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Enalapril Maleate RAAS inhibitor

Name: Enalapril Maleate
SKU: S1941
Availability: InStock
Rating: 5 (5 reviews)

Cat.No.S1941

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

Chemical Structure

Molecular Weight: 492.52

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 99.98%

99.98

Related Targets	Adrenergic Receptor Estrogen/progestogen Receptor GPR Androgen Receptor Glucocorticoid Receptor ACE Opioid Receptor THR PGES Aromatase 5-alpha Reductase CCK receptor Mineralocorticoid Receptor GHSR SSTR TSH Receptor GNRH Receptor PGDS
Related Products	Temocapril HCl Delapril Hydrochloride Zofenopril calcium VTP-27999 TFA Temocapril Imidapril HCl

Chemical Information, Storage & Stability

Molecular Weight	492.52	Formula	C₂₀H₂₈N₂O₅.C₄H₄O₄	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	76095-16-4	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	MK-421 Maleate			Smiles	CCOC(=O)C(CCC1=CC=CC=C1)NC(C)C(=O)N2CCCC2C(=O)O.C(=CC(=O)O)C(=O)O

Solubility

In vitro
Batch:

DMSO : 98 mg/mL (198.97 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 17 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	5.000mg/ml (10.15mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	2.500mg/ml (5.08mM)	Taking the 1 mL working solution as an example, add 50 μL of 50 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

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

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

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	ACE ^[1]
In vitro	Enalapril Maleate is rapidly converted by ester hydrolysis to enalaprilat, a potent ACE inhibitor; this compound itself is only a weak ACE inhibitor. It lowers peripheral vascular resistance without causing an increase in heart rate. ^[1]
In vivo	Enalapril Maleate treatment abolishes the deleterious effects of eNOS deficiency on blood pressure (BP), atherosclerosis, and kidney dysfunction in nnee mice. ^[2] This compound causes a dose-dependent increase in fore limb strength in the mdx mouse. It causes a dose-dependent reduction of superoxide anion production in tibialis anterior muscle of the mdx mouse as observed by dihydroethidium staining. This chemical (5 mg/kg) reduces the area of muscle necrosis in both gastrocnemious muscle and diaphragm, without significant effect on non-muscle area. ^[3] It 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. This compound results in increased mesangial cell proliferation, matrix expansion and enlarged mesangial area in the kidney of the diabetic rats. It 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]
References	[1] https://pubmed.ncbi.nlm.nih.gov/2982541/ [2] https://pubmed.ncbi.nlm.nih.gov/10683374/ [3] https://pubmed.ncbi.nlm.nih.gov/21689754/ [4] https://pubmed.ncbi.nlm.nih.gov/12379508/

Clinical Trial Information

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

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

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