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Kisspeptin-10

Hormonal Axis
KP-10Metastin(112-121)

Overview

Kisspeptin-10 (KP-10), also known as Metastin(112-121), is a decapeptide derived from the larger kisspeptin protein, which is encoded by the KISS1 gene. It is a key regulator of the reproductive hormonal axis, particularly influencing the release of gonadotropin-releasing hormone (GnRH). KP-10 is synthesized as part of a larger precursor protein and is cleaved to its active form. The structure of KP-10 consists of a sequence of 10 amino acids, making it a relatively small peptide with significant biological activity. Researchers have primarily focused on KP-10's role in reproductive biology and its potential therapeutic applications. It has been observed to stimulate the release of GnRH, thereby influencing the secretion of luteinizing hormone (LH) and follicle-stimulating hormone (FSH). These effects have implications for fertility treatments and the management of reproductive disorders. Additionally, KP-10 has been investigated for its role in cancer metastasis, as it was initially discovered in the context of its ability to suppress tumor spread. The mechanism of action of KP-10 involves binding to the G-protein coupled receptor GPR54, also known as the kisspeptin receptor. This interaction triggers a cascade of intracellular signaling pathways that ultimately lead to the release of GnRH from the hypothalamus. The activation of GPR54 is crucial for the initiation of puberty and the maintenance of reproductive function. Pharmacokinetic studies of KP-10 indicate that it has a relatively short half-life, with rapid degradation in the bloodstream. Its stability and bioavailability can vary depending on the route of administration, with subcutaneous and intravenous routes being more effective than oral administration due to poor bioavailability. Current research on KP-10 is focused on its potential therapeutic applications in reproductive health and oncology. However, it is not yet approved as a medicinal product by major regulatory agencies, and its use is primarily confined to research settings.

Mechanism of Action

Kisspeptin-10 exerts its effects by binding to the GPR54 receptor, a G-protein coupled receptor. This interaction activates intracellular signaling pathways that lead to the release of gonadotropin-releasing hormone (GnRH) from the hypothalamus, influencing the reproductive hormonal axis.

Molecular Data

FormulaC63H83N17O14
Molecular Weight1302.4 g/mol
CAS Number374675-21-5
PubChem CID25240297

Half-Life

SubcutaneousData limited
Intravenous~30 minutes
OralPoor bioavailability

KP-10 is rapidly degraded in the bloodstream, limiting its half-life and necessitating specific routes of administration for effective delivery.

Storage

Lyophilized

Stable for 2+ years at -20°C, 12 months at 4°C

Reconstituted

Use within 14 days when refrigerated at 4°C

Avoid

Avoid repeated freeze-thaw cycles, direct light

Solvent

Bacteriostatic water or sterile saline recommended

Solubility

Kisspeptin-10 is soluble in water and DMSO.

Legal Status

🇩🇪DE

Not approved as a medicinal product. Not a controlled substance. Sale as research chemical is a legal grey area.

🇺🇸US

Not approved by the FDA as a medicinal product. Not scheduled by the DEA.

🇦🇺AU

Not listed on the TGA schedule.

🇬🇧UK

Not approved by the MHRA as a medicinal product.

Legal status information is provided for general reference only and may not reflect the most current regulatory changes. Always verify with official government sources before making any decisions.

9 Research Publications

Kisspeptin isoforms: versatile players in reproduction and beyond.

Review

Journal of molecular endocrinology · 2025

Researchers reviewed the various forms of kisspeptin, a key hormone involved in reproduction, and its receptor. They found that kisspeptin plays important roles not only in regulating reproductive hormones but also in metabolic processes and potential therapeutic applications. The study highlights the structural diversity of kisspeptin isoforms and their implications for future research.

  • Kisspeptin is crucial for regulating the reproductive hormone system in mammals.
  • The study identified four kisspeptin isoforms, with Kp-10 being the most active form.
  • Kisspeptin has potential roles beyond reproduction, including metabolic regulation and therapeutic uses.
PubMed

Kisspeptin-10 Protects Against TNF-α-Induced Chondrocyte Senescence via the SIRT1/p53/p21 Signaling.

In Vitro

Journal of biochemical and molecular toxicology · 2025

Researchers studied the effects of a peptide hormone called Kisspeptin-10 on chondrocytes, which are cells important for cartilage health, in the context of osteoarthritis. They found that Kisspeptin-10 can reduce cellular aging caused by inflammation, potentially improving cartilage function.

  • Researchers observed that Kisspeptin-10 reduced signs of cellular aging in chondrocytes exposed to inflammatory signals.
  • The study found that Kisspeptin-10 restored the expression of a key protein, SIRT1, which is important for cellular health.
  • Kisspeptin-10 was shown to influence important pathways related to aging, suggesting its potential as a therapeutic strategy for osteoarthritis.
PubMed

[Not Available].

Human

Biomedical chromatography : BMC · 2024

Researchers studied kisspeptin-10, a hormone that can boost levels of important reproductive hormones in humans, which raises concerns about its potential misuse in sports. They successfully developed a testing method to detect kisspeptin-10 in urine, which is now on the World Anti-Doping Agency's prohibited list for 2024.

  • Researchers found that kisspeptin-10 increases levels of follicle-stimulating hormone, luteinizing hormone, and testosterone in humans.
  • The study validated a new testing procedure for detecting kisspeptin-10 in urine, enhancing sensitivity by mimicking its metabolism in human serum.
  • Analysis of a black-market kisspeptin-10 sample revealed it had degraded more than a standard reference, but contained no unexpected impurities.
PubMed

Kisspeptin-10 binding to Gpr54 in osteoclasts prevents bone loss by activating Dusp18-mediated dephosphorylation of Src.

Animal

Nature communications · 2024

Researchers observed that a protein called Kisspeptin-10 can help prevent bone loss by interacting with a receptor in bone cells known as GPR54. This interaction activates a process that reduces the activity of a key enzyme involved in bone breakdown. The study suggests that targeting this pathway could be a potential strategy to combat age-related bone loss.

  • Kisspeptin-10 activates the GPR54 receptor, which helps regulate bone cell activity.
  • The activation of GPR54 leads to a reduction in the activity of Src, an enzyme linked to bone loss.
  • Mice lacking components of this pathway showed increased bone loss, highlighting its importance in bone health.
PubMed

Kisspeptin-10 Mitigates α-Synuclein-Mediated Mitochondrial Apoptosis in SH-SY5Y-Derived Neurons via a Kisspeptin Receptor-Independent Manner.

Unknown

International journal of molecular sciences · 2023

Researchers found that kisspeptin-10, a neurohormone, can protect certain neurons from damage caused by a protein linked to neurodegenerative diseases. This protective effect occurs independently of its usual receptor, suggesting a novel mechanism of action. The study highlights the potential of kisspeptin-10 in mitigating neuron death associated with conditions like Parkinson's disease.

  • Kisspeptin-10 significantly reduced neuron death caused by the α-synuclein protein in engineered neurons.
  • The protective effects of kisspeptin-10 were observed even when its receptor was blocked, indicating a receptor-independent mechanism.
  • Treatment with kisspeptin-10 decreased the presence of harmful proteins associated with neurodegeneration in affected neurons.
PubMed

Safety Evaluation of KP-10 (Metastin 45-54) Following once Daily Intravenous Administration for 14 Days in Dog.

Human

International journal of toxicology · 2021

Researchers studied the safety of a compound called KP-10, which may help with reproductive issues, by administering it to dogs daily for 14 days. They found no signs of toxicity or adverse effects, indicating that KP-10 has a favorable safety profile.

  • No drug-related toxicity was observed in clinical signs, body weights, or other health measures.
  • Luteinizing hormone levels peaked shortly after dosing, showing that KP-10 was effectively present in the body.
  • All dogs remained in anestrous, indicating no reproductive changes during the study period.
PubMed

Roles of the kisspeptin/GPR54 system in pathomechanisms of atherosclerosis.

Review

Nutrition, metabolism, and cardiovascular diseases : NMCD · 2020

Researchers observed that kisspeptin-10 (KP-10) and its receptor GPR54 play significant roles in the development of atherosclerosis, a condition characterized by plaque buildup in arteries. The study highlights how KP-10 affects various cellular processes that may contribute to plaque instability and progression.

  • KP-10 suppresses the movement and growth of certain blood vessel cells while increasing their aging.
  • KP-10 enhances the adhesion of immune cells to blood vessel cells and promotes inflammation.
  • The presence of KP-10 may lead to the worsening of atherosclerotic plaques, suggesting it could be a target for new treatments.
PubMed

KISS1 in breast cancer progression and autophagy.

Review

Cancer metastasis reviews · 2019

Researchers reviewed the role of the KISS1 protein in breast cancer progression. They found that KISS1 is often reduced in metastatic tumors and may play a complex role in cancer cell behavior, potentially serving as a marker for cancer progression and a target for new therapies.

  • KISS1 is a tumor suppressor protein that is typically downregulated in metastatic breast cancer.
  • The protein may help prevent the spread of cancer cells to other organs and is involved in processes like tumor blood vessel formation and cell death.
  • KISS1 shows promise as a potential diagnostic marker for cancer progression and a target for new anti-cancer treatments.
PubMed

GPR54 and kisspeptin in reproduction.

Review

Human reproduction update · 2006

Researchers reviewed the role of kisspeptins, proteins linked to the GPR54 receptor, in regulating puberty and reproductive functions. They found that these proteins are crucial for activating reproductive hormones and are influenced by factors like sex hormones and metabolism.

  • Researchers observed that mutations in the GPR54 gene can lead to delayed puberty and reproductive issues in humans.
  • The study highlighted that kisspeptins are powerful stimulators of reproductive hormone activity across various species.
  • Researchers found that the KiSS-1/GPR54 system plays a key role in activating neurons that control reproductive hormone release during puberty.
PubMed

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This page is for informational and research purposes only. All information is based on published scientific literature. Nothing on this page constitutes medical advice or replaces consultation with a qualified healthcare professional.