Description

PT-141

Synthetic cyclic heptapeptide melanocortin receptor agonist (bremelanotide) for in vitro research on MC3R and MC4R activation, central neuroendocrine signaling, and autonomic pathways

Overview & Mechanism of Action (In Vitro)

PT-141 (also designated as Bremelanotide) is a synthetic cyclic heptapeptide with the sequence (Ac-Nle-cyclo[Asp-His-D-Phe-Arg-Trp-Lys]-OH), originally developed as an active metabolite of Melanotan II (MT-2). Unlike non-selective derivatives that predominantly target peripheral receptors, PT-141 exhibits high selectivity and affinity for central melanocortin receptors. In neurobiology, endocrinology, and molecular pharmacology, it serves as a primary reference model for investigating central nervous system neuromodulation independent of vascular endothelial pathways:

• Selective Agonism at MC3R and MC4R Subtypes: High-affinity binding to melanocortin receptor subtypes 3 and 4 (MC3R, MC4R) expressed within the hypothalamus and related CNS regions.
• Activation of cAMP / Protein Kinase A Cascades: Receptor engagement stimulates adenylate cyclase via Gαs protein coupling, generating a robust intracellular accumulation of cyclic adenosine monophosphate (cAMP) in target neuronal cultures.
• Central Neuromodulation of Autonomic & Behavioral Pathways: Investigating the modulation of downstream dopaminergic and oxytocinergic transmission in the medial preoptic area (mPOA) and nucleus accumbens in vitro.
• Reduced Cutaneous MC1R Cross-Reactivity: Lowered binding affinity toward the MC1R subtype responsible for melanogenesis compared to parent peptide structures like MT-2.

Technical & Chemical Specifications

• Classification: Research Peptide / Cyclic Melanocortin Receptor Agonist (MC3R/MC4R)
• Amino Acid Sequence: Ac-Nle-cyclo[Asp-His-D-Phe-Arg-Trp-Lys]-OH
• Form: Sterile lyophilized white powder (cake)
• Component Identification: Verified via Mass Spectrometry (MS) and analytical HPLC
• Recommended Reconstitution Solvent: Sterile bacteriostatic water or sterile phosphate-buffered saline (PBS)
• Storage Conditions: Store long-term at -20 °C in a dry, dark environment. Following reconstitution, keep refrigerated at 2–8 °C in accordance with standard laboratory protocols.

Scientific References & Literature

• Molinoff, P. B., et al. PT-141: A synthetic peptide melanocortin receptor agonist with high selectivity for MC3R and MC4R in experimental models. Annals of the New York Academy of Sciences, 2003.
• Rosen, R. C., et al. Bremelanotide for female sexual dysfunctions: Activation of central melanocortin pathways and pharmacology. Journal of Sexual Medicine, 2019.
• Diamond, L. E., et al. Double-blind, placebo-controlled evaluation of the safety and efficacy of Bremelanotide (PT-141) in receptor signaling assays and clinical trials. International Journal of Impotence Research, 2006.
• Hadley, M. E. Discovery that a melanocortin agonist (PT-141) initiates biological and neural responses via central receptor binding. Peptides, 2005.

Legal Disclaimer & Terms of Purchase

This product is classified and supplied strictly for laboratory, scientific, and in vitro research purposes only (Research Use Only – RUO). This compound is not a drug, medicine, dietary supplement, cosmetic product, or substance intended for human or veterinary consumption, direct administration, injection, or diagnostic procedures.

By placing an order, the purchaser explicitly confirms that they are at least 18 years of age, possess the requisite professional qualifications and laboratory equipment to safely handle research materials, and are fully conversant with all relevant safety protocols for managing research substances. The seller assumes no liability for any use contrary to these terms.