Description
Chemical Identity
PT-141 (Bremelanotide) is a synthetic cyclic heptapeptide with the molecular formula C50H68N14O10 and a molecular weight of 1025.18 Da (CAS number 189691-06-3). The amino acid sequence is Ac-Nle-c[Asp-His-D-Phe-Arg-Trp-Lys]-OH, structurally derived from Melanotan-2 but with a free carboxylic acid C-terminus instead of an amide. PT-141 was developed as a selective melanocortin receptor agonist for sexual dysfunction research.
PT-141 has received FDA approval under the brand name Vyleesi for hypoactive sexual desire disorder (HSDD) in premenopausal women, making it the first melanocortin receptor-targeted compound approved for a sexual dysfunction indication.
| Property | Value |
|---|---|
| Molecular Formula | C50H68N14O10 |
| Molecular Weight | 1025.18 Da |
| CAS Number | 189691-06-3 |
| Sequence | Ac-Nle-c[Asp-His-D-Phe-Arg-Trp-Lys]-OH |
| Research Status | FDA-approved (Vyleesi) |
Research Overview
PT-141 has been investigated through the complete clinical development pathway, culminating in FDA approval. The primary mechanism involves selective agonism of melanocortin-4 receptors (MC4R) in the central nervous system, particularly in hypothalamic regions involved in sexual arousal and desire. Unlike phosphodiesterase inhibitors that act peripherally on vascular smooth muscle, PT-141 acts centrally through neuronal pathways to modulate sexual function.
The development of PT-141 from Melanotan-2 illustrates rational drug design, where the melanogenesis-focused parent compound was modified to reduce MC1R-mediated pigmentation effects while preserving MC4R-mediated effects on sexual function.
Key areas of published research include:
- Hypoactive Sexual Desire Disorder: Pivotal Phase 3 trials (RECONNECT studies) demonstrated that PT-141 significantly improved sexual desire, arousal, and associated distress scores compared to placebo in premenopausal women with HSDD, leading to FDA approval in 2019.
- Male Erectile Function: Earlier clinical studies evaluated PT-141 for erectile dysfunction, demonstrating efficacy through a central mechanism distinct from PDE5 inhibitors. The compound showed activity in patients unresponsive to conventional treatments.
- Melanocortin Receptor Pharmacology: PT-141 has been instrumental in characterizing the role of MC4R in sexual function, establishing this receptor as a validated therapeutic target for sexual dysfunction.
PT-141 is FDA-approved as Vyleesi for HSDD in premenopausal women. Research-grade material is available for preclinical studies.
Specifications
All PT-141 supplied by Prescott Bio Canada is manufactured to research-grade standards.
| Specification | Detail |
|---|---|
| Purity | >98% (HPLC) |
| Form | Lyophilized powder |
| Appearance | White to off-white powder |
| Storage (lyophilized) | -20°C, protected from light |
| Storage (reconstituted) | 2-8°C, use within 30 days |
| Solubility | Soluble in bacteriostatic water, sterile water, or normal saline |
Each vial is accompanied by a Certificate of Analysis (COA) documenting purity, identity, and endotoxin testing.
Research Applications
PT-141 is supplied exclusively for in vitro and in vivo laboratory research. Published experimental applications include:
- Melanocortin-4 receptor signaling and sexual function research
- Central nervous system pathways of sexual arousal and desire
- Comparative melanocortin receptor selectivity studies
- Neuroendocrine regulation of reproductive behavior
- Structure-activity relationship studies with melanocortin peptide analogs
Researchers should consult the primary literature and institutional review protocols before designing experiments with PT-141.
Storage and Handling
Lyophilized powder: Store at -20°C in the original sealed vial, protected from light and moisture. Under these conditions, PT-141 maintains stability for up to 24 months.
Reconstituted solution: Reconstitute with bacteriostatic water or sterile water. Store reconstituted PT-141 at 2-8°C and use within 30 days. Avoid repeated freeze-thaw cycles.
Handling precautions: This product is intended for research use only (RUO). Not for human or veterinary diagnostic or therapeutic use. Handle using standard laboratory safety practices including appropriate PPE.