KPV - 5MG

KPV – 5MG

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KPV Peptide

KPV (Lys–Pro–Val) is a tripeptide derived from the C-terminus of α-MSH with potent anti-inflammatory and mucosal-healing actions. KPV primarily inhibits NF-κB and MAPK signaling, lowering pro-inflammatory cytokine secretion in epithelial and immune cells. It is actively transported via PepT1, which is upregulated in the inflamed colon—focusing activity to diseased tissue.[1]

Mechanism & Cellular Uptake

  • Suppresses NF-κB/MAPK pathways → ↓ TNF-α, IL-1β, other cytokines in gut epithelium and immune cells.[1,2,4,5]
  • PepT1-mediated entry enhances epithelial uptake during IBD flares (PepT1 upregulated).[1]
  • Anti-inflammatory activity partly melanocortin-receptor independent → minimal pigmentary effects versus α-MSH.[2,4,5]

Efficacy in Colitis & Mucosal Healing

  • DSS/TNBS colitis (mice): oral/rectal KPV ↓ histologic inflammation, cytokines, and MPO; improves weight recovery and mucosal repair.[1–3]
  • Oral mucositis: mucoadhesive KPV hydrogels reduce inflammation/bacterial burden and promote epithelial repair.[6]

Broader Anti-Inflammatory Applications

  • Peritonitis and other sterile inflammation models: ↓ neutrophil infiltration and pro-inflammatory mediators.[4]
  • Vascular disease: carrier-free KPV nanodrugs show anti-inflammation and anti-calcification effects in preclinical models.[8]

Formulation & Delivery

  • Hydrogel encapsulation improves peptide stability, mucosal retention, and in vivo efficacy in colitis.[3,6]
  • Transdermal strategies (iontophoresis/microneedles, microporated skin) enable enhanced delivery across human skin.[7]

Safety

  • KPV and derivatives (e.g., (CKPV)2) show a favorable preclinical safety profile with no significant cytotoxicity or pigmentary effects reported.[2,4,5,9]

Key Takeaways

  • Targeted gut delivery: PepT1-guided epithelial uptake concentrates action in inflamed colon.
  • Multi-pathway anti-inflammation: NF-κB/MAPK inhibition plus cytokine reduction and epithelial repair.
  • Translational flexibility: oral/rectal hydrogels and transdermal systems broaden therapeutic options.

References

  1. Dalmasso G, Charrier-Hisamuddin L, Nguyen HT, et al. Gastroenterology. 2008;134(1):166-178. doi:10.1053/j.gastro.2007.10.026.[1]
  2. Kannengiesser K, Maaser C, Heidemann J, et al. Inflamm Bowel Dis. 2008;14(3):324-331. doi:10.1002/ibd.20334.[2]
  3. Sun J, Xue P, Liu J, et al. ACS Biomater Sci Eng. 2021;7(10):4859-4869. doi:10.1021/acsbiomaterials.1c00792.[3]
  4. Getting SJ, Schiöth HB, Perretti M. J Pharmacol Exp Ther. 2003;306(2):631-637. doi:10.1124/jpet.103.051623.[4]
  5. Brzoska T, Böhm M, Lügering A, et al. Adv Exp Med Biol. 2010;681:107-116. doi:10.1007/978-1-4419-6354-3_8.[5]
  6. Shao W, Chen R, Lin G, et al. Biomater Sci. 2021;10(1):227-242. doi:10.1039/d1bm01466h.[6]
  7. Pawar K, Kolli CS, Rangari VK, Babu RJ. J Pharm Sci. 2017;106(7):1814-1820. doi:10.1016/j.xphs.2017.03.017.[7]
  8. Zhang L, Li D, Aierken Y, et al. Adv Healthc Mater. 2024;13(32):e2402320. doi:10.1002/adhm.202402320.[8]
  9. Gatti S, Carlin A, Sordi A, et al. J Surg Res. 2006;131(2):209-214. doi:10.1016/j.jss.2005.08.009.[9]

All information provided is for research purposes only.

All COA’s available upon request: info@truformlabs.com

All information provided is for research purposes only.

Storage & Handling (Research Use)

  • Lyophilized powder: Store sealed at −20 °C to −80 °C (desiccated, light-protected). Short-term (≤2–3 weeks) at 2–8 °C is acceptable.
  • After reconstitution: Store at 2–8 °C and use within 7 days, or aliquot and freeze at −20 °C to −80 °C for ≤3 months.
  • Handling: Prepare small aliquots to avoid freeze–thaw; keep on ice during prep; minimize air/light exposure.
  • Vehicle & pH: Reconstitute per lot guidance (e.g., sterile saline/BWFI) near pH 7.0–7.4; avoid reactive metals/oxidants.
  • Labeling: Record concentration, solvent, and prep date; follow lab SOPs and lot-specific stability notes.

All information provided is for research purposes only.