Endocrine

Kisspeptin

Kisspeptin is the name for the family of peptides encoded by the KISS1 gene. Kisspeptin-54 (also called metastin) and the shorter kisspeptin-14, -13 and -10 share a C-terminal RF-amide end and activat...

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Certificate of Analysis included with every order.

Technical Specifications

Purity≥98%
FormLyophilized Powder
Storage-20°C

About Kisspeptin

Kisspeptin is the name for the family of peptides encoded by the KISS1 gene. Kisspeptin-54 (also called metastin) and the shorter kisspeptin-14, -13 and -10 share a C-terminal RF-amide end and activate the receptor KISS1R, formerly called GPR54.[1][2][13] Pepitiva supplies kisspeptin as a lyophilized peptide powder (10 mg vials, ≥98% purity) for in vitro and preclinical research. This product is the peptide ligand itself, not an antibody against kisspeptin or KISS1R.

Why researchers study kisspeptin

Loss-of-function mutations in the kisspeptin receptor cause hypogonadotropic hypogonadism and absent puberty in humans and mice, and an inactivating mutation in KISS1 itself causes failure of pubertal progression.[3][4][6] Kisspeptin acts directly on gonadotropin-releasing hormone (GnRH) release, which places it at the top of the reproductive hormone axis.[5]

Which kisspeptin?

Kisspeptin-54 and kisspeptin-10 behave differently in vivo, so the form matters for experimental design.[8] Check the batch Certificate of Analysis for the exact form and sequence supplied.

Regulatory status

Kisspeptin is not an approved medicine. Human studies are experimental, including a phase 2 trial in IVF, and its use as a test of hypothalamic function is still being evaluated.[9][11]

For research use only. Not for human consumption.

Quality & Storage

≥98% purity. Lyophilized Powder. Storage: -20°C. For research purposes only.

Mechanism of Action

KISS1R (GPR54) signaling

Kisspeptins bind human and rat GPR54 with low nanomolar affinity and stimulate PIP2 hydrolysis, calcium mobilization, arachidonic acid release and ERK1/2 and p38 MAP kinase phosphorylation; in cell lines they also inhibited proliferation.[2] Mutant receptors from patients with hypogonadotropic hypogonadism showed decreased inositol phosphate accumulation.[4]

Direct control of GnRH release

GPR54 transcripts colocalize with GnRH neurons in the mouse hypothalamus. Kisspeptin stimulated LH and FSH release in wild-type mice but had no effect in mice lacking GPR54, and central administration in sheep produced a dramatic release of GnRH into the cerebrospinal fluid with a parallel rise in LH.[5]

Kisspeptin-54 versus kisspeptin-10

All kisspeptins share the C-terminal decapeptide YNWNSFGLRF-NH2, which is kisspeptin-10 (C63H83N17O14, 1302.4 g/mol).[13][14] In male mice, kisspeptin-54 had a blood half-life of about 32 minutes against about 4 minutes for kisspeptin-10, sustained LH release far longer, and was the only form that activated GnRH neurons behind the blood-brain barrier after peripheral injection.[8]

Origin as a metastasis suppressor

KISS1 was first known as a gene that suppresses metastasis of human melanoma and breast carcinoma; its 54-residue product inhibited chemotaxis and invasion of receptor-expressing cells and reduced pulmonary metastasis of receptor-transfected melanoma in mice.[1]

Research Applications

Human research highlights

  • Kisspeptin-54 in men (2005): a 90-minute intravenous infusion raised LH, FSH and testosterone against saline; the plasma half-life of kisspeptin-54 was about 28 minutes.[7]
  • Oocyte maturation in IVF (2015): in a phase 2 trial of 60 women at high risk of ovarian hyperstimulation syndrome, a single kisspeptin-54 injection triggered oocyte maturation in 95% of women, and none developed moderate, severe or critical OHSS.[9]
  • Chronic kisspeptin-10 in men (2026): continuous infusion kept testosterone elevated but gonadotropins returned to vehicle levels after 5 days, while daily intermittent infusions sustained gonadotropin rises for 12 days.[10]
  • Sexual brain processing (2022): in women with hypoactive sexual desire disorder, kisspeptin-54 modulated brain responses to erotic and facial-attraction stimuli on functional MRI.[12]

Laboratory research applications

  • GnRH pulse generator and puberty: KISS1R signaling in hypothalamic neurons and pubertal onset models.[3][4][5]
  • Receptor pharmacology: Gq-coupled KISS1R signaling, calcium and MAP kinase readouts in transfected cells.[2]
  • Peptide length and pharmacokinetics: comparing kisspeptin-54 and kisspeptin-10 action and brain access.[8]
  • Hypothalamic function testing: kisspeptin as a probe of hypothalamic versus pituitary causes of hypogonadism.[11]
  • Cancer cell motility: the original metastasis-suppressor findings in receptor-expressing cells.[1]
  • Related endocrine research: the melanocortin agonist PT-141 (bremelanotide) has also been studied in hypoactive sexual desire disorder, through a different receptor system.

The human findings above are scientific background only. This product is a research-grade peptide for laboratory use and is not intended for human or veterinary use.

Storage & Handling Guidelines

Proper storage and handling are essential to maintain peptide integrity and ensure reliable research results. All Pepitiva Biolabs peptides are supplied as lyophilized (freeze-dried) powder, which provides excellent long-term stability when stored correctly. Store lyophilized peptides at -20°C for long-term storage or 2-8°C for short-term use. Once reconstituted, peptide solutions should be stored at 2-8°C and used within the timeframe specified in the product documentation. Always use sterile bacteriostatic water for reconstitution and handle peptides in a clean laboratory environment to prevent contamination. Avoid repeated freeze-thaw cycles, as thermal stress can cause peptide degradation and loss of biological activity.

Quality Control & Certification

This product is manufactured under strict quality control protocols and has been verified through comprehensive analytical testing. Each batch undergoes reverse-phase HPLC analysis for purity determination and electrospray ionization mass spectrometry (ESI-MS) for molecular identity confirmation. A detailed Certificate of Analysis (COA) is available for download, documenting purity percentage, molecular weight verification, appearance, and recommended storage conditions. Pepitiva Biolabs maintains batch-level traceability from synthesis through delivery, ensuring complete transparency and quality assurance for your research.

Frequently Asked Questions

Is this a kisspeptin antibody?

No. This product is the kisspeptin peptide itself, the natural ligand of KISS1R. Antibodies against kisspeptin or KISS1R are separate immunodetection reagents (for example for immunohistochemistry or ELISA) and are not sold here.

What is kisspeptin?

A family of peptides encoded by the KISS1 gene (kisspeptin-54, -14, -13 and -10) that activate the receptor KISS1R (GPR54) and drive GnRH release, the top step of the reproductive hormone axis.

What is the difference between kisspeptin-10 and kisspeptin-54?

Kisspeptin-10 is the shared C-terminal decapeptide (YNWNSFGLRF-NH2); kisspeptin-54 is the full-length peptide, also called metastin. In mice, kisspeptin-54 lasted much longer in blood (about 32 versus 4 minutes) and sustained LH release far longer.

What is KISS1R (GPR54)?

The G protein-coupled receptor for kisspeptins. Loss-of-function mutations in it cause hypogonadotropic hypogonadism and absent puberty in humans and mice.

Which form of kisspeptin is in this vial?

Check the batch Certificate of Analysis for the exact form and sequence supplied, since kisspeptin-10 and kisspeptin-54 differ in size and in vivo behavior.

Is kisspeptin approved as a drug?

No. Kisspeptin has been tested only in experimental human studies, such as a phase 2 IVF trial, and is not an approved medicine.

How should kisspeptin be stored?

Keep the lyophilized powder at −20 °C, protected from light and moisture.

Is this product approved for human use?

No. This product is intended exclusively for in vitro scientific research and laboratory use. It is not approved for human or veterinary use, not intended for diagnostic or therapeutic purposes, and should not be administered to humans or animals under any circumstances.

How do I reconstitute this peptide?

Add sterile bacteriostatic water slowly to the vial, directing the stream against the glass wall rather than directly onto the lyophilized powder. Gently swirl the vial until the powder is fully dissolved — do not shake vigorously. The recommended reconstitution volume depends on your desired concentration. Refer to the product documentation for specific guidance.

Can I get a Certificate of Analysis (COA)?

Yes. A Certificate of Analysis is included with every order and is also available for download from the product page. The COA documents HPLC purity, mass spectrometry identity confirmation, batch number, production date, and storage recommendations.

Scientific References

  1. Ohtaki T, Shintani Y, Honda S, et al. Metastasis suppressor gene KiSS-1 encodes peptide ligand of a G-protein-coupled receptor. Nature. 2001;411(6837):613-617. PubMed
  2. Kotani M, Detheux M, Vandenbogaerde A, et al. The metastasis suppressor gene KiSS-1 encodes kisspeptins, the natural ligands of the orphan G protein-coupled receptor GPR54. J Biol Chem. 2001;276(37):34631-34636. PubMed
  3. de Roux N, Genin E, Carel JC, et al. Hypogonadotropic hypogonadism due to loss of function of the KiSS1-derived peptide receptor GPR54. Proc Natl Acad Sci U S A. 2003;100(19):10972-10976. PubMed
  4. Seminara SB, Messager S, Chatzidaki EE, et al. The GPR54 gene as a regulator of puberty. N Engl J Med. 2003;349(17):1614-1627. PubMed
  5. Messager S, Chatzidaki EE, Ma D, et al. Kisspeptin directly stimulates gonadotropin-releasing hormone release via G protein-coupled receptor 54. Proc Natl Acad Sci U S A. 2005;102(5):1761-1766. PubMed
  6. Topaloglu AK, Tello JA, Kotan LD, et al. Inactivating KISS1 mutation and hypogonadotropic hypogonadism. N Engl J Med. 2012;366(7):629-635. PubMed
  7. Dhillo WS, Chaudhri OB, Patterson M, et al. Kisspeptin-54 stimulates the hypothalamic-pituitary gonadal axis in human males. J Clin Endocrinol Metab. 2005;90(12):6609-6615. PubMed
  8. d'Anglemont de Tassigny X, Jayasena CN, Murphy KG, Dhillo WS, Colledge WH. Mechanistic insights into the more potent effect of KP-54 compared to KP-10 in vivo. PLoS One. 2017;12(5):e0176821. PubMed
  9. Abbara A, Jayasena CN, Christopoulos G, et al. Efficacy of Kisspeptin-54 to Trigger Oocyte Maturation in Women at High Risk of Ovarian Hyperstimulation Syndrome (OHSS) During In Vitro Fertilization (IVF) Therapy. J Clin Endocrinol Metab. 2015;100(9):3322-3331. PubMed
  10. Yeung AC, Phylactou M, Koysombat K, et al. Chronic subcutaneous kisspeptin-10 stimulates gonadotropin secretion for 12 days in healthy men. Eur J Endocrinol. 2026;195(2):206-216. PubMed
  11. Pierret ACS, Patel AH, Daniels E, et al. Kisspeptin as a test of hypothalamic dysfunction in pubertal and reproductive disorders. Andrology. 2026;14(4):1002-1016. PubMed
  12. Thurston L, Hunjan T, Ertl N, et al. Effects of Kisspeptin Administration in Women With Hypoactive Sexual Desire Disorder: A Randomized Clinical Trial. JAMA Netw Open. 2022;5(10):e2236131. PubMed
  13. UniProt Q15726: Metastasis-suppressor KiSS-1 (human); peptides metastin/kisspeptin-54 (residues 68-121), kisspeptin-14, -13 and -10 (residues 112-121), C-terminal phenylalanine amide. Source
  14. PubChem. Kisspeptin-10 (human), CID 25240297: C63H83N17O14, 1302.4 g/mol. Source

Sources are peer-reviewed publications indexed in PubMed and trial registrations on ClinicalTrials.gov. Each citation was checked against its PubMed record.

For research use only. Not for human consumption.

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