PT-141 (Bremelanotide)
PT-141, also known as bremelanotide, is a cyclic heptapeptide studied for its interaction with melanocortin receptors, with particular research interest in the melanocortin-4 receptor (MC4R). Research has focused on its effects on neurological pathways related to behavior and response mechanisms. As a synthetic analog in the alpha-melanocyte-stimulating hormone (alpha-MSH) lineage, it is used as a pharmacological tool for probing melanocortin receptor signaling in laboratory models.
Available Options
Research Context
PT-141 (bremelanotide) is a synthetic cyclic heptapeptide belonging to the melanocortin receptor ligand class. Structurally it is an N-acetylated, lactam-cyclized analog derived from the alpha-melanocyte-stimulating hormone (alpha-MSH) sequence, developed as part of a broader medicinal chemistry effort to produce metabolically stable melanocortin agonists. It acts as a non-selective agonist across melanocortin receptor subtypes, with functional activity reported at MC1R, MC3R, and MC4R; the MC4R, a Gs-coupled G protein-coupled receptor expressed predominantly in the central nervous system, has drawn the most research attention.
In vitro studies have characterized the binding affinity, receptor selectivity, and downstream cAMP signaling profile of bremelanotide and related melanocortin ligands using recombinant receptor expression systems. This body of work has helped map structure-activity relationships within cyclic melanocortin peptides, including how N-terminal acetylation, D-amino acid substitution, and side-chain cyclization influence potency, stability, and receptor subtype preference. More recent in vitro research has examined biased signaling at MC4R, asking whether different ligands preferentially engage distinct intracellular transducers.
Animal model research, primarily in rodents, has used bremelanotide and related agonists to investigate the role of central melanocortin pathways in behavior, autonomic regulation, and neural response mechanisms. These studies have contributed to the broader understanding of MC4R neurobiology, a field in which the receptor is also studied intensively for its role in energy homeostasis. Open questions include the degree of functional selectivity achievable among melanocortin receptor subtypes, the contribution of biased agonism to observed physiological responses, and how peptide modifications translate into altered signaling at the receptor level.
This material is supplied as a lyophilized powder with purity verified by HPLC and a published certificate of analysis. It is intended strictly for laboratory research use and is not for human or veterinary use.
Specifications
| Form | Lyophilized powder |
| Purity | >=99% (HPLC) |
| Sequence | Ac-Nle-cyclo[Asp-His-D-Phe-Arg-Trp-Lys]-OH (2-7 lactam) |
| Molecular formula | C50H68N14O10 |
| Molecular weight | 1025.2 g/mol |
| CAS | 189691-06-3 |
| Storage | Store lyophilized at -20C; refrigerate (2-8C) after reconstitution |
Storage & Handling
Store the lyophilized powder at -20C, protected from light and moisture. After reconstitution, refrigerate at 2-8C and use promptly. For step-by-step handling, see our reconstitution and storage guide and the reconstitution calculator.
Certificate of Analysis
🛡 COA — 10mgRelated Compounds
References
- Sweeney P et al. Targeting the central melanocortin system for the treatment of metabolic disorders. Nat Rev Endocrinol. 2023. PMID 37365323
- Yuan XC, Tao YX. Ligands for Melanocortin Receptors: Beyond Melanocyte-Stimulating Hormones and Adrenocorticotropin. Biomolecules. 2022. PMID 36291616
- Tao YX, Ji RL. Small molecule ligands for the melanocortin-4 receptor: pharmacology, biased signaling, and pharmacoperone potential. Mol Cell Endocrinol. 2026. PMID 42508632