Bremelanotide(CAS:1607799-13-2)

Bremelanotide (PT141, CAS 1607799-13-2) is a synthetic cyclic polypeptide modified from natural α-MSH structure. As the world’s first clinically transformed central sexual function regulatory drug, it fundamentally breaks the limitation of traditional sexual drugs that only act on peripheral blood vessels, becoming an indispensable high-purity research peptide raw material in the fields of sexual neuropharmacology, endocrine regulation and central nervous system function research. It appears as white lyophilized powder with stable polypeptide sequence and excellent physicochemical properties. Featuring superior water solubility, it dissolves stably in pure water, buffer solutions and DMSO, supporting in vitro cell administration, in vivo subcutaneous injection and intranasal modeling. Purified by professional peptide refining technology with HPLC purity over 98%, it strictly controls truncated peptides, isomers, residual ions and pyrogen impurities, meeting high-end research peptide standards. It fully supports full-process research including melanocortin receptor target verification, neuroendocrine cell experiments, sexual dysfunction animal modeling and central dopamine pathway analysis with uniform batch activity and reliable experimental repeatability.

It possesses a unique central neuroregulatory mechanism that differentiates it radically from conventional PDE5 inhibitors. Drugs such as sildenafil and tadalafil only improve erection by dilating peripheral cavernous blood vessels and cannot solve central disorders including low sexual desire and arousal dysfunction. In contrast, Bremelanotide efficiently crosses the blood-brain barrier and targets core sexual regulation brain regions including the hypothalamic medial preoptic area and paraventricular nucleus. It selectively activates MC4R receptors and synergistically modulates MC3R receptors, precisely regulating the release of central neurotransmitters such as dopamine and norepinephrine. This pathway effectively elevates sexual desire, enhances arousal response and relieves sexual psychological depression, fundamentally improving sexual dysfunction caused by neurological, endocrine and psychological factors. Pharmacological studies verify that it significantly promotes proceptive behaviors in female animals and induces penile erection in male models, achieving bidirectional sexual regulation. With no peripheral cardiovascular activity, it avoids hypotension and visual side effects of traditional drugs and provides a wider safety experimental window.

Bremelanotide delivers diversified core research and clinical value. Clinically, its preparation is an FDA-approved specific treatment for premenopausal women with acquired generalized hypoactive sexual desire disorder (HSDD), filling the clinical gap of targeted central drugs for female sexual dysfunction. Scientifically, it covers four core research directions: exploring the pathogenesis of central sexual dysfunction caused by MC4R mutation and dopamine pathway disorder; evaluating drug efficacy in bidirectional male and female sexual function models and comparing mechanistic differences with peripheral vasodilators; supporting cross-disciplinary neuroendocrine research involving melanin secretion, energy metabolism and appetite regulation; and guiding structural optimization, affinity modification and low-toxicity lead compound screening for novel melanocortin peptides.

In terms of supply and industrial value, Bremelanotide is synthesized via mature solid-phase peptide synthesis (SPPS), with precise amino acid assembly, oxidative cyclization and HPLC purification to completely remove truncated and polymeric impurities while retaining complete biological activity. Available in milligram and gram specifications, it fully meets the demands of university basic research, CRO pharmacological evaluation and innovative peptide drug development. It supports flexible administration routes including subcutaneous injection and intranasal delivery with excellent long-term in vivo tolerance and no obvious hepatorenal or neurological toxicity. With rising global demand for sexual dysfunction research and treatment, central-targeted, bidirectional and low-side-effect peptide drugs have become a mainstream R&D direction. As the benchmark MC4R tool peptide with comprehensive preclinical and clinical data, Bremelanotide maintains irreplaceable core research value in central neuroregulation, endocrine pharmacology and innovative peptide drug development, promising broad long-term application prospects in global pharmaceutical research.