PT-141 (Bremelanotide) Peptide

Chemical diagram for PT-141 (Bremelanotide) by Vaccinationist – Own work using: PubChem, Public Domain, https://commons.wikimedia.org/w/index.php?curid=53052077

KEY SPECIFICATIONS

PRODUCT OVERVIEW

PT-141 (Bremelanotide) is a synthetic cyclic heptapeptide and selective agonist of melanocortin receptors MC3R and MC4R. Originally derived from Melanotan II research, PT-141 was structurally optimized to minimize MC1R activation (tanning effects) while preserving central nervous system signaling through MC3R/MC4R.

This compound enables investigation of hypothalamic and limbic brain pathways distinct from peripheral vascular mechanisms. BIONIX supplies research-grade PT-141 with ≥99% purity and batch-specific analytical documentation for laboratory studies of melanocortin signaling.

MECHANISM OF ACTION

PT-141 binds selectively to melanocortin receptors MC3R and MC4R in the central nervous system, activating neuronal signaling pathways through G-protein coupling and cAMP elevation. This mechanism differs fundamentally from peripheral vascular approaches.

Melanocortin Receptor Selectivity:

Key Distinction: PT-141 demonstrates high selectivity for MC3R/MC4R with minimal MC1R activity—unlike non-selective melanocortin agonists that induce tanning effects.

Signaling Pathway:

PT-141 Binding → MC3R/MC4R Activation → G-protein Coupling → 
cAMP Elevation → Hypothalamic/Limbic Neuronal Activation

Central vs. Peripheral Mechanisms:

This distinction makes PT-141 valuable for investigating central nervous system signaling pathways independent of peripheral vascular mechanisms.

RESEARCH APPLICATIONS

Melanocortin Receptor Studies: Investigation of MC3R/MC4R activation, binding affinity, receptor signaling, and downstream cAMP pathways in neuronal cell cultures and tissue explants.

Behavioral Research: Analysis of central melanocortin pathways in motivation, reward processing, and social interaction models—providing insights into neurobiological foundations of complex behaviors.

Neuroendocrine Research: Examination of hypothalamic melanocortin pathways and interactions with the HPA axis, stress responses, and energy homeostasis mechanisms.

Appetite and Metabolism Studies: Investigation of MC4R-mediated satiety signaling, appetite regulation, and energy balance mechanisms relevant to metabolic disorder research.

Central Signaling Models: Research distinguishing central neuronal mechanisms from peripheral effects—enabling isolation of CNS pathways in physiological response studies.

Comparative Profile:

ANALYTICAL VERIFICATION

BIONIX PT-141 undergoes comprehensive analytical characterization:

• HPLC Analysis: ≥99% purity confirmation via optimized chromatographic separation
• Mass Spectrometry: Molecular weight verification (1025.2 Da) and sequence confirmation
• Peptide Content: Amino acid analysis for accurate quantification
• Endotoxin Testing: Laboratory quality assurance

Physical Characteristics:

DEVELOPMENT STATUS

PT-141 has completed clinical development for specific indications:

• FDA Approval (June 2019): Bremelanotide (Vyleesi®) approved for acquired, generalized hypoactive sexual desire disorder (HSDD) in premenopausal women
• Administration: 1.75 mg subcutaneous injection
• Mechanism: First approved medication targeting central desire pathways
• Research Compound Status: BIONIX PT-141 is intended exclusively for laboratory research, not for therapeutic use, human administration, or clinical applications
• Regulatory Note: WADA prohibited substance

BIONIX PT-141 is supplied for laboratory research purposes only.

FREQUENTLY ENCOUNTERED INQUIRIES

What is PT-141 and how does it function?
PT-141 (Bremelanotide) is a synthetic cyclic heptapeptide and selective MC3R/MC4R agonist. It activates hypothalamic and limbic brain regions through central melanocortin signaling rather than peripheral mechanisms. The compound elevates cAMP levels in MC3R/MC4R-expressing neurons, influencing CNS pathways distinct from vascular approaches.

How does PT-141 differ from PDE5 inhibitors?
PT-141 targets CNS melanocortin receptors (MC3R/MC4R) in the hypothalamus and limbic system, operating through receptor-mediated neuronal signaling. PDE5 inhibitors work peripherally on vascular smooth muscle via nitric oxide/cGMP pathways. This fundamental distinction enables research into central versus peripheral physiological mechanisms.

What distinguishes PT-141 from Melanotan II?
PT-141 was structurally optimized for MC3R/MC4R selectivity with minimal MC1R activity, eliminating pronounced tanning effects associated with Melanotan II. While both are cyclic heptapeptides derived from α-MSH, PT-141’s modifications removed MC1R activation (tanning) while preserving central signaling properties, making it more selective for CNS pathway research.

What are the primary research applications?
Melanocortin receptor binding studies, behavioral research models, neuroendocrine pathway investigation, appetite and energy homeostasis studies, and central signaling mechanism research. All applications limited to controlled laboratory environments.

What storage conditions are required?
Lyophilized powder requires -20°C storage for long-term stability. Post-reconstitution, store at 2-8°C and use within 7 days. For extended storage, prepare aliquots and freeze at -20°C, avoiding repeated freeze-thaw cycles.

Is PT-141 approved for therapeutic use?
Bremelanotide (Vyleesi®) received FDA approval in 2019 for a specific indication. However, BIONIX PT-141 is supplied exclusively for laboratory research. It is not for human use, therapeutic applications, or clinical purposes. WADA prohibited substance.

References

1. Wessells H et al., “Synthetic melanotropic peptide initiates erections in men with psychogenic erectile dysfunction,” Int J Impot Res, 2000;12(4):181-185. PMID: 11079360
2. Diamond LE et al., “An effect on the subjective sexual response in premenopausal women,” J Sex Med, 2006;3(4):628-638. PMID: 16776877
3. Pfaus JG et al., “Selective facilitation of sexual solicitation in the female rat by a melanocortin receptor agonist,” Proc Natl Acad Sci, 2004;101(29):10201-10204. PMID: 15199184