
PT-141 (Bremelanotide) is a synthetic cyclic heptapeptide analog of alpha-melanocyte-stimulating hormone (a-MSH), acting as a melanocortin receptor agonist. Unlike PDE5 inhibitors (Viagra, Cialis), PT-141 works via the central nervous system by activating melanocortin receptors in the hypothalamus. It is the first peptide approved for female sexual dysfunction. Each vial contains 10mg of research-grade PT-141.
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About this compound
PT-141 (bremelanotide) is a synthetic cyclic heptapeptide analogue of alpha-MSH, and the active metabolite of Melanotan II. In 2019 it became the world's first FDA-approved drug for hypoactive sexual desire disorder (HSDD) in premenopausal women (Vyleesi™), and the only approved sexual dysfunction therapy to act purely within the central nervous system — via melanocortin receptors (MC3R/MC4R) in the hypothalamus — rather than peripherally via vascular mechanisms like PDE5 inhibitors. This makes it the primary research tool for studying CNS arousal circuits, melanocortin-dopamine cross-talk, and sexual dysfunction neuropharmacology.


Research Data
Research Snapshot — PT-141
Key Mechanisms & Pathways
- MC4R Agonism / PVNActivates melanocortin-4 receptor in the paraventricular nucleus — triggering dopamine release in the NAc and initiating the central arousal cascade.
- MC3R Agonism / ARCMC3R activation in arcuate nucleus initiates sexual motivation circuits and modulates energy homeostasis cross-talk.
- Mesolimbic DopamineD1/D2 receptor-mediated dopamine signalling in the MPOA — the brain region essential for sexual motivation in all mammals.
- Spinal Erection CentresMC4R in thoracolumbar intermediolateral columns activates pro-erectile spinal circuits — effective even in PDE5 non-responders.
- Endogenous OTR ReleaseMC4R activation in PVN directly stimulates oxytocin release from parvocellular neurons — linking melanocortin and OTR systems.
- Serotonin 5-HT2C Cross-TalkReduces inhibitory serotonergic tone on sexual motivation pathways — complementing dopaminergic arousal circuits.
Preclinical & Clinical Research Summary
| Research Area | Key Finding | Source |
|---|---|---|
| FDA Approval (HSDD) | Bremelanotide (Vyleesi) approved June 2019 for premenopausal HSDD — first CNS-acting sexual dysfunction drug. | FDA approval 2019 |
| Phase III Efficacy | RECONNECT trials: significant increase in SSEs and reduced FSDS-DAO distress scores; p<0.001 for both endpoints. | Kingsberg SA et al., 2019 — Obstet Gynecol |
| PDE5 Non-Responders | Produced erections in 17/20 men who had completely failed sildenafil — including severe vascular disease cases. | Shadiack AM et al., 2007 — Ann NY Acad Sci |
| Genital Arousal | Increased vaginal pulse amplitude (objective haemodynamic measure) in both sexually dysfunctional and healthy women. | Pfaus JG et al., 2004 |
References
- Kingsberg SA et al. "Bremelanotide for the Treatment of Hypoactive Sexual Desire Disorder." Obstet Gynecol, 2019;134(5):899–908.
- Simon JA et al. "Bremelanotide: pharmacology and clinical efficacy in female sexual dysfunction." Clin Obstet Gynecol, 2019;62(4):732–743.
- Shadiack AM et al. "Melanocortins in the treatment of male and female sexual dysfunction." Curr Top Med Chem, 2007;7(11):1137–1144.
- Pfaus JG et al. "Who, what, where, when (and maybe even why)? How sexual reward connects desire, preference, and performance." Arch Sex Behav, 2012;41(1):31–62.
Specifications
- Sequence
- Cyclic heptapeptide α-MSH analogue
- Molecular Weight
- 1025.2 Da
- Amino Acids
- 7 (cyclic)
- Half-Life
- ~2.7 hours
- CAS Number
- 189691-06-3
- Vial Size
- 10mg
- Purity
- ≥99% (HPLC)
- Form
- Lyophilized powder
- Reconstitution
- Bacteriostatic water (0.9% benzyl alcohol)
- Storage
- Sealed: 2–8 °C · Reconstituted: 2–8 °C, use within 28 days
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Full mechanism breakdowns and peer-reviewed references for this compound.
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