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Formula | C18H24N2O5.2H2O |
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Molecular Weight | 348.4 | CAS No. | 84680-54-6 | |
Solubility (25°C)* | In vitro | DMSO | 70 mg/mL (200.91 mM) | |
Water | Insoluble | |||
Ethanol | Insoluble | |||
* <1 mg/ml means slightly soluble or 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. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
Description | Enalaprilat (MK-422) is an angiotensin-converting enzyme (ACE) inhibitor with IC50 of 1.94 nM. | ||
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Targets |
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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] | ||
Features | The 1st dicarboxylate-containing ACE inhibitor developed to overcome captopril limitations. |
Kinase Assay:[1] |
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Cell Assay:[4] |
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Animal Study:[5] |
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Pulmonary midkine inhibition ameliorates sepsis induced lung injury [ J Transl Med, 2021, 19(1):91] | PubMed: 33639987 |
Establishment of a Drug Screening Model for Cardiac Complications of Acute Renal Failure [ Biomolecules, 2021, 11(9)1370] | PubMed: 34572583 |
Functional Study of Carboxylesterase 1 Protein Isoforms. [ Proteomics, 2019, 19(4):e1800288] | PubMed: 30520264 |
A Comprehensive Functional Assessment of Carboxylesterase 1 Nonsynonymous Polymorphisms. [ Drug Metab Dispos, 2017, 45(11):1149-1155] | PubMed: 28838926 |
Sacubitril Is Selectively Activated by Carboxylesterase 1 (CES1) in the Liver and the Activation Is Affected by CES1 Genetic Variation. [ Drug Metab Dispos, 2016, 44(4):554-9] | PubMed: 26817948 |
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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.
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