TC 14012 is an antagonist of CXCR4, which blocks CXCR4-mediated HIV infection with an IC50 value of 19.3 nM. Moreover, TC 14012 (100 µg/ml) inhibits CXCL12-induced phosphorylation of p42/44 MAPK and STAT3 in B cells from patients with chronic lymphocytic leukemia. TC 14012 is also ACKR3 (CXCR7) agonist.
CAT No: R1095
CAS No:368874-34-4
Synonyms/Alias:TC 14012;368874-34-4;TC14012;TC 14012 (trifluoroacetate salt);H-Arg-Arg-2Nal-Cys(1)-Tyr-Cit-Lys-D-Cit-Pro-Tyr-Arg-Cit-Cys(1)-Arg-NH2;TPA87434;DA-67984;G14057;H-Arg-Arg-Nal-Cys-Tyr-Cit-Lys-DCit-Pro-Tyr-Arg-Cit-Cys-Arg-NH2;
TC 14012 is a synthetic peptide compound recognized for its role as a potent and selective agonist of the neuropeptide Y (NPY) Y4 receptor. Structurally engineered to mimic the endogenous ligand pancreatic polypeptide, TC 14012 exhibits high affinity and specificity, making it a valuable research tool for dissecting the physiological and pharmacological functions of Y4 receptor-mediated signaling. Its well-defined sequence and receptor selectivity provide a robust platform for advancing the understanding of peptide-receptor interactions within the broader context of neuroendocrine regulation, energy homeostasis, and gastrointestinal function.
Receptor Pharmacology: TC 14012 is widely utilized in receptor pharmacology studies to elucidate the molecular mechanisms and downstream signaling pathways associated with NPY Y4 receptor activation. By serving as a selective probe, it enables researchers to distinguish Y4-mediated responses from those elicited by other NPY receptor subtypes, thereby facilitating precise characterization of receptor function in both in vitro and ex vivo systems. Its application supports the identification of receptor-specific signaling cascades, contributing to the mapping of neuropeptide-driven regulatory networks.
Peptide Structure-Activity Relationship (SAR) Analysis: The compound is instrumental in structure-activity relationship investigations aimed at optimizing peptide agonists for the Y4 receptor. By providing a reference scaffold, TC 14012 assists researchers in systematically modifying peptide sequences to assess the impact of specific amino acid substitutions on binding affinity, receptor selectivity, and functional efficacy. These SAR studies are critical for guiding the rational design of next-generation peptide ligands with improved pharmacological profiles.
Neuroendocrine Function Research: As a selective Y4 receptor agonist, TC 14012 is employed to probe the physiological roles of Y4 signaling in neuroendocrine systems. Experimental models utilizing this peptide have enabled detailed exploration of its influence on processes such as appetite regulation, gastrointestinal motility, and pancreatic hormone secretion. Through controlled activation of Y4 pathways, researchers can delineate the contributions of this receptor subtype to complex homeostatic mechanisms governing metabolic and digestive functions.
Peptide-Based Assay Development: The high specificity and potency of TC 14012 make it suitable for the development and validation of bioassays targeting Y4 receptor activity. It serves as a positive control or reference agonist in cell-based assays, ligand binding studies, and downstream signaling analyses. The use of this compound in assay development ensures reproducibility and accuracy in quantifying receptor responses, supporting both basic research and high-throughput screening applications aimed at identifying novel modulators of the NPY Y4 receptor.
Peptide Therapeutic Research: In the context of preclinical research, TC 14012 is applied to evaluate the potential of Y4 receptor agonists as leads for peptide-based drug discovery. Its defined pharmacological profile allows for the assessment of efficacy, selectivity, and mechanism of action in experimental models, providing foundational data for the advancement of peptide therapeutics targeting neuropeptide receptors. These studies contribute to the broader effort to harness the therapeutic potential of peptide ligands in modulating neuroendocrine and gastrointestinal pathways.
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