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Kisspeptin receptor agonist

Kisspeptin-10

Research compoundEarly human dataPeptideIn the catalog

In short: The shortest active fragment of kisspeptin, the upstream signal for GnRH. Studied in human physiology research on reproductive hormones.

What it is

Kisspeptin-10 is a synthetic copy of the 10-amino-acid C-terminal fragment of kisspeptin, a hypothalamic neuropeptide encoded by the KISS1 gene, and is the minimal kisspeptin sequence with full intrinsic bioactivity. It appears in human reproductive endocrinology research on gonadotropin and testosterone secretion, puberty, and hypogonadism. It is an investigational compound and is not an approved medicine in any market.

How it works

Kisspeptins activate the kisspeptin receptor (KISS1R, formerly GPR54) on hypothalamic GnRH neurons, stimulating GnRH release and, downstream, LH and FSH secretion from the pituitary. Loss-of-function GPR54 mutations cause hypogonadotropic hypogonadism in humans and mice, which established the pathway's role in puberty.

Regulatory status

  1. Cosmetic ingredient
  2. Research compound
  3. In clinical trials
  4. Approved medicine

Not approved as a medicine by the FDA or the EMA. Some are registered in individual countries. Supplied for laboratory research only.

What published research is studying

  • LH, FSH, and testosterone secretion in healthy men after intravenous and subcutaneous administration
  • Differences in gonadotropin response between men and women, and across the menstrual cycle
  • Low testosterone in men with type 2 diabetes and other forms of central hypogonadism
  • Sustained stimulation versus desensitisation with continuous or intermittent administration over days

Key findings

  1. In healthy men, intravenous bolus kisspeptin-10 raised serum LH rapidly and dose-dependently, from 4.1 to 12.4 IU/L at 30 minutes at the peak-response dose; a 22.5-hour infusion raised testosterone from 16.6 to 24.0 nmol/L, and a lower-rate infusion increased LH pulse frequency from 0.7 to 1.0 pulses per hour.

    George JT et al., J Clin Endocrinol Metab 2011
  2. In a comparison of healthy men and women (4 to 5 per group), intravenous kisspeptin-10 raised LH and FSH in men and in women in the preovulatory phase, but produced no gonadotropin change in women in the follicular phase even at the highest doses tested.

    Jayasena CN et al., J Clin Endocrinol Metab 2011
  3. In a single-blinded, placebo-controlled study in healthy men (5 per dose group), 3-hour intravenous infusions of kisspeptin-10 and kisspeptin-54 produced similar gonadotropin responses, while GnRH produced roughly 3-fold higher LH and FSH than kisspeptin-10.

    Jayasena CN et al., Hum Reprod 2015
  4. In a proof-of-concept study in men with type 2 diabetes and low testosterone, an 11-hour kisspeptin-10 infusion in 4 men raised LH from 3.9 to 20.7 IU/L and testosterone from 8.5 to 11.4 nmol/L, with LH pulse frequency rising from 0.6 to 0.9 pulses per hour.

    George JT et al., Clin Endocrinol (Oxf) 2013
  5. In a randomised, single-blinded, placebo-controlled study in 15 healthy men, daily 8-hour subcutaneous kisspeptin-10 infusions sustained gonadotropin rises over 12 days, whereas after 5 days of continuous infusion gonadotropin levels were similar to vehicle despite persistently raised testosterone.

    Yeung AC et al., Eur J Endocrinol 2026

What the studies measured

Study durations

  • Intravenous infusion study in healthy men: infusions of up to 22.5 hours (George et al., J Clin Endocrinol Metab 2011).
  • Men with type 2 diabetes and low testosterone: 12 hours of baseline sampling, then an 11-hour intravenous infusion 5 days later (George et al., Clin Endocrinol 2013).
  • Kisspeptin-10, kisspeptin-54, and GnRH comparison: 3-hour intravenous infusions on study days at least a week apart (Jayasena et al., Hum Reprod 2015).
  • Chronic subcutaneous study: 5 days of continuous infusion, and 12 days of daily 8-hour infusions (Yeung et al., Eur J Endocrinol 2026).

Endpoints

  • Serum LH and FSH concentrations
  • LH pulse frequency and secretory burst mass by deconvolution analysis
  • Serum testosterone
  • Area under the curve for serum LH during infusion
  • Gonadotropin response to a kisspeptin-10 bolus after chronic administration

How strong is the evidence?

Early human data

Human data for kisspeptin-10 come from small physiological studies, typically 4 to 7 participants per group, that measure hormone responses over hours to 12 days rather than clinical outcomes such as fertility.

Common questions

Is Kisspeptin-10 an approved medicine?

Research compound. Not approved as a medicine by the FDA or the EMA. Some are registered in individual countries. Supplied for laboratory research only.

How much human research is there on Kisspeptin-10?

Human data for kisspeptin-10 come from small physiological studies, typically 4 to 7 participants per group, that measure hormone responses over hours to 12 days rather than clinical outcomes such as fertility.

Does UU supply Kisspeptin-10?

Yes, as premium-grade research material for laboratory use. Every batch is tested by an independent lab and the certificate of analysis is published.

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The UU library is an educational reference. It is not medical advice, does not make a health claim, and does not tell anyone how to use a compound. UU products are sold for laboratory research use only and are not for human consumption. Regulatory status changes: confirm it with the relevant authority before relying on it.