TFLL Pharma · Molecule 08
PT-141
Bremelanotide — Cyclic Melanocortin Heptapeptide
PT-141 (bremelanotide) is a synthetic cyclic melanocortin heptapeptide and the active metabolite of Melanotan II, developed by Palatin Technologies from α-MSH / melanocortin research. It acts centrally at melanocortin-4 receptors (MC4R) rather than on peripheral vasculature. This product is supplied as a lyophilized research-grade peptide for in vitro and preclinical laboratory investigation only.
Identity
| Names |
PT-141 · Bremelanotide |
| Structure |
Ac-Nle-cyclo[Asp-His-D-Phe-Arg-Trp-Lys]-OH (cyclic heptapeptide) |
| Length |
7 amino acids (cyclic heptapeptide) |
| Molecular formula |
C50H68N14O10
|
| Molecular weight |
1025.2 Da |
| Primary target |
MC4R (CNS); receptor order MC1R > MC4R > MC3R |
| Pharmacokinetics |
t½ ≈ 2 h · effect window 4–8 h |
| Origin |
Palatin Technologies · active metabolite of Melanotan II |
Research axes
Graded by evidence strength — established indication vs investigational directions. Not therapeutic claims.
-
◆Established (FDA-approved): sexual desire in premenopausal HSDD — RCT-supported (RECONNECT)
-
◆Central, on-demand modulation of desire independent of the vascular pathway
-
◆Investigational (off-label, limited data): male low libido; erectile dysfunction refractory to PDE5 inhibitors
-
◆Investigational (off-label, limited data): SSRI/antidepressant-associated and selected neurogenic sexual dysfunction
Mechanism at a glance
PT-141 uses a central-first mechanism. MC4R agonism in the paraventricular nucleus drives cAMP/PKA/CREB signaling and increased neuronal excitability; mesolimbic dopamine release (VTA–NAc) contributes the desire/motivation component, with PVN oxytocin co-activation adding bonding/reward signaling. The downstream vascular response is descending and NOS-mediated — independent of the peripheral cGMP pathway used by PDE5 inhibitors.
Key literature: Pfaus et al. (melanocortin arousal pathways) · Clayton et al., RECONNECT Phase-3 program · Safarinejad, 2008 (PDE5-refractory cohort).
Regulatory status
| Intended use (this product) |
Research use only — not for human or animal use |
| FDA |
Approved 21 June 2019 as Vyleesi (bremelanotide, 1.75 mg SC; NDA 210557) for acquired, generalized HSDD in premenopausal women |
| WADA |
Prohibited (S2) |
| Other uses |
Research / off-label |
Handling & Storage
-
◆Packaging: 5 × 10 mg lyophilized powder, sterile glass vials
-
◆Storage: Store at 2–8 °C (refrigerated)
-
◆Solubility: Dissolves readily in bacteriostatic water
-
◆Reconstitution: Best used shortly after preparation for optimal stability
-
◆Purity: HPLC-verified ≥ 98% · batch CoA
Research Quality & Scientific Integrity
◆ Purity
HPLC-verified ≥ 98% with batch CoA |
◆ Evidence
Peer-reviewed citations for all mechanistic claims |
◆ Transparency
Evidence limitations stated per molecule |
◆ Safety
Research use only — not for human or animal consumption |
For Research Use Only. This product is strictly intended for laboratory and research use only. Not suitable for human or animal consumption, diagnostic, or therapeutic use. All use must comply with local regulations and ethical research standards.
PT-141 (Vyleesi) is FDA-approved for acquired generalized HSDD in premenopausal women only. All other uses are for research purposes exclusively.
TFLL Pharma · TFLL BV · Belgium · Life Span · Health Span · Brain Span · www.tfllpharma.com
