Description
PT-141
Bremelanotide
A synthetic cyclic heptapeptide derived from α-MSH — a melanocortin receptor agonist that acts through the central nervous system, activating hypothalamic MC4R pathways rather than the peripheral vascular route of conventional agents.
A brain-penetrant melanocortin agonist — signaling from the central nervous system, not the vasculature.
| PT-141, known by its clinical name bremelanotide, is a cyclic seven-amino acid peptide derived from α-melanocyte-stimulating hormone (α-MSH) and refined from the earlier compound Melanotan II. Its cyclic lactam architecture and non-standard residues resist enzymatic breakdown and allow passage across the blood–brain barrier, where it engages central melanocortin receptors.
Originating from melanocortin research at the University of Arizona and developed by Palatin Technologies, PT-141 is supplied by Guardian Labs as a research-grade lyophilized powder — HPLC-verified above ninety-nine percent purity and lot-verified for consistent receptor-pharmacology and CNS-signaling data. |
Where PDE5 inhibitors act peripherally on the vascular system, PT-141 works upstream in the brain — a mechanistically distinct, centrally mediated pathway.
|
Four defining features — a central pathway, not a peripheral one.
i
Melanocortin AgonismActs as a non-selective agonist across the melanocortin receptor family (MC1R, MC3R, MC4R, MC5R), with its cyclic structure conferring resistance to enzymatic degradation. |
ii
Central MC4R ActivationBrain-penetrant peptide that activates hypothalamic MC3R and MC4R neurons — the melanocortin subtypes implicated in central arousal and appetite pathways. |
iii
cAMP & DopamineRaises intracellular cAMP in MC4R-expressing cells and increases dopamine release in the medial preoptic area of the hypothalamus in preclinical models. |
iv
Central, Not VascularOperates through central-nervous-system pathways — a mechanism distinct from the peripheral PDE5-inhibitor route of agents such as sildenafil and tadalafil. |
On Selectivity
PT-141 is the more centrally selective derivative of Melanotan II: development at Palatin reduced its peripheral MC1R (melanogenesis) activity while retaining the central MC3R and MC4R activity relevant to arousal-pathway research. This shift toward CNS selectivity is what established PT-141 as a well-characterized melanocortin tool compound.
Primary subjects of investigation — strictly laboratory use.
A.01
Melanocortin PharmacologyStudies of melanocortin receptor binding, agonist activity, and downstream cAMP signaling across the MC1R–MC5R family. |
A.02
Central Arousal PathwaysResearch into MC4R-mediated central nervous system signaling and the hypothalamic circuits governing sexual-function pathways. |
A.03
Receptor SelectivityInvestigating subtype selectivity and the structural basis for central versus peripheral melanocortin activity. |
A.04
Energy BalanceExamining MC4R’s role in appetite and energy homeostasis, a pathway central to obesity and metabolic research models. |
Peer-reviewed literature supporting the research potential of this peptide.
| i. |
A Melanocortin Agonist for Sexual DysfunctionA foundational pharmacology paper characterizing PT-141 as a melanocortin receptor agonist acting on central pathways of sexual function — the reference that framed the compound’s mechanism of action. |
View on PubMed → |
| ii. |
Preclinical CNS Effects on Female FunctionA preclinical review reporting that bremelanotide increases dopamine release in the medial preoptic area and elicits appetitive sexual behavior in rodent models — establishing its centrally mediated profile. |
View on PubMed → |
| iii. |
MC4R cAMP SignalingReceptor-pharmacology work demonstrating that PT-141 binds MC3R and MC4R and drives intracellular cAMP accumulation in MC4R-expressing cell lines — the basis for its use as a reference agonist. |
View on PubMed → |
| iv. |
Clinical Development & Regulatory ReviewThe clinical program supporting bremelanotide’s 2019 regulatory approval for hypoactive sexual desire disorder in premenopausal women — the most rigorous clinical characterization of the compound. |
View on PubMed → |
Certificate of analysis available upon request.
| Chemical Name | PT-141 · Bremelanotide |
| Sequence | Ac-Nle-cyclo[Asp-His-D-Phe-Arg-Trp-Lys]-OH |
| Molecular Formula | C₅₀H₆₈N₁₄O₁₀ |
| Molecular Weight | 1025.18 g/mol |
| CAS Number | 189691-06-3 |
| Receptor Target | Melanocortin MC3R / MC4R (agonist) |
| Format | Lyophilized Powder (Freeze-dried) |
| Vial Size | 10 mg |
| Purity | > 99% (HPLC Verified) |
| Storage | Store at −20°C · Protect from light |
| Reconstitution | Bacteriostatic Water |
All products listed are intended exclusively for laboratory research and development purposes. They are not intended for human consumption, diagnostic, or therapeutic use. Customers must be at least 21 years of age to purchase.
