KPV (10 mg)

At a Glance

KPV (Lys-Pro-Val) is a naturally occurring tripeptide — the C-terminal fragment of α-MSH — that retains the anti-inflammatory activity of the full melanocortin hormone without any melanotropic effects. Research focuses on its ability to suppress gut inflammation, accelerate wound healing, and reduce systemic inflammatory signalling. Unlike full α-MSH, KPV does not alter skin pigmentation and is well tolerated in animal models of IBD.[1]

• Reconstitute: Add 3.0 mL bacteriostatic water → 3.33 mg/mL (3,333 mcg/mL) concentration.
• Starting dose: 200 mcg once daily (6 units / 0.06 mL) subcutaneous for the first week.
• Easy measuring: At 3.33 mg/mL on a U-100 syringe, 1 unit = 0.01 mL = 33.3 mcg.
• Doses per vial: 20 doses at the 500 mcg maintenance level; use within 30 days of reconstitution.
• Storage: Lyophilised: freeze at −20 °C; reconstituted: refrigerate at 2–8 °C; use within 30 days.

Overview

• Goal: Suppress gut and systemic inflammation via inhibition of NF-κB and MAP kinase signalling, reducing TNF-α, IL-6, and IL-1β production.[1]
• Schedule: Once-daily subcutaneous injection; dose escalated weekly over 3 weeks.
• Dose range: 200 mcg (initiation) → 500 mcg (maintenance).
• Reconstitution: 3.0 mL BAC water per 10 mg vial → 3.33 mg/mL.
• Storage: Lyophilised at −20 °C; reconstituted at 2–8 °C; use within 30 days.

What You’ll Need

Plan based on an 8-week course titrated from 200 mcg to 500 mcg once daily (total ≈ 26,600 mcg / 26.6 mg).

• KPV Vials (10 mg each): 26.6 mg cumulative → 3 vials (with buffer).
• Insulin Syringes (U-100, 1 mL): 1 per injection → 56 syringes for the 8-week course.
• Bacteriostatic Water (10 mL bottles): 3.0 mL per vial → 1 × 10 mL bottle covers all three vials.
• Alcohol Swabs: 2 per injection → 112 swabs for the course.

How to Reconstitute

1. Allow frozen lyophilised vial to reach room temperature (10–15 minutes).
2. Draw 3.0 mL bacteriostatic water with a sterile syringe.
3. Inject slowly down the inner vial wall; do not inject directly onto the powder cake.
4. Gently swirl or roll until fully dissolved — do not shake. Solution should be clear and colourless.
5. Label with reconstitution date; refrigerate at 2–8 °C. Use within 30 days.

Dosing Schedule

Frequency: Inject once daily subcutaneously. Gradual titration over the first three weeks helps establish tolerability before reaching the 500 mcg maintenance dose. At 500 mcg/day, a 10 mg vial (3.33 mg/mL, 3.0 mL total) yields 20 doses. Doses are calculated at 33.3 mcg per unit for convenient measurement on a standard U-100 insulin syringe.[2]

Protocol Details

• Week 1: 200 mcg (6 units / 0.06 mL) once daily — initiation and tolerability.
• Week 2: 300 mcg (9 units / 0.09 mL) once daily.
• Week 3: 400 mcg (12 units / 0.12 mL) once daily.
• Weeks 4–8: 500 mcg (15 units / 0.15 mL) once daily — maintenance.[2]
• Injection site: Abdomen, thigh, or upper arm. Rotate sites between injections.

Storage

• Lyophilised: Store at −20 °C (−4 °F) or below; protect from moisture and light.
• Reconstituted: Refrigerate at 2–8 °C. Do not freeze. Use within 30 days.
• Appearance: Clear and colourless. Discard if cloudy, coloured, or particulate.

How KPV Works

KPV is the C-terminal tripeptide (Lys-Pro-Val) of α-melanocyte-stimulating hormone (α-MSH). While full α-MSH exerts its anti-inflammatory effects primarily through MC1R signalling, KPV appears to work through both melanocortin receptor-dependent and receptor-independent mechanisms. Critically, KPV inhibits nuclear factor-kappa B (NF-κB) activation — the master transcription factor governing pro-inflammatory cytokine production — and suppresses MAP kinase signalling pathways, reducing downstream expression of TNF-α, IL-6, and IL-1β.[1]

In experimental colitis models, KPV reduces macrophage infiltration and epithelial barrier disruption. A key pharmacological advantage is that KPV enters inflamed intestinal epithelial cells via the PepT1 transporter — a di/tripeptide uptake system that is up-regulated in inflammatory bowel disease — making the gut lumen itself a preferential site of KPV accumulation during active inflammation.[2][3] This biology underpins efforts to develop oral and nanoparticle-based KPV delivery systems for Crohn’s disease and ulcerative colitis.

Good to Know

• KPV is a tripeptide with a very small molecular weight (≈340 Da) and is absorbed via the intestinal PepT1 di/tripeptide transporter — which means oral and nanoparticle-encapsulated formulations are actively investigated for IBD.[3]
• Unlike full α-MSH, KPV does not activate MC1R in melanocytes and therefore does not cause skin darkening or melanotropic side effects.
• If GI side effects (nausea, loose stool) occur during titration, hold at the current dose for an additional week before advancing.
• KPV has no known melanotropic activity, but it does bind MC3R and MC5R in addition to showing NF-κB inhibition via non-receptor cytoplasmic mechanisms.[1]
• Mild injection site redness or swelling is the most commonly reported side effect in animal studies; this typically resolves within 24 hours.
• IBD & colitis (animal data): KPV significantly reduced macroscopic and histological colitis scores in murine DSS- and TNBS-induced colitis models, outperforming vehicle controls on inflammatory markers.[2]
• Oral delivery feasibility: Nanoparticle-encapsulated KPV administered orally reduced colitis severity in mice, demonstrating gut epithelial absorption via PepT1 even at low doses.[3]
• Wound healing (animal data): Topical and subcutaneous KPV reduced wound-induced inflammatory cytokines and accelerated healing in murine wound models.[4]
• No melanotropic activity: No skin pigmentation changes observed in any published animal study, differentiating KPV from full α-MSH.
• Side effects: Mild, transient injection site reactions are the predominant reported effect; no systemic toxicity at studied doses in rodent models.
• Human data: No published human clinical trial data exist for subcutaneous KPV. All efficacy conclusions are extrapolated from preclinical models.
• For background on KPV's mechanism, evidence, and safety profile, see What Is KPV?.

Tips for Best Results

• For gut-focused research protocols, some researchers administer KPV 30–60 minutes before meals to align peptide absorption with active PepT1 upregulation in the gut epithelium.
• Minimise dietary triggers of gut inflammation (ultra-processed foods, alcohol, NSAIDs) during the protocol to avoid confounding KPV’s anti-inflammatory effects.
• If stacking with BPC-157 for gut repair protocols, consider alternating injection sites and timing — both peptides are well tolerated in animal models when combined.[2]
• Track gut symptom severity (frequency, urgency, stool consistency) with a daily log to assess response across the titration phase.
• Refrigerate reconstituted vials promptly and adhere to the 30-day use window — tripeptides are stable but not indefinitely so.

Injection Tips

• Clean the vial stopper and injection site with separate alcohol swabs; allow both to air-dry fully before proceeding.
• Using a 29–31 gauge insulin syringe (5/16″ to 1/2″ needle), draw the calculated dose precisely.
• Pinch a fold of skin and insert the needle at 45° into subcutaneous fat (90° is acceptable with a short needle into a well-pinched fold).
• Inject slowly over 2–3 seconds; do not aspirate. Withdraw the needle, apply gentle pressure, and do not rub the site.
• Rotate injection sites (abdomen, thighs, upper arms) and dispose of each syringe in a sharps container immediately after use.