All information below describes the compound's chemical identity, laboratory handling, and the published research literature. It describes molecular targets and results in laboratory and animal models only — not effects in humans — and is not evidence of any human benefit.
What Is KPV?
KPV is a synthetic tripeptide composed of three amino acids — lysine, proline, and valine (sequence Lys-Pro-Val) — corresponding to the C-terminal fragment (residues 11–13) of alpha-melanocyte-stimulating hormone (alpha-MSH). It represents the shortest alpha-MSH-derived sequence that has been characterized in the melanocortin and inflammatory-signaling literature, and it has been a recurring subject of preclinical laboratory investigation since it was described in the early 1990s.
It is supplied as a reference compound for in vitro and animal research use only. The sections below summarize its chemical identity, laboratory handling, the molecular targets and model systems examined in the published literature, and the primary references — without describing outcomes, efficacy, or effects in humans.
Research Targets & Pathways
Published preclinical literature has examined KPV in relation to several molecular systems. These are pathway associations reported in laboratory and animal models; refer to the cited studies for methods and findings.
- Melanocortin-1 receptor (MC1R) — examined as a membrane receptor for alpha-MSH-derived peptides in dermal and immune cell systems.
- Melanocortin-3 receptor (MC3R) — investigated within the broader melanocortin receptor family in inflammatory model systems.
- NF-κB transcription pathway — studied in relation to nuclear factor kappa B nuclear translocation in intestinal epithelial and macrophage assays.
- PepT1 (SLC15A1) transporter — characterized as a di/tripeptide transporter mediating cellular uptake of KPV in intestinal epithelial models.
- Pro-inflammatory cytokine signaling — examined in relation to IL-1β, TNF-α, and IL-8 expression in stimulated cell cultures.
Model Systems Studied
KPV has been used as a test compound across a range of published preclinical model systems, primarily in rodents and in vitro cell assays. Refer to the cited literature for study designs, endpoints, and findings.
- Gastrointestinal — DSS-induced and TNBS-induced colitis models in mice and rats.
- Intestinal epithelium (in vitro) — Caco2-BBE and HT-29 epithelial cell lines and PepT1-transfected systems.
- Immune cells — macrophage and monocyte cultures in cytokine and NF-κB reporter assays.
- Cutaneous — keratinocyte and dermal inflammation model systems.
- Targeted-delivery formulation — hyaluronic-acid-functionalized nanoparticle and polysaccharide-hydrogel carriers evaluated in colitis models.
Stability & Handling
KPV is a low-molecular-weight tripeptide handled in the laboratory as a lyophilized powder. As with other short peptides, the published literature notes susceptibility to enzymatic hydrolysis by peptidases in biological media, which is one reason encapsulated and transporter-targeted delivery formats have been described in the research record. Lyophilized material is stored cold and desiccated to maintain structural integrity, and reconstituted solutions are handled to minimize freeze–thaw exposure. Values below are general laboratory guidance for in vitro and animal research.
Molecular & Technical Profile
C16H30N4O4 | MW 342.43 g/mol | CAS 67727-97-3 | Sequence: Lys-Pro-Val (KPV)
Storage, Reconstitution & Working Concentrations
Storage, reconstitution, and working-concentration values are general laboratory guidance for in vitro and animal research; always confirm against the lot-specific Certificate of Analysis.
Current Research Status
As of the time of this writing, KPV has not been approved by the U.S. Food and Drug Administration (FDA) for any human medical use. The available evidence base is primarily preclinical, derived from rodent and in vitro models, and has been reported by multiple independent research groups working in gastrointestinal, immunological, and dermatological model systems. Translation to human clinical contexts has not been established through controlled clinical trials. Ongoing research continues to characterize the compound's mechanistic profile — including its transporter-mediated uptake and receptor associations — and to develop delivery formulations for experimental use.
Research FAQ
Is KPV approved for human use?
No. KPV has not been approved by the FDA for any human medical use. The evidence base is preclinical (rodent and in vitro models), and the compound is supplied for laboratory research use only — not for human consumption.
What is KPV's molecular formula and sequence?
A synthetic tripeptide, sequence Lys-Pro-Val (the C-terminal fragment of alpha-MSH) — molecular formula C16H30N4O4, MW 342.43 g/mol, CAS 67727-97-3.
How is KPV stored and reconstituted?
Store lyophilized at −20°C, desiccated and protected from light. Reconstitute in sterile or bacteriostatic water; store the reconstituted solution at 2–8°C for up to ~28 days and avoid repeated freeze–thaw.
What mechanisms has KPV been studied for?
Preclinical work has characterized melanocortin receptor (MC1R) associations, the NF-κB inflammatory transcription pathway, and PepT1 (SLC15A1) transporter-mediated uptake across intestinal epithelial, macrophage, and cutaneous models. The reported data derive from multiple independent research groups.
Selected References
- Brzoska T, Luger TA, Maaser C, Abels C, Böhm M. (2008). Alpha-melanocyte-stimulating hormone and related tripeptides: biochemistry, antiinflammatory and protective effects in vitro and in vivo, and future perspectives. Endocrine Reviews, 29(5):581–602.
- Dalmasso G, Charrier-Hisamuddin L, Nguyen HTT, Yan Y, Sitaraman S, Merlin D. (2008). PepT1-mediated tripeptide KPV uptake reduces intestinal inflammation. Gastroenterology, 134(1):166–178.
- Kannengiesser K, Maaser C, Heidemann J, et al. (2008). Melanocortin-derived tripeptide KPV has anti-inflammatory potential in murine models of inflammatory bowel disease. Inflammatory Bowel Diseases, 14(3):324–331.
- Laroui H, Dalmasso G, Nguyen HTT, Yan Y, Sitaraman SV, Merlin D. (2010). Drug-loaded nanoparticles targeted to the colon with polysaccharide hydrogel reduce colitis in a mouse model. Gastroenterology, 138(3):843–853.
- Xiao B, Xu Z, Viennois E, et al. (2017). Orally Targeted Delivery of Tripeptide KPV via Hyaluronic Acid-Functionalized Nanoparticles Efficiently Alleviates Ulcerative Colitis. Molecular Therapy, 25(7):1628–1640.
- Li X, et al. (2021). Self-Cross-Linked Hydrogel of Cysteamine-Grafted γ-Polyglutamic Acid Stabilized Tripeptide KPV in a TNBS-Induced Ulcerative Colitis Rat Model. ACS Biomaterials Science & Engineering.