Enalapril Maleate

Catalog No.S1941 Synonyms: MK-421 Maleate

For research use only.

Enalapril (MK-421) Maleate is an angiotensin-converting enzyme (ACE) inhibitor, used in the treatment of hypertension, diabetic nephropathy, and chronic heart failure.

Enalapril Maleate Chemical Structure

CAS No. 76095-16-4

Selleck's Enalapril Maleate has been cited by 2 Publications

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Biological Activity

Description Enalapril (MK-421) Maleate is an angiotensin-converting enzyme (ACE) inhibitor, used in the treatment of hypertension, diabetic nephropathy, and chronic heart failure.
Targets
ACE [1]
In vitro

Enalapril is rapidly converted by ester hydrolysis to enalaprilat, a potent ACE inhibitor; Enalapril itself is only a weak ACE inhibitor. Enalapril lowers peripheral vascular resistance without causing an increase in heart rate. [1]

In vivo Enalapril treatment abolishes the deleterious effects of eNOS deficiency on blood pressure (BP), atherosclerosis, and kidney dysfunction in nnee mice. [2] Enalapril causes a dose-dependent increase in fore limb strength in the mdx mouse. Enalapril causes a dose-dependent reduction of superoxide anion production in tibialis anterior muscle of the mdx mouse as observed by dihydroethidium staining. Enalapril (5 mg/kg) reduces the area of muscle necrosis in both gastrocnemious muscle and diaphragm, without significant effect on non-muscle area. [3] Enalapril Maleate results in significant increases in kidney weight and in concentrations of urinary albumin, N-acetyl-fl-d-glucosamidase (NAG) and serum ET-1 in streptozotocin (STZ)-induced diabetic (STZ-DM) rats as compared with the non-diabetic rats, and the concentration of ET-1 in the kidneys tended to be increased. Enalapril Maleate results in increased mesangial cell proliferation, matrix expansion and enlarged mesangial area in the kidney of the diabetic rats. Enalapril Maleate reduces increased concentrations of urinary albumin and NAG in the STZ-DM rats to the control values with a slight improvement in the electron microscopic changes.[4]

Protocol (from reference)

Solubility (25°C)

In vitro

DMSO 99 mg/mL
(201.0 mM)
Ethanol 4 mg/mL
(8.12 mM)
Water Insoluble

Chemical Information

Molecular Weight 492.52
Formula

C20H28N2O5.C4H4O4

CAS No. 76095-16-4
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CCOC(=O)C(CCC1=CC=CC=C1)NC(C)C(=O)N2CCCC2C(=O)O.C(=CC(=O)O)C(=O)O

In vivo Formulation Calculator (Clear solution)

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

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% 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.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04736329 Recruiting Drug: Telmisartan Heart Failure With Reduced Ejection Fraction|Renal Insufficiency Cairo University February 1 2021 Not Applicable
NCT03265574 Recruiting Drug: Enalapril Breast Cancer|Non Hodgkin Lymphoma South Tees Hospitals NHS Foundation Trust|Newcastle University|University of Durham|Newcastle-upon-Tyne Hospitals NHS Trust September 1 2017 Phase 3
NCT03051282 Suspended Drug: Enalapril Healthy Volunteers University of Michigan April 1 2017 Phase 4
NCT03460366 Recruiting Drug: Enalapril Obesity Morbid Norwegian University of Science and Technology|St. Olavs Hospital|Volvat Medisinsk Senter Stokkan|Namsos Hospital|Alesund Hospital November 2 2016 --
NCT02654678 Unknown status Drug: Enalapril Orodispersible Minitablet Heart Failure|Dilated Cardiomyopathy|Congenital Heart Disease Ethicare GmbH March 2016 Phase 2|Phase 3

(data from https://clinicaltrials.gov, updated on 2022-01-17)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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