PL-3994, an exquisitely tailored receptor antagonist exhibiting formidable potency, has been ingeniously formulated to combat the intricacies of heart failure. By establishing an exceptional binding affinity to angiotensin II receptors, this remarkable compound exerts a formidable inhibitory effect on the deleterious consequences instigated by angiotensin II.
CAT No: R2048
CAS No:952295-80-6
Chemical Name:2-[(4R,7S,10S,13S,16S,19R,22S,28R,31S,34S,37S)-31-benzyl-10-[(2S)-butan-2-yl]-19-butyl-13,22-bis(3-carbamimidamidopropyl)-4-[[(2S)-1-[(2S,5R)-2-(3-carbamimidamidopropyl)-5-carbamoyl-3-oxopiperazin-1-yl]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]carbamoyl]-37-(heptanoylamino)-7-(hydroxymethyl)-34-(1H-imidazol-4-ylmethyl)-28-methyl-6,9,12,15,18,21,24,27,30,33,36-undecaoxo-1,2-dithia-5,8,11,14,17,20,23,26,29,32,35-undecazacyclooctatriacont-16-yl]acetic acid
PL-3994 is a synthetic peptide compound recognized for its potent and selective agonism of natriuretic peptide receptor A (NPR-A), a key receptor involved in the regulation of cardiovascular and renal function. Structurally engineered to mimic the activity of endogenous natriuretic peptides, PL-3994 exhibits enhanced metabolic stability and receptor specificity, making it a valuable molecular tool for investigating natriuretic peptide signaling pathways. Its unique pharmacological profile enables researchers to dissect the physiological roles of natriuretic peptides in various biological systems, particularly in the context of fluid homeostasis, vasodilation, and cellular signaling cascades. As a research-use-only compound, PL-3994 serves as an advanced resource for elucidating the mechanisms underlying peptide-receptor interactions and downstream biological effects.
Receptor Pharmacology Studies: PL-3994 is widely utilized in receptor pharmacology research to characterize the binding affinity, selectivity, and activation dynamics of natriuretic peptide receptors, especially NPR-A. By providing a highly selective agonist, it allows for precise delineation of receptor-mediated signaling events, including the stimulation of cyclic guanosine monophosphate (cGMP) production. Such investigations are critical for understanding the physiological and pathophysiological functions of natriuretic peptide systems in cardiovascular, renal, and endocrine tissues.
Signal Transduction Analysis: Researchers employ PL-3994 to probe intracellular signaling pathways activated by natriuretic peptide receptor engagement. Its ability to robustly stimulate cGMP synthesis makes it an effective tool for dissecting downstream signaling events, such as protein kinase G activation, ion channel modulation, and gene expression regulation. These studies contribute to a deeper understanding of how natriuretic peptides influence cellular responses, tissue remodeling, and homeostatic mechanisms at the molecular level.
Cardiovascular and Renal Physiology Models: In preclinical experimental settings, PL-3994 is applied to in vitro and ex vivo models to investigate the physiological effects of natriuretic peptide receptor activation on vascular tone, sodium excretion, and fluid balance. By mimicking the action of endogenous peptides, it enables controlled studies of vasodilation, natriuresis, and diuresis, supporting research into the mechanisms that govern blood pressure regulation and renal function.
Peptide Structure-Activity Relationship (SAR) Exploration: The synthetic nature and receptor specificity of PL-3994 make it a valuable reference compound in structure-activity relationship studies. Researchers use it as a benchmark to evaluate how modifications in peptide sequence or conformation impact receptor binding, activation potency, and metabolic stability. These insights facilitate the rational design of novel peptide analogs with tailored pharmacological properties for research applications.
Analytical Method Development: PL-3994 also serves as a reference standard in the development and validation of analytical methods for peptide quantification and characterization. Its defined structure and receptor activity profile support the calibration of bioassays, chromatographic techniques, and mass spectrometry protocols aimed at detecting and quantifying natriuretic peptides or related analogs in complex biological samples. This application is essential for ensuring the accuracy and reproducibility of experimental results in peptide research.
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