All information below describes the compound's chemical identity, laboratory handling, and the published research literature. It describes molecular targets and results in laboratory and animal models only — not effects in humans — and is not evidence of any human benefit.
What Is PT-141?
PT-141 (Bremelanotide) is a synthetic heptapeptide (CAS 189691-06-3, molecular weight 1025.18 g/mol) belonging to the melanocortin peptide class. It is a structural analogue derived from the melanocortin family and does not occur freely in nature; it is characterized in the literature as a synthetic melanocortin-receptor agonist with subtype selectivity distinct from earlier, non-selective compounds in the same peptide class. It is a metabolite-derived successor to the melanotan-series peptides and has been described across preclinical and clinical pharmacology reports.
It is supplied as a reference compound for in vitro and animal research use only. The sections below summarize its chemical identity, laboratory handling, the molecular targets and model systems examined in the published literature, and the primary references — without describing outcomes, efficacy, or effects in humans.
Research Targets & Pathways
Published literature has examined PT-141 in relation to several molecular systems. These are pathway associations reported in laboratory and animal models; refer to the cited studies for methods and findings.
- Melanocortin receptor MC4R — examined in relation to receptor binding and agonist activity at the type-4 melanocortin receptor.
- Melanocortin receptor MC3R — examined in relation to central melanocortin-receptor subtype activity alongside MC4R.
- cAMP signaling — studied via downstream cyclic-AMP functional-activation assays following receptor engagement.
- Beta-arrestin-2 / MC4R axis — examined in relation to MC4R intracellular-pathway dependencies in receptor-expressing neurons.
- Central nitric oxide (NO) pathways — examined as a downstream signaling system within spinal and supraspinal reflex circuits.
- MC1R / MC3R melanocortin binding — examined in melanocortin-peptide receptor-binding studies within the broader peptide class.
Model Systems Studied
PT-141 has been used as a test compound across a range of published preclinical model systems, primarily in rodents and in vitro receptor assays. Refer to the cited literature for study designs, endpoints, and findings.
- In vitro receptor pharmacology — radioligand-displacement and receptor-binding assays at melanocortin receptor subtypes, and cAMP functional-activation assays.
- Central nervous system — rodent models with intracerebroventricular peptide administration examining melanocortin-receptor signaling.
- Reflex-circuit models — rat spinal and supraspinal reflex-circuit models examining central melanocortin receptors and downstream nitric oxide pathways.
- Genetic knockout models — murine MC4R-expressing-neuron beta-arrestin-2 knockout models characterizing intracellular pathway dependencies.
- Endocrine / immune models — adrenal and immune-cell models examining melanocortin-system interactions with the ACTH–cortisol axis.
Molecular & Technical Profile
C50H68N14O10 | MW 1025.18 g/mol | CAS 189691-06-3 | Class: synthetic heptapeptide (melanocortin)
Storage, Reconstitution & Working Concentrations
Storage, reconstitution, and working-concentration values are general laboratory guidance for in vitro and animal research; always confirm against the lot-specific Certificate of Analysis.
Current Research Status
The bremelanotide drug product (marketed as Vyleesi) carries U.S. Food and Drug Administration (FDA) approval for a single indication, hypoactive sexual desire disorder in premenopausal women. The research-grade material supplied by Explicit Research is not that drug product; it is a reference compound for laboratory research use only and is not an approved drug. Outside of that single regulatory context, the wider literature summarized here is preclinical and investigational, derived from rodent and in vitro receptor models, and has not been established for other human contexts through controlled clinical trials. Ongoing research continues to characterize the compound's mechanistic profile at melanocortin receptors.
Research FAQ
Is PT-141 approved for human use?
The bremelanotide drug product (marketed as Vyleesi) carries FDA approval for a single indication, hypoactive sexual desire disorder in premenopausal women. The research-grade material supplied by Explicit Research is not that drug product — it is a reference compound for laboratory research use only, is not for human consumption, and is not an approved drug. Other applications discussed in the literature remain investigational or preclinical.
What is PT-141's molecular formula?
A synthetic heptapeptide of the melanocortin class — molecular formula C50H68N14O10, MW 1025.18 g/mol, CAS 189691-06-3.
How is PT-141 stored and reconstituted?
Store lyophilized at −20°C, protected from light and moisture. Reconstitute in sterile water for injection or bacteriostatic (0.9%) saline; store the reconstituted solution at 2–8°C for up to ~28 days and avoid repeated freeze–thaw.
What targets and model systems has PT-141 been studied in?
Published work has examined melanocortin receptor subtypes (MC3R and MC4R), downstream cAMP signaling, beta-arrestin-2-dependent MC4R signaling, and central nitric oxide pathways — using rodent intracerebroventricular models, rat spinal/supraspinal reflex-circuit models, murine MC4R-neuron knockout models, and in vitro receptor-binding and cAMP assays.
Selected References
- Hadley et al. - Pharmacology and preclinical characterization of bremelanotide (PT-141), including receptor binding and initial in vivo profiling - Expert Opin Investig Drugs, 2004
- Hruby et al. - Structure-activity relationships of melanocortin peptides at MC1R through MC5R subtypes examined via cyclic lactam analogues - J Med Chem, 2001
- Wikberg et al. - New aspects on the melanocortins and their receptors - Pharmacol Res, 2000
- Molinoff et al. - PT-141: a melanocortin agonist for the treatment of sexual dysfunction - Ann N Y Acad Sci, 2003
- Lau et al. - Beta-arrestin-2 knockout in MC4R-expressing neurons measured for metabolic and signaling deficits in murine models, characterizing MC4R intracellular pathway dependencies - JCI Insight, 2026
- Van der Ploeg et al. - Melanocortin receptor subtypes MC3R and MC4R assessed for role in CNS-mediated erectile response in rodent models following intracerebroventricular peptide administration - Proc Natl Acad Sci USA, 2002
- Giuliano et al. - Central melanocortin receptors and their downstream nitric oxide pathways measured in spinal and supraspinal erectile reflex circuits in rat models - Neuroscience, 2003
- Catania et al. - Anti-inflammatory properties of melanocortin peptides measured in peripheral and CNS tissue models, including cytokine suppression assays and MC1R/MC3R binding studies - Pharmacol Rev, 2004
- Cone et al. - Hypothalamic melanocortin circuitry assessed for regulation of energy homeostasis and neuroendocrine output via MC3R and MC4R rodent knockout and pharmacological models - Nat Neurosci, 2005
- FDA Clinical Pharmacology Review - Bremelanotide pharmacokinetics, transient hemodynamic effects, and contraindication in cardiovascular disease assessed during regulatory review preceding 2019 FDA approval - Clin Pharmacol Drug Dev, 2019
