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PEPTIDES COLLECTIVE

Compound explainer · 14 min read

What is kisspeptin?

Written by [author]. Reviewed by [reviewer].

Updated . How we research and review.

Short answer

Kisspeptin is a family of peptide hormones cut from the KISS1 gene product. Every form activates the kisspeptin receptor (KISS1R, first called GPR54), which switches on GnRH release from the hypothalamus. [1] Kisspeptin-10 is the shortest active form, a 10-amino-acid peptide. Small controlled studies gave it to healthy men and women to measure LH, FSH and testosterone. [2]

What is kisspeptin?

Kisspeptin is an endogenous peptide hormone encoded by the KISS1 gene. Cells make a 145-residue precursor and cleave it into kisspeptin-54, -14, -13 and -10. The shared C-terminal decapeptide carries the activity, and kisspeptin-10, the smallest isoform, is reported to activate the receptor fully. [1]

The molecule began as a cancer gene. In 1996 a Pennsylvania State University group in Hershey isolated a gene they called KiSS-1 from melanoma cells whose ability to metastasise had been suppressed. [8] The Society for Endocrinology's patient site says the name honours the chocolate Kisses made in Hershey. [9] In 2001 Takeda scientists isolated the 54-residue peptide from human placenta and named it metastin. [10] The same year a Brussels group isolated the 54, 14 and 13-residue forms and named them kisspeptins. [11] Kisspeptin-10 still carries the synonym metastin 45-54 from that period. [3]

Research vials sold as kisspeptin, ours included, are listed as kisspeptin-10. The certificate's mass result confirms which form a vial holds. Kisspeptin in 10mg vials is in stock with a batch certificate.

How does kisspeptin work?

Kisspeptin binds KISS1R, a G protein-coupled receptor, and drives the hypothalamus to release gonadotrophin-releasing hormone (GnRH). GnRH then stimulates the pituitary to release luteinising hormone (LH) and follicle-stimulating hormone (FSH). [9] Imperial College researchers describe kisspeptin-10 and kisspeptin-54 as hormones that stimulate endogenous GnRH secretion from the hypothalamus. [12]

The receptor pharmacology comes from 2001. The Brussels group reported that the kisspeptins bound rat and human GPR54 with low nanomolar affinities and triggered calcium mobilisation and MAP kinase signalling in cultured cells. [11] A 2015 review adds that the different kisspeptins bind the receptor with equal efficacy. [13]

Where it acts matters for how researchers read their results:

  • Two hypothalamic populations. Kisspeptin neurons sit in the arcuate and anteroventral periventricular nuclei. Oestrogen feeds back negatively through the first and positively through the second. [13]
  • KNDy neurons. Arcuate neurons release kisspeptin with neurokinin B and dynorphin, and are nicknamed KNDy ("candy"). [9]
  • Genetic proof. In 2003 two groups found that loss-of-function mutations in GPR54 cause hypogonadotropic hypogonadism. [14][15] Gpr54-deficient mice showed the same picture and still responded to GnRH. [15] A 2008 review calls the receptor an "indisputable gatekeeper" of reproductive function. [16]

The genetics are the strongest part of the kisspeptin story. They show the receptor is required for normal puberty in people. They say nothing about what an added peptide does over time.

What is the structure of kisspeptin?

Kisspeptin-10 is a linear decapeptide, Tyr-Asn-Trp-Asn-Ser-Phe-Gly-Leu-Arg-Phe, with an amidated C-terminus. PubChem's systematic synonym spells it out as L-tyrosyl-L-asparaginyl-L-tryptophyl-L-asparaginyl-L-seryl-L-phenylalanyl-glycyl-L-leucyl-L-arginyl-L-phenylalaninamide. [3]

FieldKisspeptin-10Kisspeptin-54
CAS number374675-21-5388138-21-4
PubChem CID2524029771306396
Molecular formulaC63H83N17O14C258H401N79O78
Molar mass1302.4 g/mol5857 g/mol
Monoisotopic mass1301.63 DaNot recorded here
SequenceYNWNSFGLRF-NH254 residues ending in the same ten
Length10 amino acids54 amino acids
C-terminusAmideAmide
Other namesMetastin 45-54, KP-10, NSC 741805Metastin

The kisspeptin-10 column comes from PubChem [3] and the kisspeptin-54 column from its separate PubChem record. [17] We checked each value on 29 September 2026. Counted from the full 145-residue precursor, kisspeptin-10 is residues 112 to 121. [18]

Two details are worth knowing before you handle a vial. First, the two forms differ by more than 4,500 g/mol, so a mass spectrometry result separates them at a glance. Second, the sequence holds a tryptophan at position 3 and asparagines at positions 2 and 4, residues that matter for storage (covered below).

What has research on kisspeptin examined?

Kisspeptin has been examined in cell and animal work, human genetics and small human physiology studies. In the studies reviewed here, the human pharmacology came from groups in Edinburgh and London, and the larger trials used kisspeptin-54. The longest kisspeptin-10 exposure in people ran 22.5 hours. [2]

YearStudy (PMID)ModelWho was studiedReported finding
1996KiSS-1 discovery (8944003)Human melanoma cellsCell linesKiSS-1 expressed only in non-metastatic melanoma cells; highest tissue expression in placenta [8]
2001Metastin (11385580)Cells, micePlacental extract, transfected cells54-residue amidated peptide identified as the receptor's ligand [10]
2003GPR54 genetics (14573733)Humans, miceFamilies with absent puberty; knockout miceReceptor mutations cause hypogonadotropic hypogonadism [15]
2005First human kisspeptin-54 study (16174713)Human, double-blind crossover6 healthy menMean LH 10.8 against 4.2 U/L with saline [19]
2009Repeated exposure (19820030)Human, randomised double-blind10 women with hypothalamic amenorrhoea, 2 weeksLH rise of 24.0 IU/L on day 1 fell to 2.5 IU/L by day 14 [20]
2011First kisspeptin-10 study in men (21632807)HumanHealthy men, groups of 4 to 6LH rose from 4.1 to 12.4 IU/L within 30 minutes (n = 6) [2]
2011Men and women compared (21976724)HumanHealthy men and women, 4 to 5 per groupNo gonadotrophin change in women in the follicular phase; rises in men and preovulatory women [4]
2015Kisspeptin-10, kisspeptin-54, GnRH (26089302)Human, single-blindHealthy men, 5 per groupGnRH produced about 3-fold more LH than kisspeptin-10 [12]
2015IVF trial (26192876)Human, phase 2, open label60 women at high risk of ovarian hyperstimulationOocyte maturation in 95% of women; kisspeptin-54 [5]
2021Toxicology (34126799)Dogs14 days plus 14-day recoveryNo overt drug-related toxicity [21]
2025Intranasal kisspeptin-54 (40215751)Human, double-blind crossoverHealthy men and women, women with hypothalamic amenorrhoeaGonadotrophin release in all groups [22]

The 2011 Edinburgh study is the core kisspeptin-10 paper. Its authors note that kisspeptin-10 had not been studied in men before. During a continuous infusion in four men, testosterone rose from 16.6 to 24.0 nmol/L and LH pulse frequency rose from 0.7 to 1.0 pulses per hour. [2] The 2011 Imperial study found no change in LH or FSH in women studied in the follicular phase. [4]

Every finding above describes what one study reported in its own participants. None of it is a claim about a research vial.

What does the kisspeptin evidence not show?

The evidence shows that kisspeptin releases LH and FSH within minutes in controlled settings. It leaves four large gaps.

  1. The kisspeptin-10 studies are tiny. Groups held four to six people, and the 2015 comparison lists its small sample size as its main limitation. [12]
  2. Repeated exposure blunts the response. In women with hypothalamic amenorrhoea, the LH response fell by about 90% over two weeks, while the pituitary still responded to GnRH. [20] No kisspeptin-10 study tested repeated exposure in people.
  3. The response depends on sex and hormonal phase. Women in the follicular phase showed no response to kisspeptin-10 in the 2011 study. [4]
  4. Clinical use remains research. A 2025 review of IVF triggers says kisspeptin's use "remains predominantly within the research setting", limited to early-phase or highly selected studies. [23]

The cancer history is also narrower than it sounds. The metastasis-suppressor findings come from melanoma cell lines and a mouse metastasis model. [8][10] They describe the gene's discovery. No human cancer trial sits behind them in this record.

What adverse events have studies of kisspeptin reported?

The human kisspeptin-10 abstracts reviewed here (PMIDs 21632807, 21976724 and 26089302) report no adverse-event data at all. They were short hormone-response studies in healthy volunteers, and silence in an abstract is an absence of reporting.

The other published records cover different models or a different isoform:

  • Dogs, kisspeptin-10 (2021). A 14-day toxicology study with a 14-day recovery period reported no overt signs of drug-related toxicity in clinical signs, body weight, food consumption, clinical pathology, histopathology, urinalysis, ECG or respiratory rate. The highest level tested was classed as the no-observed-adverse-effect level. [21]
  • Humans, kisspeptin-54 (2025). In the intranasal crossover trial, the authors reported that no adverse events were encountered in healthy men, healthy women or women with hypothalamic amenorrhoea. [22] Kisspeptin-54 is a different molecule, so this record does not transfer to kisspeptin-10.
  • Humans, kisspeptin-54 IVF trial (2015). Among 60 women at high risk of ovarian hyperstimulation syndrome, no woman developed moderate, severe or critical ovarian hyperstimulation. [5]
  • Desensitisation (2009). Repeated kisspeptin-54 exposure reduced the LH response by day 14, a pharmacological effect the authors flagged as important for further development. [20]

These are the records the published abstracts contain. They are small, short and mostly from one group, and they describe trial conditions only.

Is kisspeptin approved or scheduled in Australia?

Kisspeptin is not named in the Poisons Standard. We searched the June 2026 instrument (F2026L00633), which commenced on 1 June 2026, for "kisspeptin" and "metastin" and found no entry. Schedule 4 runs from khellin and kitasamycin to labetalol with nothing between. [6] Its neighbours in the reproductive axis are scheduled: gonadorelin and human chorionic gonadotrophin both sit in Schedule 4. [6]

"Not named" is a narrow finding. Schedule 4 also carries a general entry for gonadotrophic hormones, [6] and the TGA states that a "research use only" label does not change whether a product is regulated as a therapeutic good. [24] Our guide to Australian peptide law and the Poisons Standard explains what each schedule means.

For sport, the answer is plain. The WADA 2026 Prohibited List, effective 1 January 2026, places "kisspeptin and its agonist analogues" in S2.2.1, testosterone-stimulating peptides in males. S2 substances are prohibited at all times, in and out of competition. [7] Anti-doping laboratories test for it: a 2026 Ghent method for 54 prohibited compounds in blood includes kisspeptin-10. [25] Some overseas explainers still say kisspeptin is absent from the List; the 2026 text names it.

How does kisspeptin compare with hCG and gonadorelin?

The three compounds act at three levels of the same axis. Kisspeptin works at the hypothalamus, gonadorelin (GnRH) at the pituitary, and hCG stands in for the LH surge at the ovary. [12][26]

FeatureKisspeptin-10Gonadorelin (GnRH)hCG
Level of actionHypothalamus, via KISS1RPituitaryGonad, as an LH substitute
Molecule10-residue peptide, 1302.4 g/molPeptide, 1182.3 g/molTwo-subunit glycoprotein
Poisons Standard (June 2026)Not namedSchedule 4Schedule 4, except pregnancy test kits
WADA 2026 ListS2.2.1, malesS2.2.1, malesS2.2.1, males

The masses come from PubChem [3][27] and the legal rows from the Poisons Standard and the WADA List. [6][7]

Two direct comparisons exist. In healthy men, GnRH produced about 3-fold more LH than kisspeptin-10 and about 2-fold more than kisspeptin-54. [12] In IVF research, a 2021 meta-analysis pooled randomised trials that compared kisspeptin, and other triggers, against conventional hCG. [26] A 2025 review notes that hCG remains the most widely used trigger and carries a significant risk of ovarian hyperstimulation. [23] Research-grade hCG and kisspeptin both sit in our hormone research peptides range.

How is kisspeptin stored and handled in the lab?

Keep lyophilised kisspeptin-10 sealed, dry, dark and frozen. No published stability study covers lyophilised research-grade kisspeptin-10, so the general peptide guidance applies: -20°C for short-term storage and -80°C for longer, away from bright light, with the vial brought to room temperature before opening. [28]

The sequence adds two specific risks. Sigma-Aldrich lists tryptophan (W) among the residues prone to air oxidation, and asparagine (N) and tryptophan among residues unstable in solution. [28] Kisspeptin-10 has one tryptophan and two asparagines. Solutions therefore deserve more care than the powder.

Biological samples show how quickly the peptide breaks down once dissolved:

  • In rat plasma, kisspeptin-10 decomposed with half-lives of 6.8, 2.9 and 1.7 minutes at 4, 25 and 37°C. The main product had lost its N-terminal tyrosine. [18]
  • In human serum and plasma, kisspeptin-10 was extensively degraded after one week at 4 and 22°C, while blood samples held stable for at least two months at -20°C. [25]

For solvents, the same guide recommends sterile distilled water or sterile dilute acetic acid (0.1%) for a stock solution, split into aliquots so you avoid repeated freezing and thawing. [28] We stock BAC Water and acetic acid in 3ml vials at A$8 each. Our peptide storage guide covers temperatures and labelling, and the reconstitution guide covers solvent choice and concentration arithmetic.

Where can researchers buy kisspeptin in Australia?

Peptides Collective sells kisspeptin for laboratory research use only, in 10mg vials from A$85. Stock ships from Western Australia with tracking.

Every batch is tested by an independent lab before it goes on sale. The certificate reports purity by HPLC and identity by mass spectrometry, and it is published under the batch number printed on the vial. Search the certificate of analysis library by that number to match the report to the vial in your hand.

Read the identity result against the structure table. A kisspeptin-10 vial should show a mass near 1302 g/mol; a value near 5857 g/mol would mean the 54-residue form. Our guide on how to read a peptide certificate of analysis explains the HPLC trace, the mass spectrum and net peptide content. The kisspeptin product page links the certificate for the current batch.

Bottom line

Kisspeptin is the KISS1-derived peptide family that sits at the top of the reproductive hormone axis, and kisspeptin-10 is its 10-residue active core. Human work shows fast LH and FSH release in small, short studies, with a blunted response on repeated exposure and no response in some women. It is not named in the Australian Poisons Standard and WADA prohibits it at all times in males. For a research vial, the batch certificate settles what is inside.

Questions

What has research on kisspeptin examined?

Research has examined kisspeptin in cells, mice, dogs and small human studies. Human work measured LH, FSH and testosterone after kisspeptin-10 in healthy men and women, and after kisspeptin-54 in women with hypothalamic amenorrhoea and in a 60-woman IVF trial. Genetic studies from 2003 linked receptor mutations to absent puberty.

What adverse events have studies of kisspeptin reported?

The human kisspeptin-10 abstracts report no adverse-event data. A 14-day dog study reported no overt drug-related toxicity. A 2025 kisspeptin-54 trial reported no adverse events encountered, and the 2015 IVF trial recorded no moderate or worse ovarian hyperstimulation. Repeated kisspeptin-54 exposure blunted the LH response within two weeks.

Which is better, hCG or kisspeptin?

No study answers "better" in general, because the two act at different levels. hCG substitutes for the LH surge at the ovary; kisspeptin acts upstream on GnRH release. In IVF research, a 2021 meta-analysis compared kisspeptin with hCG as oocyte triggers. A 2025 review calls hCG the most widely used trigger and kisspeptin still predominantly a research option.

Is kisspeptin a prescription medicine in Australia?

Kisspeptin is not named in the June 2026 Poisons Standard, so it has no schedule entry of its own. Related reproductive hormones such as gonadorelin and human chorionic gonadotrophin are Schedule 4 (prescription only). A research-use label does not change how the TGA regulates a therapeutic good.

Is kisspeptin banned in sport?

Yes, for male athletes. The WADA 2026 Prohibited List names "kisspeptin and its agonist analogues" under S2.2.1, testosterone-stimulating peptides in males, and S2 substances are prohibited at all times. The List took effect on 1 January 2026 and is revised each year, so check the current edition.

What is the half-life of kisspeptin?

The plasma half-life of kisspeptin-54 in six healthy men was 27.6 minutes. Kisspeptin-10 is cleared faster. In rat plasma it decomposed with a half-life of 1.7 minutes at 37°C, and the main product had lost its N-terminal tyrosine. The abstracts reviewed here give no human kisspeptin-10 half-life.

What is the molecular weight of kisspeptin?

PubChem lists kisspeptin-10 at 1302.4 g/mol for the formula C63H83N17O14, with a monoisotopic mass of 1301.63 Da. The 54-residue form, also filed as kisspeptin, is 5857 g/mol. Check which form a certificate describes before comparing numbers.

How should kisspeptin be stored?

Store lyophilised kisspeptin-10 sealed and away from light at -20°C short term or -80°C longer, and let the vial reach room temperature before opening. Its tryptophan and asparagine residues make solutions less stable, so freeze aliquots and avoid repeated thawing. No published study covers lyophilised research-grade kisspeptin-10 specifically.

Which solvent is used to reconstitute kisspeptin?

General peptide guidance recommends sterile distilled water or sterile dilute acetic acid (0.1%) for a stock solution. Peptides Collective stocks BAC Water, sterile water with 0.9% benzyl alcohol, and acetic acid, each in 3ml vials for A$8. Record the solvent and the resulting mg per mL concentration on the vial label.

Where does the kisspeptin sequence come from?

The sequence comes from the human KISS1 gene. Its 145-residue precursor is cleaved into kisspeptin-54, -14, -13 and -10, and all four share the C-terminal decapeptide YNWNSFGLRF-NH2. Kisspeptin-10 corresponds to residues 112 to 121 of the precursor, or 45 to 54 of metastin.

Who discovered kisspeptin?

Researchers at Pennsylvania State University in Hershey, Pennsylvania, discovered the KiSS-1 gene in 1996 as a melanoma metastasis suppressor. In 2001 Takeda scientists isolated the 54-residue peptide as metastin, and a Brussels group named the peptides kisspeptins. The name refers to Hershey's chocolate Kisses.

Is kisspeptin a peptide or a small molecule?

Kisspeptin is a peptide. Kisspeptin-10 is a linear chain of ten amino acids with an amidated C-terminus and a molar mass of 1302.4 g/mol. It is also distinct from testosterone, a steroid: studies measured testosterone as a downstream response, for example 24.9 against 21.7 nmol/L with saline after kisspeptin-54.

What is the CAS number for kisspeptin?

The CAS number for kisspeptin-10 is 374675-21-5, and its PubChem CID is 25240297. The 54-residue form has a different CAS number, 388138-21-4, under PubChem CID 71306396. Match the CAS number to the form named on the certificate.

How is kisspeptin made?

In the body, cells make kisspeptin by cleaving the 145-residue KISS1 precursor. Research kisspeptin-10 is made by chemical peptide synthesis and supplied as lyophilised powder. PubChem also lists a TFA salt of kisspeptin-10, a counter-ion form common in synthetic peptides. The batch certificate confirms identity by mass spectrometry and purity by HPLC.

Sources

  1. 1. Chakraborty AP et al. Kisspeptin isoforms: versatile players in reproduction and beyond. J Mol Endocrinol, 2025.
  2. 2. George JT et al. Kisspeptin-10 is a potent stimulator of LH and increases pulse frequency in men. J Clin Endocrinol Metab, 2011.
  3. 3. PubChem (NCBI), Kisspeptin-10, CID 25240297; PUG REST captures in research/worker/pubchem-captures.json
  4. 4. Jayasena CN et al. The effects of kisspeptin-10 on reproductive hormone release show sexual dimorphism in humans. J Clin Endocrinol Metab, 2011.
  5. 5. Abbara A 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.
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  8. 8. Lee JH et al. KiSS-1, a novel human malignant melanoma metastasis-suppressor gene. J Natl Cancer Inst, 1996.
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  10. 10. Ohtaki T et al. Metastasis suppressor gene KiSS-1 encodes peptide ligand of a G-protein-coupled receptor. Nature, 2001.
  11. 11. Kotani M 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.
  12. 12. Jayasena CN et al. Direct comparison of the effects of intravenous kisspeptin-10, kisspeptin-54 and GnRH on gonadotrophin secretion in healthy men. Hum Reprod, 2015.
  13. 13. Tng EL et al. Kisspeptin signalling and its roles in humans. Singapore Med J, 2015.
  14. 14. de Roux N et al. Hypogonadotropic hypogonadism due to loss of function of the KiSS1-derived peptide receptor GPR54. Proc Natl Acad Sci U S A, 2003.
  15. 15. Seminara SB et al. The GPR54 gene as a regulator of puberty. N Engl J Med, 2003.
  16. 16. Seminara SB et al. Kisspeptin and GPR54: discovery of a novel pathway in reproduction. J Neuroendocrinol, 2008.
  17. 17. PubChem (NCBI), Kisspeptin (54-residue form), CID 71306396
  18. 18. Liu Z et al. LC-MS/MS quantification of a neuropeptide fragment kisspeptin-10 (NSC 741805) and characterization of its decomposition product and pharmacokinetics in rats. J Chromatogr B Analyt Technol Biomed Life Sci, 2013.
  19. 19. Dhillo WS et al. Kisspeptin-54 stimulates the hypothalamic-pituitary gonadal axis in human males. J Clin Endocrinol Metab, 2005.
  20. 20. Jayasena CN et al. Subcutaneous injection of kisspeptin-54 acutely stimulates gonadotropin secretion in women with hypothalamic amenorrhea, but chronic administration causes tachyphylaxis. J Clin Endocrinol Metab, 2009.
  21. 21. Terse PS et al. Safety Evaluation of KP-10 (Metastin 45-54) Following once Daily Intravenous Administration for 14 Days in Dog. Int J Toxicol, 2021.
  22. 22. Mills EG et al. Intranasal kisspeptin administration rapidly stimulates gonadotropin release in humans. EBioMedicine, 2025.
  23. 23. Baldini GM et al. The Trigger in IVF Cycles: Molecular Pathways and Clinical Implications. Int J Mol Sci, 2025.
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  25. 25. Mazzarino M et al. Rapid and harmonized analytical workflow for the determination of peptidic and non-peptidic doping agents in dried and liquid blood matrices. Analyst, 2026.
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