Kisspeptin-10

clinical trials

Also known as: KP-10, Metastin fragment

Kisspeptin-10 (KP-10), a decapeptide fragment of the metastin/kisspeptin-1 protein, acts as a potent agonist at the KISS1 receptor (KISS1R, GPR54). Its primary mechanism involves direct activation of hypothalamic gonadotropin-releasing hormone (GnRH) neurons, thereby serving as an upstream regulator of the entire reproductive hormone axis. By stimulating pulsatile GnRH secretion, KP-10 indirectly promotes luteinizing hormone (LH) and follicle-stimulating hormone (FSH) release from the anterior pituitary, making it a critical modulator of puberty onset, fertility, and gonadal function. Key research findings from clinical trials demonstrate that exogenous KP-10 administration robustly elevates LH and, to a lesser extent, FSH levels in healthy adults, with effects dependent on dose and route of administration. Studies have shown its utility in diagnosing and treating hypothalamic amenorrhea, hypogonadotropic hypogonadism, and certain forms of infertility, as it can restore endogenous GnRH pulsatility. Additionally, KP-10 has been investigated for its role in metabolic regulation, with evidence linking kisspeptin signaling to energy balance and glucose homeostasis, though these applications remain exploratory. Clinically, KP-10 is being evaluated as a diagnostic tool for assessing hypothalamic-pituitary-gonadal axis integrity and as a therapeutic agent for conditions characterized by impaired GnRH secretion, such as functional hypothalamic amenorrhea. Its rapid onset and short half-life offer advantages over traditional gonadotropin therapies, though further trials are needed to establish optimal dosing, safety, and long-term efficacy. For research purposes only — not medical advice.

Key data

Category
Sexual Health
Molecular weight
1302.4 g/mol
Molecular formula
C63H83N17O14
CAS number
374675-21-5
Administration
subcutaneous, intravenous
Research status
clinical trials
References
312
Tags
gnrh, reproductive, kiss1r

Research & studies

Kisspeptin-10 Ameliorates Obesity-Diabetes with Diverse Effects on Ileal Enteroendocrine Cells and Pancreatic Islet Morphology in High-Fat Fed Female Mice
Biomolecules · 2025 · PubMed
Kisspeptin-10 Preserves the Blood-Brain Barrier's Integrity Post-Stroke by Augmenting Claudin-10 Expression
Clinical and experimental pharmacology & physiology · 2025 · PubMed
Kisspeptin-10 Protects Against TNF-α-Induced Chondrocyte Senescence via the SIRT1/p53/p21 Signaling
Journal of biochemical and molecular toxicology · 2025 · PubMed

Kp-10 ameliorated TNF-α-induced senescence in chondrocytes, reducing SA-β-gal staining and increasing telomerase activity.; Kp-10 modulated expression of hTERT and TERF2, and suppressed the p53/p21 pathway.; Kp-10 restored SIRT1 expression, which was downregulated by TNF-α.; Silencing SIRT1 abolished Kp-10's protective effects, indicating SIRT1 is essential for its anti-senescence action.

Kisspeptin-10 Prevents the Development of Cerebral Aneurysms by Reducing the Expression of Egr-1
CNS neuroscience & therapeutics · 2025 · PubMed

KP-10 levels were reduced in both cerebral aneurysm patients and mouse models.; KP-10 reduced cerebral aneurysm size in wild-type mice but not in Gpr54 knockout mice.; KP-10 inhibited Ang II-induced proliferation, tube formation, and VEGF-A expression in HBMVECs by reducing Egr-1.; The effects of KP-10 were dependent on Gpr54, as they were abolished in Gpr54 knockdown conditions.

Author Correction: Kisspeptin-10 binding to Gpr54 in osteoclasts prevents bone loss by activating Dusp18-mediated dephosphorylation of Src
Nature communications · 2024 · PubMed
Investigating the detection of the novel doping‐relevant peptide kisspeptin‐10 in urine using liquid chromatography high‐resolution mass spectrometry
Biomedical chromatography : BMC · 2024 · PubMed

A screening and confirmation procedure for kisspeptin-10 in urine was successfully validated using LC-MS.; Four metabolites (y9, y8, y7, y5) were identified from serum incubation and included in the full-scan screening.; A degradation product from tryptophan oxidation to kynurenine was observed, requiring further kinetic study.; A black-market vial showed no unexpected impurities but had more degradation than the reference standard.

Comprehensive Analysis of Kisspeptin Signaling: Effects on Cellular Dynamics in Cervical Cancer
Biomolecules · 2024 · PubMed
Kisspeptin-10 binding to Gpr54 in osteoclasts prevents bone loss by activating Dusp18-mediated dephosphorylation of Src
Nature communications · 2024 · PubMed

Kp-10 binding to Gpr54 upregulates Dusp18, which dephosphorylates Src at Tyr 416.; Gpr54 recruits active Src and Dusp18 at its proline/arginine-rich C-terminal motif.; Kiss1, Gpr54, and Dusp18 knockout mice show osteoclast hyperactivation and bone loss.; Kp-10 treatment suppresses osteoclast activity and prevents bone loss in vivo.

Frequently asked questions

What is Kisspeptin-10?

Kisspeptin-10 (KP-10), a decapeptide fragment of the metastin/kisspeptin-1 protein, acts as a potent agonist at the KISS1 receptor (KISS1R, GPR54). Its primary mechanism involves direct activation of hypothalamic gonadotropin-releasing hormone (GnRH) neurons, thereby serving as an upstream regulator of the entire repro

How does Kisspeptin-10 work?

KISS1R agonist decapeptide that triggers hypothalamic GnRH release, upstream regulator of reproductive hormone axis.

What is the research status of Kisspeptin-10?

Kisspeptin-10 is currently classified as clinical trials, with 312 research references on record. This is for research purposes only and is not medical advice.

What is the molecular weight of Kisspeptin-10?

Kisspeptin-10 has a molecular weight of approximately 1302.4 g/mol (formula C63H83N17O14).

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