Trandolapril is a prodrug that is de-esterified to trandolaprilat. It is believed to exert its antihypertensive effect through the renin-angiotensin-aldosterone system.
CAT No: 10-101-125
CAS No:87679-37-6
Synonyms/Alias:RU 44570; (2S,3aR,7aS)-1-[(S)-N-[(S)-1-Carboxy-3-phenylpropyl] alanyl] hexahydro-2-indolinecarboxylic acid 1-ethyl ester
Trandolapril is a synthetic angiotensin-converting enzyme (ACE) inhibitor belonging to the class of pharmaceutical compounds known for modulating the renin-angiotensin-aldosterone system (RAAS). Characterized by its prodrug nature, Trandolapril undergoes biotransformation in vivo to its active metabolite, trandolaprilat, which is responsible for its biological activity. The molecular structure of this compound is engineered to ensure optimal interaction with ACE, leading to the suppression of angiotensin II synthesis. Its unique chemical features, including a bicyclic ring system and ester functional group, confer improved pharmacokinetic properties compared to earlier ACE inhibitors. Due to these attributes, Trandolapril has become a valuable tool in research settings focused on cardiovascular, renal, and metabolic processes.
Cardiovascular research: Trandolapril is widely utilized in experimental models to investigate the mechanisms underlying blood pressure regulation and cardiac remodeling. By inhibiting the conversion of angiotensin I to angiotensin II, it allows researchers to dissect the role of the RAAS pathway in hypertension and heart failure. Studies employing this compound frequently focus on its effects on vascular resistance, endothelial function, and cardiac fibrosis, providing insights into the molecular and physiological changes that occur in various cardiovascular disorders. Its use in in vitro and in vivo systems helps elucidate the downstream signaling events triggered by ACE inhibition, supporting the development of novel therapeutic strategies for cardiovascular health.
Renal function studies: In nephrology research, Trandolapril serves as a critical agent for exploring the impact of RAAS modulation on kidney function. Researchers employ this ACE inhibitor to assess its effects on glomerular hemodynamics, proteinuria, and renal fibrosis in animal models of chronic kidney disease. The compound's ability to attenuate the actions of angiotensin II is instrumental in understanding the progression of renal injury and the potential for renoprotective interventions. Through such studies, scientists can better characterize the molecular pathways involved in renal inflammation, oxidative stress, and extracellular matrix deposition, thereby advancing knowledge in kidney disease pathophysiology.
Metabolic syndrome and diabetes research: The application of Trandolapril extends to investigations of metabolic syndrome and diabetes-related complications. Experimental studies utilize the compound to analyze how ACE inhibition influences insulin sensitivity, lipid metabolism, and glucose homeostasis. By modulating the RAAS pathway, it provides a model for examining the interplay between vascular health and metabolic regulation. Research in this area often focuses on the prevention of endothelial dysfunction and the reduction of oxidative stress, both of which are critical factors in the development of diabetes-associated vascular complications. The insights gained from these studies contribute to a deeper understanding of the metabolic consequences of RAAS dysregulation.
Pharmacological mechanism evaluation: Scientists frequently use Trandolapril as a reference compound in comparative pharmacology to evaluate the efficacy and selectivity of new ACE inhibitors. Its well-characterized mechanism of action and predictable pharmacokinetic profile make it an ideal benchmark in preclinical studies. Researchers can assess the binding affinity, duration of action, and tissue specificity of novel agents relative to this established ACE inhibitor. Such comparative analyses are essential for optimizing the design of next-generation compounds with improved therapeutic potential and reduced side effects.
Vascular biology and endothelial function: The influence of Trandolapril on vascular biology is another important research direction. Investigators employ it to study endothelial cell signaling, nitric oxide production, and the regulation of vascular tone. By inhibiting angiotensin II synthesis, the compound enables the exploration of pathways involved in vasodilation, inflammation, and atherosclerosis development. These investigations are crucial for identifying molecular targets that may be exploited to prevent or mitigate vascular diseases, particularly those associated with aging and metabolic dysfunction. Through its multifaceted applications, Trandolapril continues to play a pivotal role in advancing scientific understanding across cardiovascular, renal, and metabolic research domains.
Trandolapril has a favourable pharmacological profile and an antihypertensive efficacy at least comparable to that of other ACE inhibitors. The pharmacological characteristics of trandolapril allow it to provide good 24-hour control of BP with once-daily administration. Trandolapril has also demonstrated some efficacy in a small number of patients with CHF. In addition, trandolapril provides long term protection against all-cause mortality in patients with LV dysfunction after MI. The results of the Prevention of Events with Angiotensin Converting Enzyme Inhibition (PEACE) study will determine its potential as a cardioprotective agent in patients with coronary artery disease and preserved LV function. Thus, trandolapril represents an effective, well-tolerated and convenient treatment option for patients with mild to moderate hypertension or LV systolic dysfunction after MI.
Trandolapril. An update of its pharmacology and therapeutic use in cardiovascular disorders.
Trandolapril is a well known angiotensin converting enzyme (ACE) inhibitor with many cardiovascular (CV) indications. The objectives of this article are to review the pharmacokinetics and pharmacodynamics properties of trandolapril and to focus on its clinical relevance in cardiovascular medicine. Various populations have been studied in large clinical trials including patients with congestive heart failure (CHF) after an acute myocardial infarction (AMI), diabetics, patients with hypertension (HTN), stable coronary artery disease (CAD) and prevention of proteinuria. Long-term treatment with trandolapril in patients with reduced left ventricular function soon after AMI significantly reduced the risk of overall mortality, mortality from CV causes, sudden death, and the development of severe CHF. Treatment with trandolapril after AMI complicated by left ventricular dysfunction appears to be of considerable importance in patients with diabetes mellitus by saving lives and substantially reducing the risk of progression to severe CHF as well. Moreover, trandolapril reduces progression to proteinuria in high-risk patients. Some of the advantages of trandolapril over other ACE inhibitors are the wide spectrum of patient populations studied, the well established dosage and its proven trough-to-peak effect ratios permitting a safe once-a-day administration.
Diaz, A., & Ducharme, A. (2008). Update on the use of trandolapril in the management of cardiovascular disorders. Vascular health and risk management, 4(6), 1147.
1. Urinary Metabolites Associated with Blood Pressure on a Low-or High-Sodium Die
2. High fat diet and GLP-1 drugs induce pancreatic injury in mice
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