KPV
Lys-Pro-Val Anti-Inflammatory Tripeptide
Evidence grade 1 of 5, Untested. Read how the Atlas grades evidence.
The anti-inflammatory activity of KPV, the C-terminal tripeptide (residues 11 to 13) of alpha-MSH, rests almost entirely on cell-culture and rodent work. The core mechanistic paper (Dalmasso et al., Gastroenterology 2008) showed PepT1-mediated uptake reduced colitis in DSS and TNBS mouse models and in human epithelial and Jurkat cell lines, and Xiao et al. (Molecular Therapy 2017) improved oral delivery with hyaluronic-acid nanoparticles in DSS mice, but no registered controlled human trial of KPV exists for any indication. The FDA's own July 2026 PCAC briefing found human clinical evidence of effectiveness absent, so an animal-only grade of 1 is the honest level.
Counted on the record: 0 human studies, 0 randomized trials, 0 participants, 6 animal studies, 3 lab studies.
No randomized human trial of KPV is recorded. The stored study and participant totals have conflicting scope.
- FDA
- Not FDA-approved for any indication. Reviewed at the July 2026 PCAC meeting, where FDA proposed NOT adding KPV to the Section 503A bulk drug substances list, citing that the substance is not well characterized and that human evidence of effectiveness and safety is lacking. Sold as a research chemical and via compounding, not as an approved drug.
- WADA
- Not specifically named on the WADA Prohibited List.
Reference only. Not medical advice.
What can go wrong
Human data essentially absent; anti-inflammatory claims are extrapolated from rodent colitis and cell studies, and gray-market product carries variable purity and unassessed immunogenicity risk.
Talk to a clinician before taking this. The Atlas can tell you what has been studied about KPV. It cannot tell you how it would interact with your body, your history, or anything else you are taking, and nothing on this page is a reason to start.
KPV is the C-terminal tripeptide (residues 11 to 13) of alpha-MSH, studied mainly for gut inflammation, inflammatory bowel disease, intestinal permeability, and wound and skin models. Its anti-inflammatory effect is PepT1-mediated rather than melanocortin-receptor-mediated, and it does not cause pigmentation. The supporting evidence is preclinical, drawn from cell lines and rodent colitis models, with no registered controlled human trial.
The anti-inflammatory tail of MSH. Gut-specific. Now in front of the FDA committee.
What people take it for
These are the reasons people give for taking it. They are not effects it has been shown to have.
How it is supposed to work
KPV is anti-inflammation stripped down to its bare minimum. It is just three amino acids, the tail end of a larger hormone called alpha-MSH, which the body uses to rein in inflammation. This is why alpha-MSH comes up so often when KPV is discussed: KPV is proposed to be the small fragment that carries forward much of alpha-MSH's calming effect on inflammation. Researchers found that almost all of that calming, anti-inflammatory power survives in those last three building blocks, while the parent hormone’s other jobs, like darkening skin and curbing appetite, fall away. The result is a tiny, stable peptide that, in the lab, quiets the inflammatory machinery inside cells, especially in the gut.
- Step 1PepT1 transportA transporter called PepT1, a protein on intestinal cells that normally moves small chains of amino acids across the cell membrane, can carry KPV into intestinal cells.
- Step 2Inflammatory signalingIn cell and animal models, KPV reduced several inflammation-linked signals, including activity of NF-kB, a molecular switch inside cells that turns on inflammatory genes and is linked to conditions such as inflammatory bowel disease (IBD).
- Step 3MC3R in the airwayIn human bronchial cells KPV works through the melanocortin-3 receptor, or MC3R, one of the receptors that the natural hormone alpha-MSH (yes, this is the pigmentation peptide, but it also has anti-inflammatory effects crucial for inhibiting certain cytokines like IL-10) normally acts on, to damp NF-kB (inflammation).
In mice, KPV reduced inflammation-linked colon tumors only when PepT1 was present and they observed the interaction of the MC3R in certain parts of the mouse model like the lungs. This was an animal cancer model, not evidence that KPV prevents or treats cancer in people.
Three amino acids, the tail of alpha-MSH. Lys-Pro-Val (Lysine - Proline - Valine).
- Type
- Tripeptide of alpha-MSH
- Action
- Anti-inflammatory
- Best data
- Gut, skin
- Human trials
- None
- Safety look
- Clean (preclinical)
- Approved
- No
Alpha-MSH Distilled, But Never Tested In People
KPV is one of the more elegant ideas in this library and one of the better-pedigreed gray-market peptides, which makes its limits worth stating precisely. The concept is genuinely clever: take alpha-MSH, a natural brake on inflammation, and keep only the three amino acids that carry most of that effect, leaving behind the pigmentation and appetite signaling. In cell and animal studies the result is potent and clean, calming the master inflammatory switch NF-kB, lowering inflammatory cytokines, and protecting the gut lining, with a notable study showing it reduces experimental colitis after being pulled into intestinal cells. The honest caveats are two. First, despite this strong preclinical record, there are essentially no published human clinical trials, so its benefits in people are unestablished. Second, its mechanism is murkier than the marketing suggests: it is often sold as a melanocortin-receptor activator, but the same researchers who first reported it binding that receptor later found it may not, and much of its activity now appears to run through other pathways. The safety record looks remarkably clean, but that too rests on preclinical and anecdotal data rather than trials.
How it is taken
Rectal
self-cross-linked hydrogel KPV in a self-cross-linked cysteamine-grafted polyglutamic-acid hydrogel. The hydrogel helped KPV retain biological activity for two hours at body temperature. This is formulation-specific rat and laboratory evidence, not a general KPV shelf life. Rectal administration in rats with chemically induced colitis.
Rectal
double-network hydrogel KPV held inside a negatively charged double-network polyglutamic-acid hydrogel. The hydrogel helped KPV retain activity during a 50 C laboratory stress test. This is a carrier-specific stress test, not room-temperature or refrigerated shelf life. Intracolonic administration in rats with chemically induced colitis.
Oral
nanoparticles in an alginate-chitosan hydrogel KPV-loaded nanoparticles inside an alginate-chitosan carrier. The carrier remained intact in stomach-like laboratory conditions and then broke down under colon-like conditions. This describes the carrier, not the chemical or storage stability of KPV itself. Given orally to mice with chemically induced colitis.
Research
lyophilized research sample KPV or a related peptide made by solid-phase synthesis. Patent examples stored lyophilized samples at minus 20 C. This is not a validated shelf life for an approved or standardized commercial product. Patent manufacturing example for KPV or a related peptide.
Injection
sterile buffered solution A protected KPV derivative in sterile isotonic saline with a near-neutral buffer. The patent also discusses copper salts and lipophilic carriers. The patent does not provide a validated shelf life, vial-storage period, or post-reconstitution stability period. Patent composition and animal experiments using a protected KPV derivative.
Safety in detail
- KPV keeps the anti-inflammatory part of alpha-MSH and leaves out the pigmentation signal, so it avoids that effect.
- The FDA's July 2026 briefing flagged incomplete characterisation and unassessed immunogenicity for injectable peptides in this group.
Children and teenagers
KPV is an unapproved anti-inflammatory peptide with no human trials, which makes it inappropriate for children. Pediatric inflammatory bowel disease and gut conditions belong with pediatric gastroenterology and approved therapies. There is no appropriate pediatric use.
What people get wrong
Often saidKPV is already proven to treat inflammatory bowel disease
ActuallyKPV has reduced inflammation in cell, mouse, and rat models, but no controlled human trial has established that it treats inflammatory bowel disease.
Often saidBecause KPV comes from alpha-MSH, its receptor mechanism is settled
ActuallyKPV keeps some anti-inflammatory activity from alpha-MSH, but published work does not support one simple, settled melanocortin-receptor explanation. Intestinal uptake and intracellular inflammatory signaling also matter.
Who profits, and who pushes back
Nobody is named here yet, because we have not done that work on this entry. Read that as unfinished. Somebody almost certainly sells this, and somebody almost certainly disputes it. Assume both until we have checked.
KPV’s money runs through gray-market peptide vendors selling it as an oral, topical or injectable anti-inflammatory for gut health and skin, feeding the gut-health wellness market, alongside research-reagent sales. There is no approved product. It is a well-pedigreed but preclinical-only gray-market economy.
How we got here
KPV is not a designed drug but the naturally occurring C-terminal tail of alpha-melanocyte-stimulating hormone, itself a cleavage product of pro-opiomelanocortin. Its anti-inflammatory identity traces to 1980s melanocortin work associated with James Lipton and Anna Catania, who progressively truncated alpha-MSH and found the Lys-Pro-Val fragment kept much of the anti-inflammatory activity while losing pigmentation and receptor binding. The gut-specific story was built later at Emory University by Didier Merlin and colleagues, whose PepT1-uptake papers reframed KPV as a candidate for inflammatory bowel disease and drove the nanoparticle delivery programs of Bo Xiao and coworkers. Today it circulates mainly as a compounded and research-chemical product rather than an approved medicine.
Alpha-MSH was known as an anti-inflammatory melanocortin hormone, and in the 1990s researchers found that its anti-inflammatory activity survives in the final three amino acids, KPV, without the pigmentation effects. Strong preclinical data accumulated in gut, colitis and skin models, including a notable colitis study, while the receptor mechanism was later revised. KPV was then adopted gray-market for gut and inflammation well ahead of any human trials.
2003
- 1992A US patent describes KPV-related anti-inflammatory compositionsThe most detailed inflammation examples used KPV in animal models to investigate dermatological use of the peptide.
- 2000Patent WO2003002087A1An international patent filing numbered WO2003002087A1 is printed with a title covering use of a Lys-Pro-Val (KPV) tripeptide in cosmetics. The patent discusses epidermal renewal, cutaneous micro-repair and treatment of chronic venous leg ulcers in animal models.
- 2001-2003FR-2826580-A1 Patent. L'OREAL sponsor?A PubChem patent page prints French filing FR-2826580-A1 with a title naming use of Lys-Pro-Val tripeptide (KPV) for epidermic renewal, cutaneous micro-healing and appearance of wounds and scars. The priority and filing date was of 2001-06-29, it was published 2003-01-03.
Patent and early research
1992 to 2008
KPV moved from anti-inflammatory patent experiments into gut-inflammation models.
- 2008Intestinal uptake and anti-inflammatory signaling are mappedKPV entered intestinal cells through PepT1 and reduced inflammatory signaling in mouse colitis and laboratory cell models (macrophage specific)
Preclinical delivery research
2010 to 2024
Carrier systems improved delivery in animal models, but no human efficacy trial followed.
- 2022A KPV-binding hydrogel is tested in inflamed colon modelsThe carrier retained KPV activity in a formulation-specific stress test and improved measures in rats; this is not general KPV shelf-life evidence, this is invasive treatment testing KPV's molecular properties
2010
- 2010USP patent 9156881 - KPV sister moleculeThe patent's own abstract and description, read at the printed address, confirm the filing concerns the tripeptide KdPT (Lys-D-Pro-Thr) for antiapoptotic treatment, a tripeptide distinct from KPV (Lys-Pro-Val) by its third residue and its proline stereochemistry. The numbered claims text, assignee and grant date were not read in this attempt, and no statement treating KdPT as an alias of KPV was found in the passage read.
The numbers behind the grade
- Type
- Alpha-MSH tripeptide
- Action
- Anti-inflammatory
- Best data
- Gut
- Human trials
- None
- Safety
- Clean (preclinical)
- Approved
- No
The people taking it
Users are people managing gut conditions like inflammatory bowel disease or gut permeability issues / leaky gut, alongside people dealing with inflammation, autoimmunity or inflamed skin.
The three-amino-acid anti-inflammatory core of alpha-MSH, distilled to keep the calming effect and shed the pigmentation, with strong preclinical gut data and a clean safety look but no human trials, sold gray-market for gut and inflammation.
KPV’s users are people seeking gut-health support for conditions like inflammatory bowel disease and leaky gut, along with people focused on inflammation and autoimmunity and those with skin inflammation. It appeals to the gut-health and anti-inflammatory biohacking crowd dealing with chronic conditions.
A gray-market anti-inflammatory peptide for gut conditions like inflammatory bowel disease and leaky gut, plus skin and systemic inflammation, with strong preclinical data but no human trials. Not approved.
Set against the alternatives
Against its parent alpha-MSH, KPV distills the anti-inflammatory effect while discarding the pigmentation and appetite signaling, the minimal fragment versus the full hormone. Against other gut peptides like BPC-157 and larazotide, it occupies a gut-anti-inflammatory niche, sharing BPC-157’s preclinical-heavy profile but lacking even larazotide’s rigorous, if failed, human trials. Against broad immunosuppressant drugs, it is pitched as targeted rather than blanket, which would be appealing if confirmed. And against VIP, it is another anti-inflammatory peptide running ahead of human evidence. Its strength is an elegant, clean preclinical story; its weakness is the missing trials.
What we do not know
- Whether its strong preclinical gut and anti-inflammatory data translate to human benefit.
- What its actual mechanism is, given the unsettled melanocortin-receptor question.
- Which route and dose work best, oral, topical or injectable.
- Whether it could become a real inflammatory-bowel or skin therapy with trials.
What could change
Targeted anti-inflammatoryIt could become a real gut or skin therapy if trials are run.Mechanism researchWork continues to clarify its non-melanocortin pathways.Variant peptidesRelated variants are also under study.Human-trial gapIts central need remains genuine human evidence.
Legal status
KPV is not approved. It has strong preclinical data in gut, colitis and skin inflammation but no published human trials, and it is sold gray-market in oral, topical and injectable forms for gut and inflammation. The safety look is clean in preclinical work, but human efficacy is unestablished.
Status current as of July 2026. Regulatory positions change, sometimes quickly.
The market for this
What follows describes how this is bought and sold. It is not a buying guide and it is not an endorsement of any seller.
No reliable price can be given from authoritative sources: KPV is not an FDA approved drug, so there is no approved product with a list price, and the material circulates as research-use-only or compounded supply whose prices come only from vendor and clinic marketing.
The concept and preclinical gut data are genuinely appealing and the safety looks clean, but human efficacy is unestablished.
KPV is commercially sold commonly in oral or topical form, with some nasal formulations, it stands in a preclinical-stage compound rather than a proven therapy. Sold for research purposes only.
Synthesized overseas, mainly in China, and sold gray-market in oral, topical and injectable forms, with no approved or human-grade product.
China and research vendorsSupply gray-market and research-use-only material.Multiple formsSold as oral capsules, topicals and injectables.No approved supplyThere is no regulated, human-grade source.
At a glance
- Amino acid sequence
- Lys-Pro-Val (Lysine - Proline - Valine)
- Amino acids
- 3
- Parent
- Alpha-MSH
- Action
- Gut anti-inflammatory, Skin anti-inflammatory, Skin protection
- Route
- Oral, Topical, Lotion, Injection
- Status
- PCAC review July 2026 pending FDA decision
What this entry does not yet cover
What follows is unfinished work on our side, not a finding about KPV.
Nothing outstanding on this one.
Sources
KPV is transported into intestinal cells via PepT1 and reduces inflammation in DSS and TNBS mouse colitis and human epithelial/T-cell lines by inhibiting NF-kB and MAPK signaling
Original PepT1-mediated KPV colitis study, peer-reviewed journal record and PubMed index
PepT1-mediated tripeptide KPV uptake reduces intestinal inflammation, PubMed 18061177
Oral hyaluronic-acid-functionalized nanoparticles delivering KPV accelerate mucosal healing and reduce inflammation in DSS-induced ulcerative colitis mice; free KPV context of a 12,000-fold lower effective concentration in nanoparticle form
PepT1-targeted co-assembled nanodrug of KPV plus an immunosuppressant treats acute and chronic DSS colitis in mice, a 2024 continuation of the preclinical delivery line
FDA is proposing NOT to add KPV to the Section 503A bulk drug substances list, citing that the substance is not well characterized and that human clinical evidence of effectiveness and safety is absent
FDA Pharmacy Compounding Advisory Committee convened July 23-24, 2026 to evaluate seven peptides including KPV for the 503A bulks list; none of the seven is FDA-approved and a PCAC recommendation is advisory only
FDA Panel to Evaluate 7 Popular Peptides for Compounding Substances List, Drug Topics
KPV corresponds to positions 11 to 13 of alpha-MSH, retains anti-inflammatory activity without melanocortin-receptor binding or pigmentation effects, and human clinical trials are absent
Historical context: alpha-MSH anti-inflammatory pharmacology and the C-terminal fragment as the minimal active sequence; review of alpha-MSH as an anti-inflammatory antimicrobial peptide
Sold as a research chemical / gray-market compounded item with variable purity; vendor listing documenting research-only status and amino-acid identity Lysine-Proline-Valine
KPV Peptide 5mg (Lysine-Proline-Valine) product listing, Healius Peptides
KPV is transported into intestinal cells via PepT1 and reduces inflammation in DSS and TNBS mouse colitis and human epithelial/T-cell lines by inhibiting NF-kB and MAPK signaling
A self-cross-linked hydrogel helped KPV retain biological activity for two hours at body temperature and improved colitis measures after rectal administration in rats.
A fluorescent KPV-based probe used PepT1-related targeting to distinguish chronic from acute colitis in laboratory and animal imaging work. It was a diagnostic probe, not a treatment formulation.
KPV reduced inflammation-linked colon tumors in mice when PepT1 was present. This does not show that KPV prevents or treats cancer in people.
A review of alpha-MSH and its related tripeptides collects anti-inflammatory and protective effects acting through melanocortin receptors and through NF-kB activation, adhesion molecules, chemokine receptors, cytokine production, IL-10 synthesis and T cell activity.
In immortalised human bronchial epithelial cells, KPV and alpha-MSH produced dose-dependent inhibition of NF-kB signalling, matrix metalloproteinase-9 activity, and IL8 and eotaxin secretion.
A review argues that alpha-MSH related peptides form a class of anti-inflammatory and immunomodulating agents acting through NF-kB, adhesion molecules, chemokine receptors and cytokine production, with the effects confirmed in animal models of inflammation.
In human HaCaT keratinocytes exposed to fine particulate matter, 50 micrograms per mL of KPV restored cell viability, reduced IL-1 secretion and inhibited reactive oxygen species production.
In a mouse model of crystal-induced peritonitis, systemic treatment with KPV, alpha-MSH, the core melanocortin peptide His-Phe-Arg-Trp, and the melanocortin receptor 3/4 agonist MTII each produced significant reduction in polymorphonuclear leukocyte accumulation in the peritoneal cavity, while the selective MC1 receptor agonist MS05 did not. In cultured macrophages, alpha-MSH and MTII inhibited macrophage activation measured as release of KC and interleukin-1 beta, but KPV did not. KPV also showed anti-inflammatory effects in interleukin-1 beta induced peritonitis and in recessive yellow e/e mice carrying a nonfunctional MC1 receptor. No human data were reported.
FDA's advisory committee calendar lists a meeting of the Pharmacy Compounding Advisory Committee held on July 23 and 24, 2026, at which nominated bulk drug substances for the Section 503A compounding list, KPV among them, were on the agenda. Being considered at that meeting is a regulatory step and says nothing about how strong the evidence for KPV is.
FDA, July 23-24, 2026 Meeting of the Pharmacy Compounding Advisory Committee
FDA published a briefing document for the July 23, 2026 morning session of the Pharmacy Compounding Advisory Committee setting out points for the committee to consider on nominated 503A bulk drug substances. In the excerpt of that document read for this entry, FDA proposed that BPC-157, free base and acetate, not be included on the 503A Bulks List, and the KPV-specific line in the same document was not confirmed in that excerpt, so what FDA staff proposed for KPV is not established here.
A dimeric KPV-containing analogue, (CKPV)2 (a dimer of Ac-Cys-Lys-Pro-Val-NH2), was reported in a rat model of Candida albicans vaginitis to inhibit vaginal Candida albicans survival and macrophage sub-epithelial mucosa infiltration, and to induce macrophage M2 polarisation in that same rat model. The paper (Ji et al., 'The Synthetic Melanocortin (CKPV)2 Exerts Anti-Fungal and Anti-Inflammatory Effects against Candida albicans Vaginitis via Inducing Macrophage M2 Polarization') was published in PLoS ONE in 2013 (PLoS ONE 8(2): e56004), with listed authors affiliated to the State Key Laboratory of Natural Medicines, China Pharmaceutical University, China. Its printed funding statement names the National Natural Science Foundation of China (grant numbers 91129731 and 81072661) and the Project Program of the State Key Laboratory of Natural Medicines, China Pharmaceutical University, as sponsors. The source states no species or model beyond this single rat vaginitis model, and does not state any human data for this finding.
KPV carries CAS number 67727-97-3, PubChem CID 125672 and ChEBI identifier CHEBI:160254, with molecular formula C16H30N4O4 and molar mass 342.440 g/mol.
The studies that matter
Distillation concept1990s
KPV is the anti-inflammatory tail of alpha-MSH, keeping the calming effect while shedding pigmentation and appetite signaling.
Anti-inflammatory mechanismpreclinical
It calms NF-kB, lowers inflammatory cytokines, shifts macrophages toward repair and protects gut lining cells.
Gut and colitis data2008
A notable study showed KPV is pulled into intestinal cells by a transporter and reduces experimental colitis.
Mechanism uncertainty2003-2007
Reported to bind a melanocortin receptor, then found possibly not to, with much activity through other pathways.
Human gap2026
Despite strong preclinical data, there are essentially no published human clinical trials.