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Endocrine

PT-141 (Bremelanotide)

Bremelanotide is a cyclic heptapeptide analogue of alpha-melanocyte-stimulating hormone (α-MSH) with the sequence Ac-Nle-cyclo[Asp-His-D-Phe-Arg-Trp-Lys]-OH (CAS 189691-06-3; MW 1025.18 Da), supplied ...

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Certificate of Analysis included with every order.

Technical Specifications

Purity≥98%
FormLyophilized powder
Storage-20°C
Molecular Weight1025.18 Da
SequenceAc-Nle-cyclo[Asp-His-D-Phe-Arg-Trp-Lys]-OH
CAS Number189691-06-3

About This Peptide

Bremelanotide is a cyclic heptapeptide analogue of alpha-melanocyte-stimulating hormone (α-MSH) with the sequence Ac-Nle-cyclo[Asp-His-D-Phe-Arg-Trp-Lys]-OH (CAS 189691-06-3; MW 1025.18 Da), supplied here as PT-141 (Bremelanotide) in lyophilized powder form at ≥98% purity. Originally derived from the linear peptide Melanotan II through structural modification, bremelanotide was developed to investigate the pharmacology of the central melanocortin system with enhanced metabolic stability relative to its predecessors. Its cyclized backbone and incorporation of a D-Phe residue at position 4 confer resistance to proteolytic degradation, making it a valuable tool for extended in vitro and preclinical receptor-binding studies.

Bremelanotide selectively engages melanocortin receptor subtypes, particularly MC3R and MC4R, which are widely expressed in hypothalamic and limbic brain regions. These receptors are integral nodes in neural circuits governing energy homeostasis, autonomic tone, and neuroendocrine regulation, situating bremelanotide at the center of research into central peptidergic signaling. The compound's receptor selectivity profile distinguishes it from broader melanocortin agonists, enabling investigators to dissect subtype-specific contributions to downstream second-messenger cascades and behavioral endpoints in animal models.

As a member of the melanocortin peptide class, bremelanotide has been widely employed in neuropharmacology, neuroendocrinology, and receptor pharmacology research. Studies utilizing this compound have contributed to mapping the functional roles of MC3R and MC4R in rodent and primate model systems, advancing understanding of hypothalamic circuit dynamics. Its well-characterized pharmacokinetic properties in preclinical species also make bremelanotide a useful comparator when evaluating novel melanocortin ligands. All research applications involving this compound should be conducted under appropriate institutional protocols. For research use only. Not for human consumption.

Research Applications

≥98% purity. Lyophilized powder. Storage: -20°C. For research purposes only.

Mechanism of Action

Bremelanotide acts as a potent agonist at melanocortin receptors, principally MC3R and MC4R, which are G protein-coupled receptors (GPCRs) that signal predominantly through Gαs-mediated stimulation of adenylyl cyclase. Receptor engagement by bremelanotide leads to elevated intracellular cyclic AMP (cAMP) concentrations, subsequent activation of protein kinase A (PKA), and phosphorylation of downstream effectors including CREB and other transcription factors involved in neuronal plasticity and neuropeptide gene regulation. The D-Phe substitution in the peptide sequence enhances receptor affinity and resistance to enzymatic cleavage, allowing sustained receptor occupancy in experimental systems.

Beyond cAMP signaling, MC4R activation has been linked in preclinical studies to modulation of MAPK/ERK pathways and regulation of hypothalamic neuropeptide expression, including interactions with the melanocortin-opposing peptides AgRP and NPY. MC3R engagement is associated with feedback regulation of melanocortin tone within the arcuate nucleus and peripheral autonomic pathways. These converging signaling mechanisms make bremelanotide a versatile probe for dissecting the molecular crosstalk between melanocortinergic neurons and other neuromodulatory systems in both in vitro cell-based assays and in vivo preclinical models.

Research Applications

Bremelanotide is used across a range of preclinical and in vitro research contexts focused on melanocortin receptor pharmacology and central peptidergic signaling. Representative research application areas include:

  • Melanocortin receptor binding assays: Competitive radioligand or fluorescence-based displacement assays to characterize MC3R and MC4R binding kinetics, affinity constants, and selectivity profiles of novel ligand candidates.
  • cAMP second-messenger studies: Quantification of Gαs-coupled cAMP accumulation in heterologous expression systems (e.g., HEK293 cells stably expressing MC3R/MC4R) to establish concentration-response relationships and efficacy parameters.
  • Hypothalamic circuit and neuropeptide regulation research: In vitro and ex vivo studies examining bremelanotide-induced changes in arcuate nucleus neuropeptide expression (AgRP, NPY, POMC) using primary hypothalamic neuron cultures or acute brain slice preparations.
  • Energy homeostasis and feeding behavior models: Preclinical rodent studies investigating the role of central MC4R activation in food intake regulation, body weight dynamics, and metabolic rate using bremelanotide as a pharmacological tool.
  • Autonomic and cardiovascular neuroscience research: Examination of melanocortin-mediated autonomic modulation, including heart rate and blood pressure responses in rodent models, to map peripheral MC receptor contributions.
  • Structure–activity relationship (SAR) benchmarking: Use of bremelanotide as a reference agonist standard when evaluating novel cyclic peptide analogues for melanocortin receptor selectivity and potency.

Storage & Handling Guidelines

Proper storage and handling are essential to maintain peptide integrity and ensure reliable research results. All Pepitiva Biolabs peptides are supplied as lyophilized (freeze-dried) powder, which provides excellent long-term stability when stored correctly. Store lyophilized peptides at -20°C for long-term storage or 2-8°C for short-term use. Once reconstituted, peptide solutions should be stored at 2-8°C and used within the timeframe specified in the product documentation. Always use sterile bacteriostatic water for reconstitution and handle peptides in a clean laboratory environment to prevent contamination. Avoid repeated freeze-thaw cycles, as thermal stress can cause peptide degradation and loss of biological activity.

Quality Control & Certification

This product is manufactured under strict quality control protocols and has been verified through comprehensive analytical testing. Each batch undergoes reverse-phase HPLC analysis for purity determination and electrospray ionization mass spectrometry (ESI-MS) for molecular identity confirmation. A detailed Certificate of Analysis (COA) is available for download, documenting purity percentage, molecular weight verification, appearance, and recommended storage conditions. Pepitiva Biolabs maintains batch-level traceability from synthesis through delivery, ensuring complete transparency and quality assurance for your research.

Frequently Asked Questions

Is this product approved for human use?

No. This product is intended exclusively for in vitro scientific research and laboratory use. It is not approved for human or veterinary use, not intended for diagnostic or therapeutic purposes, and should not be administered to humans or animals under any circumstances.

How do I reconstitute this peptide?

Add sterile bacteriostatic water slowly to the vial, directing the stream against the glass wall rather than directly onto the lyophilized powder. Gently swirl the vial until the powder is fully dissolved — do not shake vigorously. The recommended reconstitution volume depends on your desired concentration. Refer to the product documentation for specific guidance.

Can I get a Certificate of Analysis (COA)?

Yes. A Certificate of Analysis is included with every order and is also available for download from the product page. The COA documents HPLC purity, mass spectrometry identity confirmation, batch number, production date, and storage recommendations.

For research use only. Not for human consumption.

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