Primary Description

Also known as:Lysine-Proline-Valineα-MSH(11-13)C-terminal tripeptide of α-MSHLys-Pro-Val (tripeptide)

KPV is a tripeptide (Lys-Pro-Val) derived from the C-terminal sequence of alpha-melanocyte stimulating hormone (α-MSH). It possesses potent anti-inflammatory properties and represents a promising therapeutic agent for inflammatory bowel disease (IBD) and other inflammatory conditions. Unlike full-length α-MSH, KPV exerts its anti-inflammatory effects through a unique PepT1-mediated mechanism rather than through melanocortin receptors. This allows it to be transported into cells via the di/tripeptide transporter PepT1, which is upregulated in inflamed colonic tissue, enabling targeted delivery to sites of inflammation. Nanomolar concentrations inhibit NF-κB and MAPK inflammatory signaling pathways. Oral administration is effective in animal models of colitis, representing a rare peptide with oral bioavailability for gut-targeted delivery.

Key Benefits

Anti-inflammatory
Gut healing
Antimicrobial

Demonstrated Effects

Potent anti-inflammatory activity at nanomolar concentrations
Targeted delivery to inflamed tissue via PepT1 transporter upregulation in IBD
Inhibits NF-κB and MAPK inflammatory signaling pathways
Reduces pro-inflammatory cytokines (IL-1β, TNF-α, IL-6)
Oral bioavailability — effective when administered orally in colitis models
Gut barrier restoration and intestinal permeability reduction
Anti-inflammatory effects in airway inflammation
Wound healing enhancement
Reduced systemic exposure compared to traditional anti-inflammatory drugs

Proposed Mechanisms of Action

Proposed mechanisms based on available research

Research Evidence & Clinical Data

Review of available research evidence and clinical data

Investigated Applications

Inflammatory Bowel Disease (IBD)

Anecdotal: Medium

Crohn's disease treatment potential, ulcerative colitis symptom reduction, colonic inflammation suppression, and pro-inflammatory cytokine reduction. PepT1 upregulation in IBD provides natural targeted delivery to inflamed colon.

Preclinical basis: Dalmasso et al. (2008) Gastroenterology: demonstrated KPV's PepT1-mediated uptake and anti-inflammatory effects in DSS and TNBS colitis models. Effective when added to drinking water in mice. Lee et al. (2015) J Crohns Colitis confirmed oral delivery efficacy.

Gut Barrier Restoration

Anecdotal: Medium

Mucosal barrier repair, intestinal permeability reduction, epithelial healing promotion, and leaky gut syndrome treatment. Promotes tight junction integrity.

Preclinical basis: Chai et al. (2019) Front Pharmacol demonstrated KPV promotes intestinal epithelial barrier function and tight junction integrity.

Systemic Inflammation

Anecdotal: Low

Chronic inflammatory conditions, autoimmune disease modulation, inflammatory skin conditions, and wound healing enhancement.

Preclinical basis: Land et al. (2012) J Immunol demonstrated KPV's systemic immune modulation and airway protection effects. Chen et al. (2017) showed inhibition of pro-inflammatory cytokines in macrophages via NF-κB and MAPK pathways.

Scientific References

1.
PepT1-mediated tripeptide KPV uptake reduces intestinal inflammation
Gastroenterology2008
2.
Melanocortin-derived tripeptide KPV has anti-inflammatory potential in murine models of inflammatory bowel disease
Inflamm Bowel Dis2008

Safety Profile

Common Side Effects

Injection site reactions — mild, transient
GI symptoms — rare with oral administration
Excessive immunosuppression — theoretical, may impair infection response
Allergic reactions — possible with any peptide
Long-term effects — unknown in humans
Minimal

Contraindications

Known hypersensitivity to KPV or related peptides
Pregnancy and breastfeeding — insufficient safety data
Active severe infections requiring intact immune response
Immunocompromised states — may further suppress immunity
Active malignancy — insufficient data
Children under 18 — no pediatric safety data
Severe liver or kidney disease — metabolism/excretion unclear
None well-established

Research Protocols

Dosing protocols based on available research data

Dosing Protocols

Typical Dose

Subcutaneous: 500–1000 mcg per injection. Oral (investigational): 1–5 mg, 1–2 times daily. IBD oral protocol: 2–5 mg twice daily. Topical: 0.5–2% KPV cream or gel.

Frequency

Once daily (subcutaneous); 1–2 times daily (oral). IBD: continuous dosing for symptom management.

Route

Subcutaneous injection (abdomen or thigh); oral administration (IBD preferred, targets inflamed colon via PepT1); topical (inflammatory skin conditions, wound healing). Iontophoresis can enhance topical penetration.

Cycle Length

4–8 week cycles (subcutaneous); continuous for IBD management.

Note: Oral administration with or without food. Empty stomach may enhance absorption. Refrigerate at 2–8°C, protect from light. Reconstituted vials use within 30 days. Lyophilized form stable at room temperature for weeks. Oral KPV is highly experimental with limited human data — bioavailability and optimal dosing in humans not established.

Monitoring & Risk Management

Monitoring guidelines based on available data

No Specific Monitoring Protocol

No structured monitoring data is available for this compound. Always consult a healthcare professional before use.

Health & Research Goals

KPV

KPV