PT-141 10 mg

PT-141 (also written PT 141, and referenced in research literature as bremelanotide) is a synthetic cyclic heptapeptide research compound classified as a melanocortin-receptor agonist. It is supplied as an investigational laboratory peptide for use in central-nervous-system receptor pharmacology research, melanocortin-receptor signaling research, and GPCR structure-activity studies on MC4R and MC3R receptor engagement.

PT-141 is investigated in laboratory research studies as a probe compound for MC4R and MC3R receptor pharmacology research. Structural modifications relative to its parent melanotan-II scaffold reduce melanocortin-1-receptor (MC1R) binding while retaining MC4R and MC3R receptor engagement, which has positioned PT-141 as a research tool for selectivity studies across the melanocortin-receptor family (Molinoff et al., 2003, Annals of the New York Academy of Sciences).

Beyond receptor selectivity research, PT-141 has been investigated in cellular research models examining cAMP signaling, GPCR receptor pharmacology, and downstream MAPK and PKA cascades following MC4R engagement. Recent research has characterized the molecule's interaction with melanocortin-receptor signaling pathways in additional laboratory models (Marchese et al., 2024, Anticancer Research).

The peptide is supplied as a lyophilized powder to ensure optimal stability during storage and handling.

The melanocortin-receptor family is a group of five class A G-protein-coupled receptors (MC1R through MC5R) that engage the endogenous melanocortin peptides derived from proopiomelanocortin (POMC). Each receptor subtype exhibits a distinct tissue-distribution and pharmacology profile, making the melanocortin-receptor family a frequent subject of GPCR pharmacology research and structure-activity research.

PT-141 was engineered as a structural analog of melanotan-II, a cyclic heptapeptide research compound that engages MC1R, MC3R, MC4R, and MC5R. By introducing modifications to the melanotan-II scaffold, PT-141 was designed to reduce MC1R receptor binding affinity while retaining engagement at MC4R and MC3R, two receptor subtypes that are widely expressed across central-nervous-system research tissues.

This receptor-selectivity profile has made PT-141 a research compound of interest for laboratory investigations of MC4R and MC3R receptor pharmacology research, downstream cAMP signaling research, and comparative GPCR pharmacology across the melanocortin-receptor family.

1. MC4R and MC3R Receptor Engagement

PT-141 engages MC4R and MC3R, two melanocortin-receptor subtypes that belong to the class A G-protein-coupled receptor (GPCR) family. Laboratory research studies indicate that PT-141 binds these receptors with nanomolar affinity in cellular research models, with preferential engagement at MC4R relative to MC1R (Molinoff et al., 2003).

2. Modulation of Cyclic AMP Signaling

Upon receptor binding, PT-141 engages Gαs-coupled signaling at MC4R and MC3R. Adenylyl cyclase activation produces intracellular cyclic AMP accumulation, which is investigated as the primary second-messenger output in melanocortin-receptor signaling research. Downstream, cAMP accumulation modulates protein kinase A (PKA) activity, a frequent subject of GPCR pharmacology research in cellular research models.

3. Receptor-Selectivity Profile

Structure-activity research has characterized PT-141 as engaging MC4R and MC3R while exhibiting reduced binding affinity at MC1R compared with its parent melanotan-II scaffold. This selectivity profile has positioned PT-141 as a research tool for laboratory investigations of MC4R-specific signaling research and comparative pharmacology across the melanocortin-receptor family.

4. Downstream Signaling Cascades

Laboratory research studies have characterized melanocortin-receptor activation as modulating downstream signaling cascades including PKA, EPAC, and MAPK research pathways in cellular research models. PT-141 is investigated as a probe compound for examining these downstream signaling networks following MC4R and MC3R engagement (Marchese et al., 2024).

Research Applications

Conclusion

PT-141 represents a synthetic cyclic heptapeptide research compound engineered for selective engagement of MC4R and MC3R within the melanocortin-receptor family. Its receptor-selectivity profile, defined cyclic heptapeptide architecture, and characterized cAMP signaling output make it a valuable investigational laboratory peptide for studies of melanocortin-receptor pharmacology research and class A GPCR signaling research models.

Research Use Disclaimer

This product is intended for research and laboratory use only. It is designed exclusively for in vitro research purposes. All information provided is for educational and research reference only. This product is not intended for human or animal use. It is not a drug, food, or cosmetic and must not be marketed, labeled, or used as such. Use and handling are restricted to trained and qualified professionals.