Home Endocrinology & Hormones RAAS inhibitor - ACE inhibitor Enalapril Maleate For research use only.

Enalapril Maleate

Synonyms: MK-421 Maleate

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

Enalapril Maleate Chemical Structure

CAS No. 76095-16-4

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Enalapril Maleate Related Products

Signaling Pathway

RAAS Signaling Pathways

RAAS Signaling Pathway

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
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
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]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04736329 Completed
Heart Failure With Reduced Ejection Fraction|Renal Insufficiency
Cairo University
 February 1 2021 Not Applicable
NCT03265574 Completed
Breast Cancer|Non Hodgkin Lymphoma
South Tees Hospitals NHS Foundation Trust|Newcastle University|University of Durham|Newcastle-upon-Tyne Hospitals NHS Trust
 October 4 2017 Phase 3
NCT03051282 Active not recruiting
Healthy Volunteers
University of Michigan
 April 1 2017 Phase 4
NCT03460366 Recruiting
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
Heart Failure|Dilated Cardiomyopathy|Congenital Heart Disease
Ethicare GmbH
 March 2016 Phase 2|Phase 3

Chemical Information & Solubility

Molecular Weight 492.52 Formula

C20H28N2O5.C4H4O4
CAS No. 76095-16-4 SDF Download Enalapril Maleate SDF
Smiles CCOC(=O)C(CCC1=CC=CC=C1)NC(C)C(=O)N2CCCC2C(=O)O.C(=CC(=O)O)C(=O)O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 99 mg/mL ( (201.0 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 4 mg/mL

Water : Insoluble


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In vivo
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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.

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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.

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