[CAS NO. 1369773-39-6] Sacubitrilhemicalciumsalt

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PRODUCTS SPECIFICATIONS [1369773-39-6]

Catalog

HY-15407A

Brand

MCE

CAS

1369773-39-6

DESCRIPTION [1369773-39-6]

Overview

MDL	MFCD28137893
Molecular Weight	430.52
Molecular Formula	C24H28Ca0.5NO5
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.[0.5Ca2+]

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 hemicalcium salt (AHU-377 hemicalcium salt) is a potent NEP inhibitor with an IC ₅₀ of 5 nM. Sacubitril hemicalcium salt is a component of the heart failure medicine LCZ696.

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 hemicalcium salt, 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 hemicalcium salt, 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 humans, Sacubitril (AHU-377)(t _max 0.5-1.1 h) are absorbed quickly. Sacubitril hemicalcium salt is converted rapidly into LBQ657 with its t _max being reached in 1.9-3.5 h. Mean t _1/2 values for the biologically active LBQ657 is 9.9-11.1 h ^[2] .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] .

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

Clinical Trial

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

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 : 125 mg/mL ( 290.35 mM ; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.3228 mL	11.6139 mL	23.2277 mL
5 mM	0.4646 mL	2.3228 mL	4.6455 mL
10 mM	0.2323 mL	1.1614 mL	2.3228 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: ≥ 6.25 mg/mL (14.52 mM); Clear solution
2.

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

Solubility: ≥ 6.25 mg/mL (14.52 mM); Clear solution
3.

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

Solubility: ≥ 6.25 mg/mL (14.52 mM); Clear solution

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

References

Synonyms

[1,1′-Biphenyl]-4-pentanoic acid, γ-[(3-carboxy-1-oxopropyl)amino]-α-methyl-, 4-ethyl ester, calcium salt (2:1), (αR,γS)-

Sacubitril hemicalcium salt

Sacubitril hemicalcium