Perindopril Erbumine is the stable form of perindopril, which is a long-acting ACE inhibitor used to treat high blood pressure, heart failure, or stable coronary artery disease.
CAT No: 10-101-120
CAS No:82834-16-0 (net), 107133-36-8 (erbumine)
Synonyms/Alias:S-9490-3; McN-A-2833-109; [(S)-1-Ethoxycarbonylbutyl]-Ala-Oic-OH t-butyl-amine salt; (2S,3aS,7aS)-1-[(2S)-2-[[(1S)-1-(Ethoxycarbonyl)butyl]amino]-1- oxopropyl]octahydro-1H-indole-2-carboxylic acid tert-butylammonium salt
Perindopril Erbumine is a synthetic, non-peptide compound classified as an angiotensin-converting enzyme (ACE) inhibitor, widely recognized for its ability to modulate the renin-angiotensin system in biochemical and pharmacological research settings. As the erbumine salt of perindopril, it offers enhanced solubility and stability, making it highly suitable for controlled laboratory investigations. Its mechanism of action centers on the inhibition of ACE, resulting in reduced conversion of angiotensin I to the potent vasoconstrictor angiotensin II, a pathway that is pivotal in the regulation of vascular tone and fluid balance. The compound's well-characterized biochemistry and reliable performance in in vitro assays have established it as a valuable tool for exploring cardiovascular, renal, and metabolic processes at the molecular and cellular level.
Enzyme inhibition assays: Perindopril Erbumine is extensively utilized in enzyme kinetics studies to characterize the inhibition of angiotensin-converting enzyme. Researchers employ it as a reference inhibitor to validate assay platforms, quantify ACE activity in biological samples, and investigate structure-activity relationships of ACE and related peptidases. Its use supports the development of robust methodologies for screening novel ACE modulators and for dissecting the molecular determinants of enzyme selectivity and potency.
Signal transduction research: The compound plays a crucial role in elucidating the downstream effects of ACE inhibition within signaling cascades that govern vascular homeostasis. By blocking the formation of angiotensin II, it enables detailed studies on the modulation of intracellular pathways such as MAPK, PI3K/Akt, and calcium signaling in endothelial and smooth muscle cells. These investigations provide insights into the cellular mechanisms underlying vascular remodeling, oxidative stress responses, and nitric oxide bioavailability.
Cardiovascular physiology models: In preclinical research, Perindopril Erbumine is employed to simulate the effects of ACE inhibition in ex vivo and in vitro models of cardiac and vascular tissue. Its application facilitates the study of hemodynamic parameters, vascular compliance, and myocardial contractility under controlled experimental conditions. Scientists leverage its well-defined activity profile to probe the interplay between neurohormonal regulation and cardiovascular function, advancing the understanding of pathophysiological states such as hypertension and heart failure at the mechanistic level.
Renal function and nephrology studies: The compound serves as a valuable tool for probing the impact of ACE inhibition on renal hemodynamics, glomerular filtration, and tubular transport processes. By modulating angiotensin II levels, it allows researchers to investigate the molecular basis of renal autoregulation, sodium handling, and proteinuria in cell-based and organotypic models. Its use supports the exploration of kidney injury mechanisms, renal fibrosis, and the interplay between systemic and intrarenal renin-angiotensin systems.
Drug interaction and metabolic profiling: Perindopril Erbumine is frequently incorporated into in vitro studies assessing the metabolic fate and interaction potential of ACE inhibitors. Researchers utilize it to evaluate cytochrome P450-mediated biotransformation, transporter interactions, and the generation of active metabolites such as perindoprilat. These investigations inform the design of drug-drug interaction studies, support the optimization of pharmacokinetic models, and contribute to the development of new chemical entities with improved metabolic stability and safety profiles.
The methods of theoretical chemistry have been used to elucidate molecular properties of the antihypertensive, cardiovascular protective and antithrombotic perindopril ((2S,3aS,7aS)-1-[(2S)-2-[[(2S)-1-ethoxy-1-oxopentan-2-yl]amino]propanoyl]-2,3,3a,4,5,6,7,7a-octahydroindole-2-carboxylic acid). The geometries and energies of various neutral and ionized complexes of perindopril erbumine and perindopril l-arginine have been computed using HF/6-31G(d) and Becke3LYP/6-31G(d) methods. The calculations showed that in both, the isolated state and water solution perindopril erbumine exists as a neutral complex. In the gas-phase perindopril l-arginine both neutral and ionic complexes are, at the HF level of theory, almost equally stable. The B3LYP level of theory slightly favors single proton transfer complex perindopril l-arginine (by about 14 kJ mol(-1)). In polar solvents like water, the ionized form of perindopril l-arginine becomes much more favored. According to our calculations l-arginine is bound to perindopril more strongly (by about 25 kJ mol(-1)) than erbumine.
Remko, M. (2009). Molecular structure and stability of perindopril erbumine and perindopril L-arginine complexes. European journal of medicinal chemistry, 44(1), 101-108.
Approximately 25% of US adults have high blood pressure (BP). Selection of effective and safe antihypertensive therapy for these individuals is an important health-care priority. High BP can be treated with a wide range of antihypertensive agents from a number of different classes. These drugs may differ in their suitability for administration to different subpopulations of patients. Results from both clinical trials and postmarketing surveillance indicate that the angiotensin-converting enzyme (ACE) inhibitor perindopril erbumine is safe and well tolerated in a wide range of patients with hypertension. Cough, the most common ACE inhibitor-associated side effect, is also the most common clinical adverse event reported for perindopril, but <2% of perindopril-treated patients discontinue therapy because of cough. Other adverse events often associated with ACE inhibitors, first-dose hypotension and hyperkalemia, appear to occur less often with perindopril than with other agents in this class. The favorable safety profile for perindopril extends to a wide range of patients, including the elderly and those with either heart failure or renal disease. Perindopril has no negative effects on lipids in patients with hyperlipidemia or on glycemic control in patients with type 2 diabetes mellitus, and it reduces proteinuria in patients with renal disease. Perindopril has no known clinically significant drug-drug interactions. Thus, perindopril is a safe BP-lowering agent with documented tolerability in a wide range of patients with hypertension.
Clark, L. T. (2001). Safety profile of perindopril. The American journal of cardiology, 88(7), 36-40.
The present study was performed to compare the bioavailability of two perindopril erbumine (CAS 107133-36-8) 4 mg tablet formulations (test formulation and reference formulation). This study was a randomized, single-blind, two-period, two-sequence cross-over study which included 20 healthy adult male and female subjects under fasting conditions. In this study, one subject withdrew from the study and one reserve subject did not appear at both periods. The pharmacokinetic parameters were assessed based on the concentrations of perindopril (CAS 82834-16-0) and perindoprilat (CAS 95153-31-4) because perindopril has litte pharmacologic activity until hydrolized in the liver into its active metabolite, perindoprilat.
Setiawati, E., Deniati, S. H., Yunaidi, D. A., Handayani, L. R., Santoso, I. D., Arland, J. A., ... & Lian, L. Y. (2011). Bioequivalence study of two perindopril erbumine tablet formulations in healthy volunteers. Arzneimittelforschung, 61(04), 234-238.
1. Cell-based adhesion assays for isolation of snake venom’s integrin antagonists
2. An Open-label, Single-center, Safety and Efficacy Study of Eyelash Polygrowth Factor Serum
5. Emu oil in combination with other active ingredients for treating skin imperfections
If you have any peptide synthesis requirement in mind, please do not hesitate to contact us at . We will endeavor to provide highly satisfying products and services.
Creative Peptides is a trusted CDMO partner specializing in high-quality peptide synthesis, conjugation, and manufacturing under strict cGMP compliance. With advanced technology platforms and a team of experienced scientists, we deliver tailored peptide solutions to support drug discovery, clinical development, and cosmetic innovation worldwide.
From custom peptide synthesis to complex peptide-drug conjugates, we provide flexible, end-to-end services designed to accelerate timelines and ensure regulatory excellence. Our commitment to quality, reliability, and innovation has made us a preferred partner across the pharmaceutical, biotechnology, and personal care industries.
Read More