KPV

The C-terminal tripeptide of alpha-melanocyte-stimulating hormone, studied for anti-inflammatory signaling primarily in cells and mouse colitis models.

Preclinical-heavyPeptide research profile

Also known as: α-MSH(11-13), Lys-Pro-Val

Dosing & scaling, explained

The 200-500 mcg daily rows are recorded research presets. The anchor literature uses cell systems and oral mouse models, not a human injection trial. This is educational source context, not a protocol or recommendation.

How sourced amounts are organized

  1. Starting pointNot clinically establishedNo validated titration window

    There is no regulator-approved starting dose for this research use. A low-looking number is not automatically safe.

  2. Recorded preset200-500 mcg / dayCalculator library reference

    This is the range represented in the in-app protocol library. It describes the source record; it does not validate the regimen.

  3. Higher exposure500 mcg / day is the high library rowRisk and uncertainty increase

    Higher exposure is not established as more effective. Human pharmacokinetic and long-term safety data may be absent.

Drug amount and device markings are different quantities. The calculator converts mass into volume, syringe units, or pen clicks.

Patterns described in source material

  • Daily in recorded presets

    The cadence represented by the recorded calculator presets.

  • Oral delivery in mouse colitis studies

    Published experiments may use a different route, formulation, timing, or population and should not be treated as interchangeable.

  • No universal schedule

    No single schedule has been validated across products or research contexts.

Clinical context

No randomized human trial establishes dose, route, or efficacy for KPV.

Storage, handling and interpretation

Lyophilized material

Keep cold, dry, and protected from light according to the manufacturer certificate or validated lab SOP.

After reconstitution

Use sterile technique, refrigerate as validated, and avoid repeated freeze-thaw cycles.

Traceability

Record lot, concentration, preparation date, and the identity/purity documentation used by the lab.

Reported protocols for KPV

What published studies and recent community write-ups report about amounts, timing and course length. 1 clinical, 3 preclinical and 4 community-reported rows, each linked to its source. These are descriptions of what others report, not instructions, and nothing here is medical advice.

ContextDoseFrequencyRouteCourseSource
Clinical1 row
FDA 503A Bulks List evaluation (nominated topical product)None; FDA found no human study, case report or exposure data for KPV by any route0.1% cream or gel (the strength proposed in the nomination)Not specified in the nominationTopicalNot specifiedNot applicableU.S. Food and Drug Administration2026
The reviewers searched PubMed, Embase, ClinicalTrials.gov, FAERS and other databases and found no trial, adverse event report, pharmacokinetic study or acute, repeat-dose, genotoxicity or reproductive toxicity study for KPV free base or KPV acetate. They noted that KPV does not cross intact cadaver skin in vitro unless iontophoresis or microneedling is used, that registered outsourcing facilities reported no KPV compounding between 2017 and June 2025, and proposed not adding either form to the 503A list.
Preclinical3 rows
Oral KPV in drinking water, mouse colitis modelsC57BL/6 mice with DSS or TNBS colitis, 10 per group; human intestinal and T cell lines100 micromolar (µM) KPV in the drinking water; nanomolar concentrations in cell cultureContinuous access to treated waterOral8 days (3% DSS model) or 48 hours (150 mg/kg TNBS model)NoneGastroenterology (PubMed Central)2008
Oral KPV roughly halved colonic myeloperoxidase activity in the DSS model and cut it by about 30% after TNBS, with less weight loss and lower inflammatory cytokine expression, while in culture it blocked NF-kB and MAP kinase activation through PepT1-mediated uptake. Because the mice drank freely, no mg/kg dose can be derived from this study.
Hyaluronic-acid nanoparticles by oral gavageMice with colitis induced by 3% DSS for 8 days16 mcg/kg of KPV per day, carried in hyaluronic-acid-coated nanoparticles inside a chitosan/alginate hydrogelDouble gavage once dailyOral5 days of treatmentNoneMolecular Therapy (PubMed Central)2017
The coated particles (about 272 nm) homed to colonic epithelium and macrophages, lowered TNF-alpha and limited mucosal damage better than uncoated particles. The amount of free KPV that an ordinary capsule would deliver to inflamed colon is unknown and cannot be read off this figure.
Colitis-associated cancer model, transporter dependenceWild-type and PepT1-knockout mice given azoxymethane plus DSS; Apc Min/+ mice100 µmol/L KPV in the drinking waterContinuous during the DSS cycles; from 5 to 18 weeks of age in Apc Min/+ miceOralTwo 7-day DSS cycles each followed by 14 days of plain water; or 13 weeks14-day recovery periods between DSS cyclesCellular and Molecular Gastroenterology and Hepatology (PubMed Central)2016
KPV prevented inflammation-driven tumour formation in wild-type mice but had no effect in PepT1-knockout mice, tying its action to transporter uptake, and it did not reduce adenomas in the genetic Apc Min/+ model. Human colorectal tumours overexpressed PepT1 in the same paper, but no person received KPV.
Community-reported4 rows
Multi-route tiered guide (oral, injection, topical, nasal)Oral 200-500 mcg; subcutaneous 100-500 mcg; intranasal 100-200 mcg; topical applied to the affected areaOnce or twice daily by mouth; once daily by injectionOral capsule or liquid, subcutaneous, topical, intranasal4-8 weeks, 8-12 weeks for long-standing gut complaints, 2-6 weeks for wounds2-4 weeks off (4 weeks after a 12-week block); topical use only during flaresCommunity resource2026
Sets out starting, standard and upper tiers (200 mcg once daily up to 500 mcg twice daily by mouth; 100 to 500 mcg once daily by injection) and pairs KPV with BPC-157 as its most common stack. It states that the ranges come from community experience plus extrapolation from microgram-per-kilogram animal data and that there are no human trials.
Reconstitution chart with community schedule200-500 mcg per dayOnce daily by injection; once or twice daily by mouthSubcutaneous, oral, topical, less often intranasalSeveral weeks followed by a review period; 4-, 6-, 8-, 12- and 16-week planning examplesA review period after each block; nothing standardizedCommunity resource2026
Mostly arithmetic: 5 mg in 1 mL or 10 mg in 2 mL gives 5,000 mcg/mL, so 200 mcg is 4 units and 500 mcg is 10 units on a U-100 syringe. Every schedule is labelled community-reported rather than clinically established, and the page records that FDA's July 2026 materials proposed against listing KPV for compounding.

How a course is commonly described

  1. Weeks 1-2Community-reported

    Community guides describe starting at 200 mcg by mouth once daily on an empty stomach, or 100-200 mcg subcutaneously once daily, to check tolerance. Topical use is described as applied to the affected skin during a flare rather than on a schedule.

  2. Weeks 2-8Community-reported

    The working range quoted is 200-500 mcg once or twice daily by mouth or 200-500 mcg once daily by injection, with a symptom and marker review at 4 weeks; one wiki suggests CRP and fecal calprotectin as the checkpoints. Chronic gut protocols are stretched to 8-12 weeks.

  3. BreakCommunity-reported

    A 2-4 week pause after each block is the usual description, or an unspecified review period before deciding whether to repeat; some guides describe an open-ended 200 mcg per day maintenance instead. No source claims evidence for any of these intervals.

  4. Preclinical comparisonPreclinical

    The mouse colitis studies behind the community figures ran for 5 to 8 days, or for two 7-day DSS cycles, using 100 µM KPV in drinking water or 16 mcg/kg per day inside colon-targeted nanoparticles. None involved weeks of dosing, a break, or a free peptide given by injection, capsule or spray.

  5. Clinical comparisonClinical

    There is nothing to compare against: FDA's 2026 review found no human study of KPV by any route, no pharmacokinetic data and no toxicity studies, and the only product ever formally proposed for compounding was a 0.1% topical cream or gel.

  • No human has received KPV in a published study by any route, so every dose, duration and break above is community convention. FDA's 2026 review found no pharmacokinetic data, which means nobody knows how much oral, injected or nasal KPV reaches tissue or for how long.
  • The animal results that guides cite were produced with 100 µM KPV in drinking water or with colon-targeted nanoparticle hydrogels at 16 mcg/kg per day; a 2026 evidence profile points out that results from those delivery systems do not predict what a capsule, spray or vial will do, and FDA noted that KPV barely crosses intact skin in vitro.
  • KPV was removed from FDA's Category 2 compounding list in April 2026 after its nomination was withdrawn, and on 23 July 2026 the Pharmacy Compounding Advisory Committee voted 8 to 6 to recommend it for the 503A list against the agency reviewers' advice; formal rulemaking was still pending. These rows describe what sources report, not recommendations.
Sources for this section (16)
  1. FDA Briefing Document: Evaluation of KPV-Related Bulk Drug Substances (KPV (Free Base) and KPV Acetate) for the 503A Bulks ListU.S. Food and Drug Administration2026Clinical
  2. July 23-24, 2026: Meeting of the Pharmacy Compounding Advisory CommitteeU.S. Food and Drug Administration2026Clinical
  3. Alpha-melanocyte-stimulating hormone and related tripeptides: biochemistry, antiinflammatory and protective effects in vitro and in vivo, and future perspectives for the treatment of immune-mediated inflammatory diseasesEndocrine Reviews (PubMed)2008Preclinical
  4. Dissection of the anti-inflammatory effect of the core and C-terminal (KPV) alpha-melanocyte-stimulating hormone peptidesJournal of Pharmacology and Experimental Therapeutics (PubMed)2003Preclinical
  5. Antimicrobial effects of alpha-MSH peptidesJournal of Leukocyte Biology (PubMed)2000Preclinical
  6. PepT1-mediated tripeptide KPV uptake reduces intestinal inflammationGastroenterology (PubMed Central)2008Preclinical
  7. Melanocortin-derived tripeptide KPV has anti-inflammatory potential in murine models of inflammatory bowel diseaseInflammatory Bowel Diseases (PubMed)2008Preclinical
  8. Drug-loaded nanoparticles targeted to the colon with polysaccharide hydrogel reduce colitis in a mouse modelGastroenterology (PubMed)2010Preclinical
  9. Orally Targeted Delivery of Tripeptide KPV via Hyaluronic Acid-Functionalized Nanoparticles Efficiently Alleviates Ulcerative ColitisMolecular Therapy (PubMed Central)2017Preclinical
  10. Critical role of PepT1 in promoting colitis-associated cancer and therapeutic benefits of the anti-inflammatory PepT1-mediated tripeptide KPV in a murine modelCellular and Molecular Gastroenterology and Hepatology (PubMed Central)2016Preclinical

Plus 6 community resources (dosing guides, forum threads and vendor write-ups), reported above but not linked.

Overview

KPV is the tripeptide lysine-proline-valine, the last three residues of alpha-melanocyte-stimulating hormone and therefore also residues 11-13 of ACTH, which begins with the same 13-amino-acid sequence. Reviews from the Munster dermatology group describe it as the part of alpha-MSH that keeps the hormone's anti-inflammatory activity without its pigment-stimulating effect, and mechanistic work suggests it acts inside cells, entering through the PepT1 peptide transporter and damping NF-kB signalling rather than binding melanocortin receptors; it also inhibits Staphylococcus aureus and Candida albicans in culture. Every efficacy result comes from cell lines or from mouse and rat models of colitis, peritonitis, skin and corneal injury, including two 2008 mouse colitis studies, and the FDA's July 2026 review for compounding found no clinical study, no human exposure data and no pharmacokinetic or toxicity study in any species. KPV is sold as a research chemical and promoted by compounding and telehealth outlets as injections, capsules, creams and nasal sprays; FDA reviewers proposed against listing it for 503A compounding, the advisory committee nevertheless voted 8 to 6 to recommend it, and rulemaking had not concluded when this dossier was written.

What researchers are exploring

These themes describe recurring questions in published research. They are not claims of effectiveness or recommendations for use.

  • 1

    Intestinal inflammation

    DSS, TNBS, and transfer-colitis mouse models are the best-developed research area.

  • 2

    PepT1 transport

    Cell studies examine uptake through the di/tripeptide transporter PepT1.

  • 3

    NF-κB and MAPK signaling

    Laboratory work reports reduced inflammatory-pathway activation and cytokine output.

  • 4

    Barrier-targeted delivery

    Formulation studies explore oral and nanoparticle approaches for intestinal exposure.

What the current evidence can support

Study models remain visible so laboratory and animal findings are not mistaken for established human outcomes.

  • Animal

    Multiple mouse colitis models

    KPV reduced selected inflammatory and histologic measures in preclinical intestinal models.

  • In vitro

    Human epithelial and immune cells

    Nanomolar KPV was studied in cytokine-stimulated cell systems with PepT1-dependent uptake.

  • Review

    No established clinical regimen

    Published evidence does not establish injectable efficacy or long-term safety in humans.

Amounts recorded for KPV

These amount records are independent from vial strength, reconstitution volume and measuring device. A recorded source is not the same as study backing, and these values are not recommendations.

  • 1
    Lower recordedSign in for schedule, duration and source context.
    200 mcg
  • 2
    Dose · upper endpointSign in for schedule, duration and source context.
    500 mcg

Chemistry identifiers

Sequence, synonyms and registry identifiers as recorded in PubChem, the National Library of Medicine's open chemistry database. Formula, mass and CAS number are summarized at the top of the page.

Sequence

Lys-Pro-Val

Also listed as

alpha-MSH (11-13), ACTH (11-13), L-Lysyl-L-prolyl-L-valine, alpha-Melanotropin (11-13), H-Lys-Pro-Val-OH, UNII 7V6LGD8S5R, CHEBI:160254, DTXSID80987067

InChIKey

YSPZCHGIWAQVKQ-AVGNSLFASA-N

Origin / design

Residues 11-13 of α-MSH

IUPAC name

(2S)-2-[[(2S)-1-[(2S)-2,6-diaminohexanoyl]pyrrolidine-2-carbonyl]amino]-3-methylbutanoic acid

Limitations and unknowns

Important limitations

  • Mouse colitis outcomes do not establish treatment effects in human inflammatory bowel disease.
  • Oral PepT1-targeted research is not equivalent to an injectable preset.
  • A calculator preset is a recorded research convention, not a recommendation or evidence of clinical benefit.
  • Identity, purity, sterility, and stability can vary substantially outside regulated manufacturing.
  • Route, formulation, and population can make results from one study inapplicable to another use.

Sources

2 curated references, each with its journal, year and study model, plus 6 community resources reported but not linked.

  1. Melanocortin-derived tripeptide KPV has anti-inflammatory potential in murine models of inflammatory bowel diseaseInflammatory Bowel Diseases2008Animal
  2. PepT1-mediated tripeptide KPV uptake reduces intestinal inflammationGastroenterology2008In vitro