Norleual is an angiotensin (Ang) IV analog, and acts as highly potent HGF/c-MET inhibitor (IC50 = 3 pM) that inhibits HGF-induced MDCK cell proliferation and invasion in vitro. It also is AT4 receptor antagonist, disrupts LTP stabilization. It shows antiangiogenic activity.
CAT No: R1054
CAS No:334994-34-2
Synonyms/Alias:Norleual;334994-34-2;L-Phenylalanine,L-norleucyl-L-tyrosyl-L-leucyl-y(CH2-NH)-L-histidyl-L-prolyl-;(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[2-[[(2S)-2-aminohexanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-4-methylpentyl]amino]-3-(1H-imidazol-5-yl)propanoyl]pyrrolidine-2-carbonyl]amino]-3-phenylpropanoic acid;AKOS025142100;DA-56260;PD080030;G91230;
Norleual is a synthetic peptide analog structurally related to endogenous opioid peptides and melanocortin receptor ligands. Distinguished by its modified amino acid sequence, Norleual functions primarily as a dual antagonist of both the melanocortin-4 receptor (MC4R) and the opioid growth factor receptor (OGFr). Its unique structural attributes and receptor selectivity make it a valuable tool in the investigation of peptide-receptor interactions, signal transduction pathways, and the physiological roles of neuropeptide systems. As a research-use compound, Norleual is widely utilized in studies aiming to dissect the functional implications of melanocortin and opioid signaling in diverse biological contexts.
Receptor Antagonism Studies: Norleual is extensively employed as a selective antagonist in the study of MC4R and OGFr pathways. Its ability to competitively inhibit ligand binding at these receptors enables researchers to delineate the downstream effects of endogenous agonists and to clarify the physiological and biochemical roles of these signaling systems. By blocking receptor activation, Norleual facilitates the investigation of cellular responses, gene expression changes, and second messenger cascades associated with melanocortin and opioid signaling, offering critical insights into neuroendocrine and metabolic regulation.
Peptide Structure-Activity Relationship (SAR) Analysis: The compound's modified peptide backbone serves as a model for structure-activity relationship studies, allowing scientists to evaluate how specific sequence alterations influence receptor binding affinity, selectivity, and functional outcomes. Norleual is frequently used as a reference compound in comparative SAR investigations, supporting the rational design and optimization of novel peptide ligands with tailored pharmacological profiles. Its application in SAR studies advances understanding of the molecular determinants governing peptide-receptor specificity and efficacy.
Neuropeptide Functional Research: As a dual antagonist, Norleual provides a strategic approach for dissecting the physiological functions of endogenous melanocortin and opioid peptides. By selectively blocking these pathways, researchers can observe the effects on neuropeptide-mediated processes such as energy homeostasis, stress response, and neuronal signaling. This functional blockade enables the differentiation of overlapping or compensatory mechanisms within neuropeptide networks, thereby refining models of neural and endocrine regulation.
Pharmacological Profiling: Norleual is instrumental in in vitro and ex vivo pharmacological assays designed to characterize receptor pharmacodynamics and ligand-receptor interactions. Its defined antagonist activity allows for precise modulation of experimental conditions, facilitating the quantification of receptor occupancy, antagonist potency, and competitive binding kinetics. Such pharmacological profiling is essential for validating new assay systems, benchmarking receptor-targeted compounds, and elucidating molecular pharmacology in peptide research.
Peptide-Based Drug Discovery Support: The compound's well-characterized antagonist properties and stability make it a valuable control or reference standard in the early stages of peptide-based drug discovery. Norleual is routinely incorporated into screening platforms to assess the specificity and functional selectivity of novel compounds targeting MC4R or OGFr. Its use in these applications aids in the identification of promising lead candidates and in the development of robust screening methodologies, thereby accelerating progress in the discovery of peptide therapeutics for research purposes.
AngIV analogs such as norleual may also mimic the conformation of the hinge region of HGF. In norleual, the reduced peptide bond increases the rotatability around the 3-4-position, making the molecule more flexible. This may permit norleual to emulate hinge conformations in HGF that are normally induced by tertiary structure (kringles) to facilitate its interaction with the c-Met.
The Angiotensin IV Analog Nle-Tyr-Leu-ψ-(CH2-NH2)3-4-His-Pro-Phe (Norleual) Can Act as a Hepatocyte Growth Factor/c-Met Inhibitor
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