Kisspeptin-10 Research Information

GPR54 (KISS1R) Agonist

For Reproductive & Metabolic Research

⚠️ Important: This information is for educational and research purposes only. Always consult with a qualified healthcare professional before use.

📑 Contents

🔬 What is Kisspeptin-10?

Kisspeptin-10 (KP-10) is a synthetic decapeptide (YNWNSFGLRF-NH₂) that represents the C-terminal 10-amino acid sequence of the naturally occurring neuropeptide kisspeptin and is the minimal pharmacophore sufficient for full KISS1R (GPR54) activation. It is derived from the 145-amino acid KISS1 gene product, which is enzymatically cleaved into various kisspeptin isoforms including KP-10, KP-13, KP-14, and KP-54.

Initially characterized as a metastasis suppressor, kisspeptin is now recognized as the master regulator of the hypothalamic-pituitary-gonadal (HPG) axis, playing an essential role in puberty onset and reproductive function. Kisspeptin-10 binds to KISS1R with high affinity (Ki = 0.042 nM, ~8-fold higher than KP-54) and exhibits potent gonadotropin-releasing hormone (GnRH) stimulation. KP-10 is available in pen and freeze-dried vial formulations for research purposes.

⚡ How Kisspeptin-10 Works

Kisspeptin-10 works through multiple mechanisms to influence reproductive and metabolic physiology:

Kisspeptin-10 exhibits a very short plasma half-life of approximately 3.3 to 4 minutes in humans and 4 minutes in mice, enabling rapid, transient LH elevation that returns to baseline within approximately 1 hour. This makes KP-10 valuable for studying acute, pulsatile GnRH/LH dynamics. KP-10 is not able to cross the blood-brain barrier following peripheral administration, in contrast to the longer isoform KP-54.

📋 Research Applications

📊 Clinical Studies

Metabolic Effects in Obesity-Diabetes (2025)

• In female high-fat diet (HFD) mice, twice-daily intraperitoneal KP-10 (25 nmol/kg) for 21 days decreased body weight, blood glucose, and energy intake to normal diet control levels
• KP-10 significantly (p < 0.05–0.01) decreased body weight and non-fasting blood glucose on days 7, 14, and 22
• By the end of the study, body weight and blood glucose were nearly identical in KP-10-treated HFD and healthy control mice
• KP-10 increased beta-cell proliferation with no alteration in beta-cell apoptosis
• Increased GIP-positive cells in ileum and restored relative insulin area to normal levels

Pharmacokinetics & Half-Life Studies

• KP-10 has a plasma half-life of approximately 3.3 to 4 minutes in humans
• In mice, KP-10 half-life is approximately 4 minutes, compared to ~32 minutes for KP-54
• Peak plasma KP-10 concentrations are observed 30 minutes after commencing intravenous infusion
• Plasma kisspeptin-IR falls nearly ten-fold within 30 minutes of cessation of infusion
• In vitro degradation half-lives: 6.8 min at 4°C, 2.9 min at 25°C, 1.7 min at 37°C

Sexual Dimorphism & Clinical Implications

• KP-10 robustly stimulates gonadotropin release in men but fails to stimulate gonadotropin release in healthy female volunteers in the follicular phase when administered by IV bolus, SC bolus, or IV infusion
• This reveals sexual dimorphism in responsiveness to KP-10 administration, with important clinical implications for potential therapeutic use
• Central administration of KP-10 decreased food intake in male mice (~50%), while increasing locomotor activity in female mice (>65%)
• Peripheral administration of KP-10 failed to alter any metabolic parameters analyzed except for small effects on locomotor activity and food intake, denoting a predominant central role in energy metabolism control

Triple-Negative Breast Cancer (2025)

• KP-10 treatment significantly reduced cell viability and migration in TNBC cell lines (IC₅₀: 110.21 nM for MDA-MB-231, 88.35 nM for MDA-MB-468)
• Induced dose-dependent upregulation of KISS1 mRNA, suggesting a positive feedback loop
• Modulated key transcription factors: upregulated GATA2, CDX2, and FLI1 while downregulating ZEB1
• EMT reversal evident from increased E-cadherin and β-catenin, reduced N-cadherin, CD44, and Vimentin
• Pro-apoptotic genes CASP3, CASP8, CASP9, and BAX were upregulated, while BCL2 was suppressed

Critical Research Considerations

• KP-10 is not able to cross the blood-brain barrier after peripheral administration, in contrast to KP-54
• KP-54 sustains LH release longer than KP-10, with repeated KP-10 dosing failing to reproduce KP-54's sustained LH profile
• Intravenous bolus doses of KP-10 ranging from 0.3–10 nmol/kg are associated with similar degrees of gonadotrophin secretion in healthy male subjects

💉 Interactive Dosing Guide

Select your vial size and dose to see the corresponding volume, clicks, dosing frequency, and how many doses per vial:

⚠️ Safety & Precautions

Kisspeptin-10 has shown a favorable safety profile in clinical studies with no dose-limiting toxicities or serious adverse events reported. However, human data is limited and KP-10 is not FDA-approved.

• Injection site reactions: Mild redness or tenderness at injection site
• Rapid degradation: Extremely short half-life minimizes systemic exposure
• Temperature-sensitive: Degrades rapidly at ambient temperature (t₁/₂ = 2.9 min at 25°C)
• No FDA approval: Investigational research compound only

Important Safety Considerations:

• KP-10 is not FDA-approved for any indication
• Sexual dimorphism in responsiveness: women in follicular phase may not respond
• Not BBB-penetrant after systemic administration
• Do not use if allergic to Kisspeptin-10 or any ingredients
• Do not use if pregnant or breastfeeding

📚 References

• Kisspeptin-10 Ameliorates Obesity-Diabetes with Diverse Effects on Ileal Enteroendocrine Cells and Pancreatic Islet Morphology. Biomolecules. 2025;15(11):1591.
• Exogenous kisspeptin-10 treatment shows pleiotropy via induction of KISS1 expression, metastasis suppression, and promotes apoptosis in triple-negative breast cancer. Scientific Reports. 2025;15:35182.
• LC–MS/MS quantification of kisspeptin-10 and characterization of its decomposition product and pharmacokinetics in rats. J Chromatogr B. 2013.
• Kisspeptins centrally modulate food intake and locomotor activity in mice. J Neuroendocrinol. 2024;36(10).
• Mechanistic insights into the more potent effect of KP-54 compared to KP-10 in vivo. PLoS One. 2017;12(5).
• Kisspeptin-10 Technical Guide. Benchchem. 2026.

This information is for educational and research purposes only. Always consult with a qualified healthcare professional.

Last updated: July 2026