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PT-141 (Bremelanotide) research material
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Sexual Health Research

PT-141 (Bremelanotide)

PT-141, known systematically as Bremelanotide, is a synthetic cyclic heptapeptide and a nonselective agonist of the melanocortin receptor family. Structurally derived from the linear melanocortin agonist Melanotan II, it features an N-terminal acetylated norleucine (Nle) residue and a cyclic lactam bridge formed between an aspartate and lysine side chain, together with a D-phenylalanine substitution at position 4. These modifications produce a conformationally constrained scaffold (formula C₅₀H₆₈N₁₄O₁₀, molecular weight approximately 1,025.17 g/mol, CAS 189691-06-3, PubChem CID 9941379) with enhanced metabolic stability relative to its endogenous melanocortin analogs.

In the preclinical literature, PT-141 is used as a probe of melanocortin receptor signaling, with documented activity across the MC1R, MC3R, MC4R, and MC5R subtypes. Research interest centers on MC4R, which is highly expressed in hypothalamic regions including the medial preoptic area and has been implicated in central neuroendocrine and behavioral signaling in animal models. This item is supplied strictly as a reference material for in vitro and laboratory research use only and is not intended for human or veterinary use.

Identification
  • MaterialPT-141 (Bremelanotide)
  • Research AreaSexual Health
  • PresentationVial
  • Available Sizes10mg
  • CAS Number189691-06-3
  • Molecular FormulaC₅₀H₆₈N₁₄O₁₀
  • Molecular Weight1,025.17 g/mol
  • TypeSynthetic cyclic heptapeptide
  • Receptor / TargetMelanocortin receptor agonist (MC1R, MC3R, MC4R, MC5R)
  • PubChem CID9941379 →
Amino Acid Sequence

Ac-Nle-cyclo[Asp-His-D-Phe-Arg-Trp-Lys]-OH

Analytical Data
  • Purity (HPLC)≥99%
  • Identity (MS)Confirmed to specification
  • TestingAccredited (ISO 17025) third-party laboratory
  • CertificateView COA · Lot 26147004 →
From$39.95

Research use only — not for human or animal consumption. Per-batch documentation is provided with the material.

Key Characteristics
Peptide NamePT-141 (Bremelanotide)
CAS Number189691-06-3
PubChem CID9941379
Molecular FormulaC₅₀H₆₈N₁₄O₁₀
Molecular Weight1,025.17 g/mol
SequenceAc-Nle-cyclo[Asp-His-D-Phe-Arg-Trp-Lys]-OH
Amino Acid Count7 amino acids (cyclic lactam structure)
Molecular TypeSynthetic cyclic heptapeptide
FormLyophilized powder (10mg vial)
Purity≥99% - HPLC and mass spectrometry confirmed
SolubilitySoluble in water; freely soluble in dilute acetic acid
StorageStore lyophilized at -20°C; protect from light and moisture
Research Context
Melanocortin receptor pharmacologyUsed as an agonist probe across the MC1R, MC3R, MC4R, and MC5R receptor subtypes in receptor-binding and functional signaling assays.
MC4R signalingInvestigated for central melanocortin-4 receptor engagement in hypothalamic tissue models and cAMP/second-messenger readouts.
Comparative structure-activity studiesCompared against its linear precursor Melanotan II to examine how cyclization and D-amino acid substitution affect subtype selectivity and stability.
Neuroendocrine researchApplied in animal models exploring melanocortin modulation of central neurotransmitter release, including dopaminergic pathways.
Peptide stability characterizationStudied for the metabolic stability conferred by its constrained cyclic lactam scaffold and N-terminal acetylation.
Research Findings

In published preclinical and clinical research, Bremelanotide has been characterized as a high-affinity, nonselective melanocortin receptor agonist with predominant functional activity at MC1R and MC4R. Animal studies have reported that MC4R activation in the medial preoptic area of the hypothalamus is associated with downstream dopamine release, providing a mechanistic framework for its extensive study within central melanocortin signaling. Its cyclic lactam architecture and D-Phe substitution are consistently reported to improve resistance to enzymatic degradation relative to linear melanocortin peptides.

History

PT-141 was developed as a metabolite-derived analog of the linear melanocortin agonist Melanotan II, engineered into a cyclic heptapeptide to improve receptor engagement and metabolic stability. It became one of the most extensively studied melanocortin receptor agonists across preclinical and clinical research, and under the name Bremelanotide (Vyleesi) received FDA approval in June 2019 for a specific clinical indication in humans, following a large clinical development program.

References
  1. Kingsberg SA, et al. Bremelanotide for the Treatment of Hypoactive Sexual Desire Disorder. Obstet Gynecol. 2019.
  2. Molinoff PB, et al. PT-141: a melanocortin agonist for the treatment of sexual dysfunction. Ann N Y Acad Sci. 2003;994:96-102.
  3. Clayton AH, et al. Safety Profile of Bremelanotide Across the Clinical Development Program. J Womens Health (Larchmt). 2022;31(2):171-182.
  4. Dhillon S, Keam SJ. Bremelanotide: First Approval. Drugs. 2019;79(14):1599-1606.
  5. PubChem Compound Summary, CID 9941379, Bremelanotide. National Center for Biotechnology Information.

View compound profile on NIH PubChem →

Cited literature refers to laboratory and preclinical research. PT-141 (Bremelanotide) is supplied strictly for research use only and is not intended to diagnose, treat, cure, or prevent any disease.

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