pharmaceuticals\|Novartis	Heart Failure	May 20, 2016
NCT03816306	Mohammed Alnims\|Cairo University	Heart Failure With Reduced Ejection Fraction	June 1, 2018
NCT05448872	Novartis Pharmaceuticals\|Novartis	Heart Failure	November 23, 2020
NCT02924727	Novartis Pharmaceuticals\|Novartis	Acute Myocardial Infarction	December 9, 2016	Phase 3
NCT01615198	Novartis Pharmaceuticals\|Novartis	Essential Hypertension	August 2012	Phase 3
NCT03300427	Novartis Pharmaceuticals\|Novartis	Heart Failure	July 5, 2018	Phase 4
NCT03917459	Novartis Pharmaceuticals\|Novartis	Heart Failure\|Heart Failure, Systolic\|Erectile Dysfunction	April 16, 2019	Phase 3
NCT03928158	National Medical Research Center for Cardiology, Ministry of Health of Russian Federation\|Ministry of Health of Russian Federation	Heart Failure\|Essential Hypertension	May 31, 2019	Phase 2
NCT03771729	The Second Affiliated Hospital of Harbin Medical University	CKD	December 30, 2018	Early Phase 1
NCT05168787	Methodist Health System	Heart Failure	August 13, 2020
NCT05387967	National Institute of Cardiovascular Diseases, Karachi	Heart Failure, Systolic	January 1, 2021	Phase 4
NCT01193101	Novartis Pharmaceuticals\|Novartis	Hypertension	August 2010	Phase 2
NCT01681576	Novartis Pharmaceuticals\|Novartis	Salt-sensitive Hypertension	August 2012	Phase 2
NCT03508739	University of Pennsylvania	Diabetes Mellitus, Type 2\|Pre-diabetic\|Hypertension\|Elevated Blood Pressure	June 1, 2018	Phase 3
NCT00913653	Novartis Pharmaceuticals\|Novartis	Heart Failure	May 2009	Phase 2
NCT04342351	RenJi Hospital	Myocardial Infarction	May 1, 2020	Phase 4
NCT01631864	Novartis Pharmaceuticals\|Novartis	Hypertension\|Concurrent Obesity	October 2012	Phase 2
NCT03744975	Mayo Clinic	Diabetes Mellitus, Type 2\|Diastolic Dysfunction	May 1, 2018	Phase 2
NCT03387163	Novartis Pharmaceuticals\|Novartis	Heart Failure, Systolic	February 9, 2018
NCT01646671	Novartis Pharmaceuticals\|Novartis	Severe Hypertension	July 2012	Phase 3
NCT04736433	Brigham and Women´s Hospital	Heart Failure	September 22, 2020
NCT01865188	Novartis Pharmaceuticals\|Novartis	Hypertension	April 2014	Phase 3
NCT04743063	Brigham and Women´s Hospital	Heart Failure, Systolic\|Frailty	January 14, 2021
NCT04397302	Italian Society of Cardiology\|Università degli Studi di Brescia\|Federico II University\|Ospedali Riuniti di Foggia\|University Of Perugia\|Monaldi Hospital\|University of Messina\|University of Siena\|University of Salerno\|Fondazione IRCCS Policlinico San Matteo di Pavia\|Azienda Ospedaliero-Universitaria di Parma\|Azienda Unità Sanitaria Locale di Piacenza	Heart Failure, Left Sided\|Left Ventricular Dysfunction\|Ventricular Remodeling	January 13, 2019
NCT01599104	Novartis Pharmaceuticals\|Novartis	Essential Hypertension	June 2012	Phase 3
NCT01281306	Novartis Pharmaceuticals\|Novartis	Systolic Hypertension	January 2011	Phase 2
NCT01593787	Novartis Pharmaceuticals\|Novartis	Hypertension With Renal Dysfunction	May 2012	Phase 3
NCT04107220	Unity Health Toronto\|Alere, Inc.	Heart Failure	June 2016	Not Applicable
NCT05096143	Novartis Pharmaceuticals\|Novartis	Heart Failure	June 3, 2020
NCT04800081	LanZhou University	Hypertension	July 9, 2020	Not Applicable
NCT01785472	Novartis Pharmaceuticals\|Novartis	Essential Hypertension	April 2013	Phase 3
NCT03760588	Torbjorn Omland\|University Hospital, Akershus\|Oslo University Hospital\|University Hospital of North Norway\|St. Olavs Hospital\|Helse Stavanger HF\|Klinbeforsk\|Norwegian Cancer Society\|Novartis	Breast Cancer Female\|Heart Failure	January 14, 2019	Phase 2
NCT05060588	Qingdao Central Hospital	Myocardial Infarction\|Hypertension	October 2021	Phase 4
NCT01035255	Novartis Pharmaceuticals\|Novartis	Heart Failure With Reduced Ejection Fraction	December 2009	Phase 3
NCT03988634	Novartis Pharmaceuticals\|Novartis	Heart Failure With Preserved Ejection Fraction (HFpEF)	June 27, 2019	Phase 3
NCT02884206	Novartis Pharmaceuticals\|Novartis	Chronic Heart Failure (CHF)	November 23, 2016	Phase 3
NCT01876368	Novartis Pharmaceuticals\|Novartis	Hypertension	September 2013	Phase 3
NCT01870739	Novartis Pharmaceuticals\|Novartis	Hypertension	October 2013	Phase 2
NCT01601470	Novartis Pharmaceuticals\|Novartis	Mild to Moderate Hypertension	September 2012	Phase 2
NCT02874794	Novartis Pharmaceuticals\|Novartis	Heart Failure and Reduced Ejection Fraction	August 17, 2016	Phase 4
NCT03738878	Vanderbilt University Medical Center	Hypertension	November 15, 2018	Phase 4
NCT02788656	Brigham and Women´s Hospital\|Novartis	Congestive Heart Failure	September 2016	Phase 4
NCT05366101	Newcastle-upon-Tyne Hospitals NHS Trust\|University Hospital Regensburg\|Assistance Publique - Hôpitaux de Paris\|Azienda Ospedaliero-Universitaria Careggi\|Institute for Cardiovascular Diseases of Vojvodina	Hypertrophic Cardiomyopathy	April 1, 2019	Phase 2\|Phase 3
NCT05279742	Horng Chen\|Mayo Clinic	Heart Failure With Preserved Ejection Fraction\|Chronic Kidney Diseases	November 2022	Phase 1\|Phase 2
NCT04929600	Shanghai Jiao Tong University School of Medicine	Hypertension\|Left Ventricular Hypertrophy	November 28, 2021	Phase 4
NCT02768298	Novartis Pharmaceuticals\|Novartis	Chronic Heart Failure With Reduced Ejection Fraction	July 12, 2016	Phase 4
NCT01663233	Novartis Pharmaceuticals\|Novartis	Essential Hypertension	August 2012	Phase 3
NCT03552575	NHS Greater Glasgow and Clyde\|University of Glasgow	Heart Failure	July 1, 2018	Phase 3
NCT04113109	Vanderbilt University Medical Center	Heart Failure	November 1, 2019	Phase 4
NCT02687932	Asan Medical Center\|Novartis	Mitral Valve Insufficiency\|Left Ventricular Dysfunction	March 2016	Phase 4
NCT02887183	Novartis Pharmaceuticals\|Novartis	Heart Failure	October 25, 2016	Phase 4
NCT02389933	Novartis Pharmaceuticals\|Novartis	Heart Failure With Reduced Ejection Fraction (HF-rEF)
NCT05613140	Novartis Pharmaceuticals\|Novartis	Chronic Heart Failure	August 2, 2021
NCT04735354	Novartis Pharmaceuticals\|Novartis	Heart Failure	October 27, 2020
NCT05243199	Ruijin Hospital	CKD5 Stage Dialysis\|Heart Failure	August 1, 2020	Phase 4
NCT02661217	Novartis Pharmaceuticals\|Novartis	Heart Failure With Reduced Ejection Fraction	February 12, 2016	Phase 4
NCT02554890	Novartis Pharmaceuticals\|Novartis	Acute Heart Failure	April 29, 2016	Phase 4
NCT05545059	Sun Yat-Sen Memorial Hospital of Sun Yat-Sen University	Resistant Hypertension	September 24, 2022	Phase 3
NCT00887588	Novartis Pharmaceuticals\|Novartis	Chronic Heart Failure	November 2009	Phase 2
NCT01920711	Novartis Pharmaceuticals\|Novartis	Heart Failure With Preserved Ejection Fraction	July 18, 2014	Phase 3
NCT01353508	Novartis Pharmaceuticals\|Novartis	Hypertension	March 2011	Phase 2
NCT04649229	Yale University	Heart Failure	May 27, 2021	Phase 4
NCT02468232	Novartis Pharmaceuticals\|Novartis	Heart Failure With Reduced Ejection Fraction (HF-rEF)	June 15, 2015	Phase 3
NCT01569815	Novartis Pharmaceuticals\|Novartis	Mild and Moderate Renal Impairment	February 2009	Phase 1
NCT03066804	Novartis Pharmaceuticals\|Novartis	Heart Failure With Preserved Ejection Fraction	August 22, 2017	Phase 3
NCT01922089	Novartis Pharmaceuticals\|Novartis	Heart Failure With Reduced Ejection Fraction	November 2013	Phase 2
NCT04164732	Novartis Pharmaceuticals\|Novartis	Cardiomyopathy, Hypertrophic	January 8, 2020	Phase 2
NCT02900378	Novartis Pharmaceuticals\|Novartis	Chronic Heart Failure With Reduced Ejection Fraction	December 20, 2016	Phase 3
NCT02690974	Novartis Pharmaceuticals\|Novartis	Hearth Failure With Reduced Ejection Fraction (HFrEF)	March 8, 2016	Phase 4
NCT01692301	Novartis Pharmaceuticals\|Novartis	Hypertension	December 2012	Phase 2
NCT05096039	Novartis Pharmaceuticals\|Novartis	Heart Failure	April 10, 2020
NCT02678312	Novartis Pharmaceuticals\|Novartis	Pediatric Heart Failure	November 3, 2016	Phase 2\|Phase 3
NCT03909295	Novartis Pharmaceuticals\|Novartis	Heart Failure With Preserved Ejection Fraction (HFpEF)	May 7, 2019	Phase 3
NCT02816736	Duke University\|National Heart, Lung, and Blood Institute (NHLBI)	Heart Failure	March 2, 2017	Phase 4
NCT02226120	Novartis Pharmaceuticals\|Novartis	Chronic Heart Failure With Reduced Ejection Fraction	October 16, 2014	Phase 3
NCT00549770	Novartis Pharmaceuticals\|Novartis	Hypertension	September 2007	Phase 2
NCT01256411	Novartis Pharmaceuticals\|Novartis	Essential Hypertension	November 2010	Phase 2
NCT02970669	Novartis Pharmaceuticals\|Novartis	Heart Failure, Reduced Ejection Fraction	December 16, 2016	Phase 4

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

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

Solvent & Solubility

In Vitro:

DMSO : ≥ 100 mg/mL ( 104.39 mM )

H ₂ O : ≥ 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: PBS

Solubility: 100 mg/mL (104.39 mM); Clear solution; Need ultrasonic
2.

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
3.

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
4.

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 available by MCE.

References

[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.
[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.
[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.
[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.

Synonyms

L-Valine, N-(1-oxopentyl)-N-[[2′-(2H-tetrazol-5-yl)[1,1′-biphenyl]-4-yl]methyl]-, compd. with α-ethyl (αR,γS)-γ-[(3-carboxy-1-oxopropyl)amino]-α-methyl[1,1′-biphenyl]-4-pentanoate, sodium salt, hydrate (2:2:6:5)

LCZ 696

Entresto

Sacubitril-valsartan mixt.

Sacubitril-valsartan

Neparvis

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