Enalaprilat Dihydrate

Catalog No.S1657 Synonyms: MK-422 Dihydrate

Enalaprilat Dihydrate Chemical Structure

Molecular Weight(MW): 348.4

Enalaprilat is an angiotensin-converting enzyme (ACE) inhibitor with IC50 of 1.94 nM.

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Description Enalaprilat is an angiotensin-converting enzyme (ACE) inhibitor with IC50 of 1.94 nM.
Features The 1st dicarboxylate-containing ACE inhibitor developed to overcome captopril limitations.
Targets
ACE [1]
1.94 nM
In vitro

Enalaprilat has high affinity for human endothelial ACE with IC50 of 1.94 nM in vitro binding assay by displacing a saturating concentration of [125I]351A, a radiolabeled lisinopril analogue from ACE binding sites, and shows bradykinin/angiotensin I selectivity ratio of 1.00 calculated from double displacement experiments. [1] Enalaprilat has the strong inhibitory effect on Aβ42-to-Aβ40-converting activity found in the N-domain of ACE, exhibiting a 10-fold lower IC50 (0.003~0.01 μM) than captopril (0.03~0.1 μM). [2] Enalaprilat (100 nM) blocks protein kinase C epsilon by directly activating bradykinin B1 receptor at the canonical Zn2+ binding site, leading to prolonged nitric oxide (NO) production in cytokine-treated human lung microvascular endothelial cells. [3] Enalaprilat attenuates the IGF-I induced neonatal rat cardiac fibroblast growth (30% reduction) in a concentration-dependent fashion, with IC50 of 90 mM. [4]

In vivo Enalaprilat has unfavourable ionisation characteristics to allow sufficient potency for oral administration, thus Enalaprilat is only suitable for intravenous administration, which is overcome by the esterification with ethanol to produce Enalapril. Administration of Enalaprilat induces a significant reduction of MAP at 70 minutes compared with the placebo group during haemorrhagic shock in rats, and results in a 50% reduction of CO, a general tendency of EB extravasation which is significant in the kidney and lungs, and a significant increase in ileal EB extravasation (53%). [5] Enalaprilat has no effect in nonhypertrophied hearts, but significantly attenuates the greater increase in left ventricular end-diastolic pressure in hypertrophied hearts compared with no drug. [6]

Protocol

Kinase Assay:[1]
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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.
Cell Research:[4]
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  • Cell lines: Rat cardiac fibroblasts cell lines
  • Concentrations: Dissolved in DMSO, final concentrations 1 nM - 10 μM
  • Incubation Time: 24 hours
  • Method: After 24 hours incubation in serum-free medium (DMEM), cells are stimulated with IGF-I (1-100 nM) and coincubated with Enalaprilat (1 nM-10 μM) for 24 hours. Cellular proliferation is assessed by 5-bromo-2'-deoxyuridine (BrdU) incorporation during the last 4 hours of the 24 hours incubation period using a colorimetric immunoassay. The extinctions are measured at 450 nm in an ELISA plate reader. All values consist of an n=9.
    (Only for Reference)
Animal Research:[5]
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  • Animal Models: Male Sprague–Dawley rats
  • Formulation: Dissolved in a vehicle solution (1 mg in 950 μL of phosphate buffered saline and 50 μL 1M Na2CO3).
  • Dosages: 1 mg/kg
  • Administration: I.V. bolus
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 70 mg/mL (200.91 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 348.4
Formula

C18H24N2O5.2H2O

CAS No. 84680-54-6
Storage powder
in solvent
Synonyms MK-422 Dihydrate

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03051282 Recruiting Drug: Enalapril Healthy Volunteers University of Michigan April 1 2017 Phase 4
NCT02654678 Unknown status Drug: Enalapril Orodispersible Minitablet Heart Failure|Dilated Cardiomyopathy|Congenital Heart Disease Ethicare GmbH March 2016 Phase 2|Phase 3
NCT02652728 Unknown status Drug: Enalapril Orodispersible Minitablet Heart Failure|Dilated Cardiomyopathy Ethicare GmbH January 2016 Phase 2|Phase 3
NCT02652741 Unknown status Drug: Enalapril Orodispersible Minitablet Heart Failure|Congenital Heart Disease Ethicare GmbH January 2016 Phase 2|Phase 3

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID