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Sacubitril hemicalcium salt Neprilysin inhibitor

Cat.No.S4426

Sacubitril (AHU-377) hemicalcium salt, a component of the heart failure medicine LCZ696, is a potent inhibitor of neprilysin (neutral endopeptidase, NEP).
Sacubitril hemicalcium salt Neprilysin inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 861.04

Quality Control

Chemical Information, Storage & Stability

Molecular Weight 861.04 Formula

C48H56CaN2O10

Storage (From the date of receipt) 3 years -20°C powder
CAS No. 1369773-39-6 -- Storage of Stock Solutions

Synonyms AHU-377 hemicalcium salt Smiles [Ca++].CCOC(=O)C(C)CC(CC1=CC=C(C=C1)C2=CC=CC=C2)NC(=O)CCC([O-])=O.CCOC(=O)C(C)CC(CC3=CC=C(C=C3)C4=CC=CC=C4)NC(=O)CCC([O-])=O

Solubility

In vitro
Batch:

DMSO : 100 mg/mL ( (116.13 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC50/Ki
NEP [1]
References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05989503 Recruiting
Heart Failure With Reduced Ejection Fraction
Universidade do Porto|Unidade de Investigação e Desenvolvimento Cardiovascular (UnIC)|Rede de Investigação em Saúde
August 4 2023 Phase 4
NCT05870709 Withdrawn
Heart Failure
Novartis Pharmaceuticals|Novartis
May 15 2023 --
NCT05564572 Enrolling by invitation
Heart Failure
Stanford University
September 7 2022 Not Applicable
NCT05194111 Recruiting
Heart Failure|Heart Dysfunction
Virginia Commonwealth University
August 11 2022 Phase 1|Phase 2
NCT05963282 Completed
de Novo Heart Failure
Novartis Pharmaceuticals|Novartis
November 29 2021 --

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