PT-141 10mg

PT-141 (Bremelanotide) is a synthetic cyclic heptapeptide analogue of alpha-melanocyte-stimulating hormone (α-MSH). It was derived from the linear melanocortin peptide Melanotan II through targeted structural modification to optimise melanocortin receptor selectivity, particularly at the MC3R and MC4R receptor subtypes expressed in the central nervous system.

The compound’s development represents a notable example of rational peptide drug design within the melanocortin system. Unlike its parent compound Melanotan II, which exhibits broad melanocortin receptor activity across MC1R-MC5R, PT-141 was engineered to preferentially engage MC3R and MC4R — receptors implicated in central nervous system pathways distinct from those governing pigmentation.

PT-141 received FDA approval in 2019 under the brand name Vyleesi for a specific clinical indication (hypoactive sexual desire disorder in premenopausal women), becoming the first melanocortin receptor agonist approved for this category. The approval was based on Phase III clinical trials involving over 1,200 participants demonstrating statistically significant efficacy versus placebo.

Mechanistically, PT-141 acts via melanocortin receptor-mediated activation of intracellular cAMP signalling cascades. Its activity profile at MC3R and MC4R has made it a valuable pharmacological tool for researchers investigating melanocortin receptor signalling, G-protein-coupled receptor (GPCR) selectivity, and downstream neuropeptide pathways.

Research applications include melanocortin receptor binding studies, structure-activity relationship comparisons within the α-MSH peptide family, GPCR signalling pathway analysis, and controlled in-vitro investigations of melanocortin receptor pharmacology.

⚗ For In-Vitro Research Use Only. Not for human consumption, veterinary use, or clinical application. No dosing guidance is provided or implied.