PT-141 (Bremelanotide) cyclic heptapeptide MC3R/MC4R-preferring melanocortin agonist for in vitro receptor research.
Every batch of PT-141 is sent to an accredited independent laboratory before it ships. Here is exactly what we screen for - and the certificate that proves it.
Melanocortin receptor signaling studied across MC3R/MC4R cellular and CNS preclinical models
PT-141 (bremelanotide) is a non-selective melanocortin agonist with preferential potency at MC3R and MC4R over MC1R. Receptor-binding studies in transfected cell lines characterize PT-141 as a high-affinity ligand that produces dose-dependent cAMP accumulation via G-alpha-s-coupled adenylyl cyclase activation.
PT-141 carries the sequence Ac-Nle-cyclo(Asp-His-D-Phe-Arg-Trp-Lys)-OH, with a side-chain lactam bridge between Asp2 and Lys7. The constrained ring locks the conserved His-D-Phe-Arg-Trp melanocortin pharmacophore into an active conformation, and the C-terminal -OH (vs the -NH2 of melanotan II) shifts receptor selectivity within the MCxR family.
Preclinical models implicate MC4R-expressing hypothalamic and limbic circuits in PT-141 central effects. Rodent studies, including those preceded by melanotan II work (Wessells et al., 2000), report MC4R-mediated CNS responses distinct from peripheral vasoactive mechanisms, supporting PT-141 as a research tool for descending melanocortin pathway pharmacology.
Selected findings from peer-reviewed melanocortin receptor and PT-141 publications
Primary areas of PT-141 in vitro and preclinical investigation
PT-141 is widely used as a reference agonist in MC1R/MC3R/MC4R/MC5R binding and cAMP functional assays in transfected HEK293 and CHO cell lines, supporting characterization of new melanocortin ligands and SAR studies.
Diamond et al. 2004 (SAR) ↗PT-141 is used to probe MC4R-mediated signaling in hypothalamic and limbic models, including studies that distinguish MC4R-dependent responses from MC3R contributions using selective antagonists and MC4R knockout models.
King et al. 2007 review ↗Rodent and ex vivo studies use PT-141 to investigate central melanocortin circuits implicated in feeding, arousal, and autonomic regulation, leveraging its blood-brain barrier penetrance reported in early melanotan II / PT-141 work (Wessells et al., 2000).
Wessells et al. 2000 ↗As a constrained heptapeptide derived from alpha-MSH and melanotan II, PT-141 serves as a structural anchor for structure-activity relationship studies comparing linear, cyclic, and small-molecule MC4R ligands.
Mountjoy 2010 melanocortin review ↗Technical specifications and analytical profile
Common questions about PT-141 research parameters
Peer-reviewed publications and clinical studies database