PT-141

Precios por volumen

Precio por envase (10 viales). El descuento se aplica únicamente a este compuesto; no se admiten combinaciones.

PT-141 — Bremelanotide / Central MC3R–MC4R Agonist for Sexual Arousal Research

PT-141, known generically as bremelanotide, is a cyclic lactam heptapeptide derived from Melanotan 2 through structural modification — specifically the hydrolysis of the C-terminal amide and conversion to the carboxylic acid form — that removes the tanning effect while retaining central melanocortin activity. Developed by Palatin Technologies from the MT-2 lineage in the late 1990s and 2000s, PT-141 received FDA approval in June 2019 under the brand name Vyleesi for hypoactive sexual desire disorder (HSDD) in premenopausal women — making it the first approved non-hormonal, centrally acting agent for a sexual dysfunction indication. Its mechanism of action is categorically distinct from phosphodiesterase-5 inhibitors: PT-141 acts centrally via MC3R and MC4R in the hypothalamus, not peripherally on vascular smooth muscle, and does not require sexual stimulation to engage arousal pathways in research models.

Why PT-141’s Central Mechanism Matters

PDE5 inhibitors (sildenafil, tadalafil) amplify nitric oxide-mediated vasodilation in genital tissue but require endogenous arousal signaling to be present — they enhance the vascular response to an existing stimulus. PT-141 operates upstream: MC4R agonism in hypothalamic nuclei, particularly the medial preoptic area and paraventricular nucleus, initiates central arousal signaling independent of peripheral stimulation. This makes PT-141 a research tool for studying the CNS architecture of sexual arousal rather than the vascular response to it. MC3R engagement contributes autoreceptor modulation and energy homeostasis signaling, while the lack of significant MC1R activity (relative to MT-2) eliminates the pigmentation signal that complicates MT-2-based research designs.

Aplicaciones de investigación

PT-141 is used in studies examining:

• Central nervous system sexual arousal pathway architecture via MC4R in hypothalamic nuclei
• Hypoactive sexual desire disorder (HSDD) mechanisms — the approved clinical indication
• Melanocortin receptor pharmacology — MC3R/MC4R selectivity and downstream signaling
• Dopaminergic reward pathway modulation downstream of central melanocortin activation
• Erectile function research — central vs. peripheral mechanism comparisons vs. PDE5 inhibitors
• Melanocortin system involvement in mood, motivation, and stress response biology

Especificaciones

Reconstitución

PT-141 arrives as lyophilized powder and must be reconstituted with bacteriostatic water prior to use. Use the formula:

Total en mg ÷ Volumen añadido (mL) = Concentración (mg/mL)

Ejemplo: vial de 10 mg + 2 ml de agua destilada = solución de 5 mg/ml

El péptido reconstituido debe conservarse a una temperatura de entre 2 y 8 °C y utilizarse en un plazo de 28 a 30 días.

Notas sobre el protocolo

The FDA-approved clinical protocol for Vyleesi provides a precise pharmacokinetic anchor: 1.75mg subcutaneous injection approximately 45 minutes before anticipated activity. Phase II and III clinical trial data report onset at 45 minutes and activity duration of 6–12 hours. Preclinical and earlier human research explored a wider range.

• Dose range: 1.25–1.75mg subcutaneous per administration in Phase II/III clinical trials; 0.3–1.0mg ranges studied in earlier dose-finding research
• Frequency: Single-dose challenge designs standard in clinical research; not more than once per 24 hours in approved clinical use
• Study duration: Acute pharmacodynamic studies typical; multi-week designs used in HSDD efficacy trials

Pilas de investigación

PT-141 is commonly paired in research settings with:

• Kisspeptin-10 — Kisspeptin-10 acts upstream in the hypothalamic-pituitary-gonadal axis, stimulating GnRH release, while PT-141 engages melanocortin receptors (MC3R/MC4R) at a parallel pathway. Researchers use both to examine complementary CNS-mediated and hormonal contributions to reproductive signaling.
• HCG — HCG mimics LH to stimulate gonadal steroidogenesis; pairing with PT-141 allows researchers to study melanocortin receptor modulation alongside direct luteinizing hormone receptor activity in models of reproductive function.
• Melanotan 2 — Both PT-141 and Melanotan 2 are melanocortin receptor agonists, but Melanotan 2 has broader receptor affinity (MC1R–MC5R). Comparative studies use both to isolate MC3R/MC4R-specific effects from pan-melanocortin receptor activation.

Garantía de pureza

Cada lote tiene una pureza ≥99 %. Si sometes tu compuesto a un análisis independiente y los resultados no coinciden, envíanos el certificado de análisis (COA) y te concederemos un vale de compra sin hacerte preguntas.