Enalaprilat Dihydrate - CAS 84680-54-6
Catalog number:
84680-54-6
Category:
Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C18H28N2O7
Molecular Weight:
384.42
COA:
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Targets:
Angiotensin-converting Enzyme (ACE)
Description:
Enalaprilat is the active metabolite of enalapril. It is the first dicarboxylate-containing ACE inhibitor.
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Purity:
>98%
MSDS:
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1.Sample Preparation and Extraction in Small Sample Volumes Suitable for Pediatric Clinical Studies: Challenges, Advances, and Experiences of a Bioanalytical HPLC-MS/MS Method Validation Using Enalapril and
Burckhardt BB1, Laeer S1. Int J Anal Chem. 2015;2015:796249. doi: 10.1155/2015/796249. Epub 2015 Mar 19.
In USA and Europe, medicines agencies force the development of child-appropriate medications and intend to increase the availability of information on the pediatric use. This asks for bioanalytical methods which are able to deal with small sample volumes as the trial-related blood lost is very restricted in children. Broadly used HPLC-MS/MS, being able to cope with small volumes, is susceptible to matrix effects. The latter restrains the precise drug quantification through, for example, causing signal suppression. Sophisticated sample preparation and purification utilizing solid-phase extraction was applied to reduce and control matrix effects. A scale-up from vacuum manifold to positive pressure manifold was conducted to meet the demands of high-throughput within a clinical setting. Faced challenges, advances, and experiences in solid-phase extraction are exemplarily presented on the basis of the bioanalytical method development and validation of low-volume samples (50 μL serum).
2.Enalapril stimulates collagen biosynthesis through prolidase-dependent mechanism in cultured fibroblasts.
Szoka L1, Karna E, Morka RP, Palka JA. Naunyn Schmiedebergs Arch Pharmacol. 2015 Jun;388(6):677-83. doi: 10.1007/s00210-015-1114-5. Epub 2015 Mar 17.
The mechanism of a lower incidence of dermatological manifestations in patients treated with enalapril compared to patients treated with other ACE-inhibitors, e.g., captopril, is not known. The finding that prolidase plays an important role in collagen biosynthesis and that some angiotensin-converting enzyme inhibitors affect prolidase activity led us to evaluate its effect on collagen biosynthesis in cultured human skin fibroblasts. Since insulin-like growth factor (IGF-I) and transforming growth factor beta 1 (TGF-β1) are the most potent stimulators of both collagen biosynthesis and prolidase activity, and prolidase is regulated by β1 integrin signaling, the effect of enalapril and enalaprilat on IGF-IR, TGF-β1, and β1 integrin receptor expressions was evaluated. Cells were treated with milimolar concentrations (0.3 and 0.5 mM) of enalapril and enalaprilat for 24 h. The activity of prolidase was determined by colorimetic assay. Collagen biosynthesis was evaluated by radiometric assay.
3.Effect of carboxylesterase 1 c.428G > A single nucleotide variation on the pharmacokinetics of quinapril and enalapril.
Tarkiainen EK1, Tornio A1, Holmberg MT1, Launiainen T1, Neuvonen PJ1, Backman JT1, Niemi M1. Br J Clin Pharmacol. 2015 Nov;80(5):1131-8. doi: 10.1111/bcp.12667. Epub 2015 Jun 11.
AIM: The aim of the present study was to investigate the effects of the carboxylesterase 1 (CES1) c.428G > A (p.G143E, rs71647871) single nucleotide variation (SNV) on the pharmacokinetics of quinapril and enalapril in a prospective genotype panel study in healthy volunteers.
4.Absorption and cleavage of enalapril, a carboxyl ester prodrug, in the rat intestine: in vitro, in situ intestinal perfusion and portal vein cannulation models.
Holenarsipur VK1, Gaud N, Sinha J, Sivaprasad S, Bhutani P, Subramanian M, Singh SP, Arla R, Paruchury S, Sharma T, Marathe P, Mandlekar S. Biopharm Drug Dispos. 2015 Mar 31. doi: 10.1002/bdd.1950. [Epub ahead of print]
In recent years prodrug strategy has been used extensively to improve the pharmacokinetic properties of compounds exhibiting poor bioavailability. Mechanistic understanding of the absorption and the role of intestine and liver in the activation of oral prodrugs is crucial. Enalapril, a carboxyl ester prodrug, is reported to be metabolized by human carboxylesterase-1 (CES1) but not by carboxylesterase-2 (CES2) to its active metabolite enalaprilat. Further, it has been reported that the small intestines of both rat and human contain mainly CES2. The objective of this work was to understand whether enalapril remains unchanged as it is absorbed through the intestine into the portal circulation. This was evaluated using different intestinal preparations, an in situ intestinal perfusion experiment and a portal vein cannulated rat model. No turnover of enalapril was seen with commercial rat intestinal S9 and microsomes, but reasonable turnover was observed with freshly prepared rat intestinal and mucosal homogenate and S9.
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CAS 84680-54-6 Enalaprilat Dihydrate

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