Overview PT-141 is the catalog designation for bremelanotide, a synthetic cyclic heptapeptide lactam described in the peer-reviewed literature as a non-selective agonist at the melanocortin receptor family.[1] Molinoff and colleagues published the original characterization of the compound as a melanocortin agonist in Annals of the New York Academy of Sciences.[1] The molecule derives from the melanotropin structure-activity programme conducted at the University of Arizona, reviewed by Hadley and

How does PT-141 work? What is its mechanism of action?

Reported Mechanism 1. Melanocortin Receptor Engagement Bremelanotide is described as a non-selective agonist across the melanocortin receptor family — MC1R, MC3R, MC4R and MC5R — all members of the rhodopsin-like (class A) GPCR superfamily.[1][5] Reported potency is graded rather than subtype-selective, which is the property that makes the compound useful as a broad-spectrum reference ligand and, equally, the property that requires selective antagonists to be co-applied when a single subtype is

What are the research applications of PT-141?

Research Applications Published investigations involving bremelanotide fall into the following areas of laboratory and clinical research. These describe the subject matter of the published record and are not statements of effect. Melanocortin receptor pharmacology — Molinoff et al. published the original characterization of the compound as a melanocortin agonist, and Yuan and Tao reviewed the broader ligand landscape for these receptors.[1][5] MC4R structural biology — Zhang et al. resolved liga

What does the research summary say about PT-141?

Research Summary Foundational and Mechanistic Studies StudyTypeSubject of ReportRef Molinoff et al. (2003)Compound characterizationOriginal description of PT-141 as a melanocortin agonist[1] Van der Ploeg et al. (2002)Receptor genetics / pharmacologyIdentification of an MC4R role in centrally mediated melanocortin pharmacology[3] Hadley & Dorr (2006)Historical reviewMelanocortin peptide development programme and its milestones[2] Zhang et al. (2021)Structural biology (cryo-EM)Ligand recognit

How should PT-141 be stored?

Store lyophilized PT-141 desiccated at -20°C for long-term stability, protected from light. After reconstitution, store at 2-8°C and avoid repeated freeze-thaw cycles.

PT-141: Chemical Properties

24 Citas PubMedRevisado por EspecialistasCertificado GMPÚltima Revisión: julio de 2026

Propiedades Químicas

Molecular Formula	C₅₀H₆₈N₁₄O₁₀
Molecular Weight	1025.2 g/mol
CAS Number	189691-06-3
PubChem CID	9941379
Sequence	Ac-Nle-cyclo[Asp-His-D-Phe-Arg-Trp-Lys]-OH
Structure	Cyclic heptapeptide; lactam bridge between Asp and Lys side chains; D-Phe substitution; N-acetylated norleucine; C-terminal free acid
Parent Molecule	α-MSH analogue; deaminated derivative of Melanotan II
Synonyms	Bremelanotide, PT-141, PT-141 free base
Class	Synthetic cyclic peptide; non-selective melanocortin receptor agonist
Regulatory Status	Research-grade material supplied for laboratory use only; a separate pharmaceutical formulation of bremelanotide holds FDA approval

Identificadores

InChI Key	FFHBJDQSGDNCIV-MFVUMRCOSA-N
Isomeric SMILES	CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)CC2=CN=CN2)CC3=CC=CC=C3)CCCN=C(N)N)CC4=CNC5=CC=CC=C54)C(=O)O)NC(=O)C
Exact Mass	1024.5243 Da (monoisotopic)
Purity Standard	≥98% by RP-HPLC
Identity Confirmation	ESI-MS; amino acid analysis for sequence verification
Detection Methods	RP-HPLC, UHPLC-MS/MS, LC-HRMS/MS

Editorial Research Note

“Research Summary Foundational and Mechanistic Studies StudyTypeSubject of ReportRef Molinoff et al.”

Pure U.S. Peptides Research Standards TeamInternal editorial group summarising published peptide research for an audience of qualified independent investigators.

Referencias

Molinoff PB, Shadiack AM, Earle D, Diamond LE, Quon CY. PT-141: a melanocortin agonist for the treatment of sexual dysfunction. Ann N Y Acad Sci. 2003;994:96-102.
Hadley ME, Dorr RT. Melanocortin peptide therapeutics: historical milestones, clinical studies and commercialization. Peptides. 2006;27(4):921-930.
Van der Ploeg LH, Martin WJ, Howard AD, et al. A role for the melanocortin 4 receptor in sexual function. Proc Natl Acad Sci U S A. 2002;99(17):11381-11386.
Zhang H, Chen LN, Yang D, et al. Structural insights into ligand recognition and activation of the melanocortin-4 receptor. Cell Res. 2021;31(11):1163-1175.
Yuan XC, Tao YX. Ligands for Melanocortin Receptors: Beyond Melanocyte-Stimulating Hormones and Adrenocorticotropin. Biomolecules. 2022;12(10):1407.
Sweeney P, Gimenez LE, Hernandez CC, Cone RD. Targeting the central melanocortin system for the treatment of metabolic disorders. Nat Rev Endocrinol. 2023;19(9):507-519.
Giuliano F. Control of penile erection by the melanocortinergic system: experimental evidences and therapeutic perspectives. J Androl. 2004;25(5):683-691.
Pfaus JG, Shadiack A, Van Soest T, Tse M, Molinoff P. Selective facilitation of sexual solicitation in the female rat by a melanocortin receptor agonist. Proc Natl Acad Sci U S A. 2004;101(27):10201-10204.
Pfaus J, Giuliano F, Gelez H. Bremelanotide: an overview of preclinical CNS effects on female sexual function. J Sex Med. 2007;4 Suppl 4:269-279.
Shadiack AM, Sharma SD, Earle DC, Spana C, Hallam TJ. Melanocortins in the treatment of male and female sexual dysfunction. Curr Top Med Chem. 2007;7(11):1137-1144.
Shadiack AM, Althof S. Preclinical effects of melanocortins in male sexual dysfunction. Int J Impot Res. 2008;20 Suppl 1:S11-S16.
Pfaus JG, Sadiq A, Spana C, Clayton AH. The neurobiology of bremelanotide for the treatment of hypoactive sexual desire disorder in premenopausal women. CNS Spectr. 2022;27(3):281-289.
Dhillon S, Keam SJ. Bremelanotide: First Approval. Drugs. 2019;79(14):1599-1606.
White WB, Myers MG, Jordan R, Lucas J. Usefulness of ambulatory blood pressure monitoring to assess the melanocortin receptor agonist bremelanotide. J Hypertens. 2017;35(4):761-768.
Sauter M, Uhl P, Burhenne J, Haefeli WE. Ultra-sensitive quantification of the therapeutic cyclic peptide bremelanotide utilizing UHPLC-MS/MS for evaluation of its oral plasma pharmacokinetics. J Pharm Biomed Anal. 2020;186:113276.
Yuvaraaj VK, Sharma N. Comprehensive characterization of bremelanotide acetate and its degradants by LC-HRMS/MS and predicting epimerization through computational modelling. Anal Methods. 2026.
Mestria S, Odoardi S, Frison G, Strano Rossi S. LC-HRMS characterization of the skin pigmentation and sexual enhancers melanotan II and bremelanotide sold on the black market of performance and image enhancing drugs. Drug Test Anal. 2021;13(4):876-882.
Suzuki S, Kitanaka C, Okada M. Melanocortin Receptor Agonist Bremelanotide Induces Cell Death and Growth Inhibition in Glioblastoma Cells via Suppression of Survivin Expression. Anticancer Res. 2024;44(9):3875-3883.
Borland JM, Kohut-Jackson AL, Peyla AC, Hall MA, Mermelstein PG, Meisel RL. Female Syrian hamster analyses of bremelanotide, a US FDA approved drug for the treatment of female hypoactive sexual desire disorder. Neuropharmacology. 2025;267:110299.
Merlino F, Jia L, Boccino I, et al. Goldilocks-Inspired Design of Mid-Size Macrocycles for Selective Targeting of Human Melanocortin Receptors. J Med Chem. 2026.
Bardhan M, Anand A, Javed A, et al. Polymorphism of Melanocortin Receptor Genes-Association with Inflammatory Traits and Diseases. Diseases. 2025;13(9):305.
Spielmans GI. Re-Analyzing Phase III Bremelanotide Trials for “Hypoactive Sexual Desire Disorder” in Women. J Sex Res. 2021;58(9):1085-1105.
Expression of Concern: Salvage of Sildenafil Failures With Bremelanotide: A Randomized, Double-Blind, Placebo Controlled Study. J Urol. 2023 Jan 10.
National Center for Biotechnology Information. PubChem Compound Summary for CID 9941379, Bremelanotide. PubChem. Accessed 2026-07-31.

Preguntas de Investigación Relacionadas

→ What Is PT-141?→ PT-141: Mechanism of Action → PT-141: Research Applications → PT-141: Safety Profile & Research Summary → Storing PT-141: Best Practices

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