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Enalaprilat Dihydrate

Catalog No. T6340   CAS 84680-54-6
Synonyms: MK-422, MK-422 Dihydrate

Enalaprilat Dihydrate (MK-422 Dihydrate) (IC50=1.94 nM) is a potent angiotensin-converting enzyme (ACE) inhibitor.

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Enalaprilat Dihydrate Chemical Structure
Enalaprilat Dihydrate, CAS 84680-54-6
Pack Size Availability Price/USD Quantity
25 mg In stock $ 33.00
50 mg In stock $ 47.00
100 mg In stock $ 84.00
200 mg In stock $ 142.00
1 mL * 10 mM (in DMSO) In stock $ 105.00
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Purity: 99.78%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Enalaprilat Dihydrate (MK-422 Dihydrate) (IC50=1.94 nM) is a potent angiotensin-converting enzyme (ACE) inhibitor.
Targets&IC50 ACE: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]
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.
Cell Research 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)
Synonyms MK-422, MK-422 Dihydrate
Molecular Weight 348.4
Formula C18H24N2O5·2H2O
CAS No. 84680-54-6

Storage

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

Solubility Information

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

DMSO: 70 mg/mL (200.91 mM)

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

TargetMolReferences and Literature

1. Ceconi C, et al. Eur J Pharmacol, 2007, 577(1-3), 1-6. 2. Zou K, et al. J Biol Chem, 2009, 284(46), 31914-31920. 3. Stanisavljevic S, et al. J Pharmacol Exp Ther, 2006, 316(3), 1153-1158. 4. van Eickels M, et al. Br J Pharmacol, 2000, 131(8), 1592-1596. 5. Schumacher J, et al. Br J Anaesth, 2006, 96(4), 437-443.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Clinical Compound Library Anti-Cancer Drug Library Anti-Cancer Approved Drug Library ReFRAME Related Library NO PAINS Compound Library Drug Repurposing Compound Library FDA-Approved Drug Library Anti-Hypertension Compound Library Bioactive Compound Library Angiogenesis related Compound Library

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Keywords

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