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[CAS NO. 149709-62-6] Sacubitril

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Catalog:	HY-15407
Brand:	MCE
CAS:	149709-62-6

Overview

MDL	MFCD00920862
Molecular Weight	411.49
Molecular Formula	C24H29NO5
SMILES	O=C(CCC(O)=O)N[C@H](CC1=CC=C(C2=CC=CC=C2)C=C1)C[C@@H](C)C(OCC)=O

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

1 Publications Citing Use of MCE

[1]Theranostics. 2021; 11(18):8797-8812.

Summary

Sacubitril (AHU-377) is a potent and orally active NEP (neprilysin) inhibitor with an IC ₅₀ of 5 nM. Sacubitril is a component of the heart failure medicine LCZ696. Sacubitril can be used for the research of heart failure, hypertension and COVID-19 ^[1] ^[2] ^[3] .

IC50 & Target

IC50: 5 nM (NEP) ^[1]

In Vitro

Sacubitril (AHU-377) is a single molecule that is comprised of molecular moieties of valsartan, an ARB, and Sacubitril (AHU-377), a neprilysin inhibitor (1:1 ratio). Sacubitril (AHU-377) is converted by enzymatic cleavage of the ethyl ester into the active neprilysin inhibiting metabolite LBQ657 ^[2] .
The inactive NEPi precursor, Sacubitril (AHU-377), does not inhibit collagen accumulation in fibroblasts nor cardiac myocyte hypertrophy. In cardiac fibroblasts, the active NEPi LBQ657 had no discernible effects. In contrast, LBQ657 modestly inhibits cardiac myocyte hypertrophy ^[3] .

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

In Vivo

In vehicle-treated dogs, ANF increases urinary sodium excretion from 17.3±3.6 to 199.5±18.4 pequivkglmin. This effect is potentiated significantly in animals which receive Sacubitril (AHU-377). Urinary volume is also potentiated in animals which receive an iv administration of Sacubitril (AHU-377) ^[1] .
In normotensive rats, pretreatment with Sacubitril (3, 10 and 30 mg/kg, PO.) augments ANP-evoked plasma cGMP levels by 2.4, 3.3 and 4.0 fold, respectively (4h AUC compared to vehicle) ^[4] .
Sacubitril (30 and 100 mg/kg, PO) produces a dose-dependent antihypertensive effect in Dahl-SS rats ^[4] .

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

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase
NCT04197050	RenJi Hospital	Myocardial Injury\|Connective Tissue Diseases	February 20, 2020	Phase 4
NCT05164653	WDB Clinical Research Co., Ltd.	Heart Failure	December 27, 2021	Phase 4
NCT05498675	Beijing Friendship Hospital	Sacubitril+Valsartan\|Hypertension\|Obesity	September 1, 2021
NCT00549770	Novartis Pharmaceuticals\|Novartis	Hypertension	September 2007	Phase 2
NCT05580510	Instituto Nacional de Cardiologia Ignacio Chavez\|Boehringer Ingelheim laboratory	Congenital Heart Disease\|Heart Failure\|Heart Failure With Reduced Ejection Fraction	February 6, 2023	Phase 2\|Phase 3
NCT03553303	Oslo University Hospital	Heart Failure, Systolic	October 16, 2018	Phase 4
NCT05508035	John Paul II Hospital, Krakow	Heart Failure With Moderately Reduced Ejection Fraction	September 15, 2022	Phase 3
NCT04753112	Germans Trias i Pujol Hospital	Pulmonary Hypertension	October 29, 2020	Phase 3
NCT04458285	Guangdong Provincial People´s Hospital	Hemodialysis Complication\|Heart Failure	January 1, 2020	Not Applicable
NCT04853758	University of Sao Paulo General Hospital\|InCor Heart Institute	Chagas Cardiomyopathy	May 6, 2021	Phase 3
NCT04149990	Jacob Moller\|Danish Heart Foundation\|Odense University Hospital\|Rigshospitalet, Denmark	Myocardial Infarction\|Diastolic Dysfunction	October 12, 2018	Phase 2
NCT04218435	Clinision	Heart Failure NYHA Class IV\|Heart Failure NYHA Class II	January 1, 2019
NCT04572724	Shenzhen Second People´s Hospital	Peritoneal Dialysis Complication\|Hemodialysis Complication\|Heart Failure	July 6, 2020	Phase 4
NCT02916160	University Hospital, Montpellier	Chronic Heart Failure\|Sleep Apnea Syndrome	September 22, 2016	Phase 4
NCT01281306	Novartis Pharmaceuticals\|Novartis	Systolic Hypertension	January 2011	Phase 2
NCT05117736	Montreal Heart Institute\|Novartis Pharmaceuticals	Systemic Right Ventricle\|Heart Failure	March 15, 2022	Not Applicable
NCT04883528	Duke University\|Novartis Pharmaceuticals	Covid19	August 6, 2021	Phase 1\|Phase 2
NCT03893435	The Young Investigator Group of Cardiovascular Research	Acute Myocardial Infarction	December 1, 2018	Not Applicable

Appearance

Solid

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 : 75 mg/mL ( 182.26 mM ; Need ultrasonic)

H ₂ O : 0.67 mg/mL ( 1.63 mM ; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.4302 mL	12.1510 mL	24.3019 mL
5 mM	0.4860 mL	2.4302 mL	4.8604 mL
10 mM	0.2430 mL	1.2151 mL	2.4302 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 (6.08 mM); Clear solution
2.

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

Solubility: ≥ 2.5 mg/mL (6.08 mM); Clear solution
3.

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

Solubility: ≥ 2.5 mg/mL (6.08 mM); Clear solution

* All of the co-solvents are available by MCE.

References

[1] Ksander GM, et al. Dicarboxylic acid dipeptide neutral endopeptidase inhibitors. J Med Chem. 1995 May 12;38(10):1689-700.
[2] Voors AA, et al. The potential role of valsartan + AHU377 ( LCZ696 ) in the treatment of heart failure. Expert Opin Investig Drugs. 2013 Aug;22(8):1041-7.
[3] 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.
[4] Hegde, L.G., et al. Comparative efficacy of AHU-377, a potent neprilysin inhibitor, in two rat models of volume-dependent hypertension. BMC Pharmacol 11, P33 (2011).

Synonyms

[1,1′-Biphenyl]-4-pentanoic acid, γ-[(3-carboxy-1-oxopropyl)amino]-α-methyl-, α-ethyl ester, (αR,γS)-

[1,1′-Biphenyl]-4-pentanoic acid, γ-[(3-carboxy-1-oxopropyl)amino]-α-methyl-, ethyl ester, [S-(R*,S*)]-

(2R,4S)-5-(Biphenyl-4-yl)-4-[(3-carboxypropionyl)amino]-2-methylpentanoic acid ethyl ester

(2R,4S)-4-[(3-Carboxy-1-oxopropyl)amino]-4-[(p-phenylphenyl)methyl]-2-methylbutanoic acid ethyl ester

Sacubitril

AHU 377

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