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Enalapril Maleate

Catalog No. T6486 CAS 76095-16-4

Synonyms: MK-421 Maleate, Renitec Maleate, Glioten Maleate, MK-421 (maleate), Vasotec Maleate

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

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Enalapril Maleate, CAS 76095-16-4

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Purity: 99.54%

Purity: 99.02%

Purity: 98%

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Chemical Properties

Storage & Solubility Information

Description	Enalapril Maleate (MK-421 Maleate), an angiotensin-converting enzyme (ACE) inhibitor, is utilized in the treatment of hypertension, chronic heart failure , and diabetic nephropathy.
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]
Kinase Assay	Single displacement binding assay: The binding assay is based on the competitive displacement of [125I]351A by Enalaprilat performed on whole endothelial cells. Subconfluent HUVECs in 6-well plates are rinsed with 2 mL binding buffer (140 mM NaCl, 2.7 mM KCl, 1.8 mM CaCl2, 1.03 mM MgCl2, 0.42 mM NaH2PO4, 10 mM HEPES, 2 mM sodium pyruvate and 5 mM glucose, pH 7.4), and the culture medium is replaced with 2.5 mL fresh binding buffer containing 5% fetal bovine serum (FBS). The Enalaprilat (2.5-12.5 μL, 0.1-50 nM) or equivalent volumes of diluent are added to the binding buffer. A saturating amount of [125I]351A (10 μL, typically 106 cpm) is then added to each sample and the plates are incubated at 37 °C for 2 hours in a thermostatic bath. The cells are then rinsed twice with 1.5 mL binding buffer. Finally, the cells are extracted with 0.5 mL NaOH 1 N, incubated for 5 minutes, and the radioactivity is counted with a gamma counter. The ratio of specific [125I]351A bound to total bound activity (B/B0) is calculated, and the inhibitory potency of Enalaprilat expressed as the concentration of ACE inhibitors able to displace 50% of the bound radioligand, i.e. the IC50.

Synonyms	MK-421 Maleate, Renitec Maleate, Glioten Maleate, MK-421 (maleate), Vasotec Maleate
Molecular Weight	492.52
Formula	C20H28N2O5·C4H4O4
CAS No.	76095-16-4

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: 4 mg/mL (8.12 mM)

DMSO: 92 mg/mL (186.8 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

References and Literature

1. Vlasses PH, et al. Clin Pharm,1985, 4(1), 27-40. 2. Knowles JW, et al. J Clin Invest,2000, 105(4), 451-458. 3. Cozzoli A, et al. Pharmacol Res,2011, 64(5), 482-492. 4. Itoh Y, et al. J Endocrinol,2002, 175(1), 233-239.

Related compound libraries

This product is contained In the following compound libraries：

Membrane Protein-targeted Compound Library EMA Approved Drug Library Inhibitor Library Drug Repurposing Compound Library Approved Drug Library Target-Focused Phenotypic Screening Library Anti-Metabolism Disease Compound Library FDA-Approved Drug Library Bioactive Compounds Library Max Pediatric Drug Library

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Keywords

Enalapril Maleate 76095-16-4 Endocrinology/Hormones RAAS Enalapril inhibit Angiotensin-converting Enzyme (ACE) Inhibitor MK 421 Maleate MK-421 Maleate Renitec Maleate Glioten Maleate MK-421 MK-421 (maleate) MK 421 MK421 MK421 Maleate Vasotec Maleate inhibitor

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