KPV is a synthetic tripeptide with the sequence Lys-Pro-Val (lysine-proline-valine). It corresponds to the C-terminal amino acids 11-13 of alpha-melanocyte stimulating hormone (α-MSH), a 13-amino acid peptide derived from pro-opiomelanocortin (POMC). KPV is registered under CAS number 13147-06-3 and has a molecular formula of C₁₆H₃₁N₅O₄ with a molecular weight of 357.45 g/mol.

Alpha-MSH has well-documented anti-inflammatory properties mediated through its interaction with melanocortin receptors, particularly MC1R and MC3R. Research has identified the C-terminal tripeptide KPV as retaining significant anti-inflammatory activity despite its much smaller size compared to the full α-MSH sequence. This finding has generated interest in KPV as a research tool for studying melanocortin-mediated anti-inflammatory pathways in a more tractable molecular format.

The most extensively studied application of KPV in preclinical research concerns intestinal inflammation. Studies in rodent models of colitis have documented anti-inflammatory effects of KPV treatment, including reductions in pro-inflammatory cytokine levels (TNF-α, IL-6, IL-1β), improvements in histological inflammation scores, and preservation of intestinal barrier integrity. Research has examined both systemic and local (intracolonic) administration routes. The gut-specific research focus of KPV contributed to its nomination for the FDA's 503A Bulks List review in 2026.

The molecular mechanism of KPV's anti-inflammatory effects is not fully characterized. Research has suggested involvement of melanocortin receptor-dependent pathways, as KPV retains the C-terminal sequence required for MC1R and MC3R interaction. However, some studies have documented anti-inflammatory effects in cells lacking melanocortin receptor expression, suggesting receptor-independent mechanisms may also contribute. Research has implicated NF-κB pathway inhibition as a potential mechanism.

For in vitro research, KPV is typically used at concentrations of 1 nM to 1 μM in cell-based anti-inflammatory assays. Common applications include cytokine production assays in stimulated macrophages or intestinal epithelial cells, NF-κB reporter assays, and barrier function assays using transepithelial electrical resistance (TEER) measurements in Caco-2 or T84 cell monolayers.

KPV was among the compounds that received a favorable recommendation from the FDA's Pharmacy Compounding Advisory Committee on July 23, 2026.