Kisspeptin-10 Vial

Kisspeptin-10 (also known as KP-10 or metastin 45-54; CAS 374675-21-5) is a synthetic 10-amino-acid C-terminal fragment of the human kisspeptin protein family encoded by the KISS1 gene.

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Description

Kisspeptin-10 (also known as KP-10 or metastin 45-54; CAS 374675-21-5) is a synthetic 10-amino-acid C-terminal fragment of the human kisspeptin protein family encoded by the KISS1 gene. The decapeptide retains the bioactive RFamide C-terminal motif shared across all kisspeptin fragments and is a high-affinity agonist of the kisspeptin receptor (KISS1R, also known as GPR54), the upstream regulator of gonadotropin-releasing hormone (GnRH) neurons in the hypothalamus. Inactivating mutations in KISS1 or KISS1R cause hypogonadotropic hypogonadism in humans; activating mutations cause precocious puberty — establishing the kisspeptin–GnRH axis as a master regulator of reproductive endocrinology. Multiple peer-reviewed human clinical trials of kisspeptin-10 have been published in the Journal of Clinical Endocrinology & Metabolism and other top endocrinology journals.

In a 2011 escalating-amount study published in the Journal of Clinical Endocrinology & Metabolism, intravenous bolus administration of kisspeptin-10 in healthy men produced concentration-dependent significant increases in serum luteinizing hormone (LH) compared with saline, with peak stimulation observed 30–40 minutes after injection and serum testosterone significantly elevated at clinically relevant amounts [1].

Published Research on Kisspeptin-10

The following peer-reviewed studies are summarized below. Full citations and direct links to each publication appear in the References section. All studies described in this section were conducted in adult human participants.

LH Pulse Frequency in Men — Chan et al., Journal of Clinical Endocrinology & Metabolism (2011)

Chan and colleagues at the Massachusetts General Hospital Reproductive Endocrine Unit conducted the first human study evaluating kisspeptin-10 specifically (rather than the longer kisspeptin-54 fragment), with the objective of testing whether kisspeptin-10 increases LH pulse frequency through stimulation of GnRH neurons in healthy adult men. The study used both single-bolus concentration-response (0.01–3.0 µg/kg) and continuous-infusion protocols, with frequent-sampling LH pulse detection.

The investigators reported that continuous infusion of kisspeptin-10 increases mean LH, LH pulse frequency, LH pulse size, and testosterone secretion in healthy adult men [1]. The findings established kisspeptin-10 as a potent stimulator of pulsatile GnRH/LH secretion in humans and supported the use of kisspeptin-10 specifically (rather than longer fragments) for pharmaceutical development given its shorter half-life and more rapid onset of action.

Read the full study: Kisspeptin-10 Is a Potent Stimulator of LH and Increases Pulse Frequency in Men (JCEM 2011).

Sexual Dimorphism Study — Jayasena et al., Journal of Clinical Endocrinology & Metabolism (2011)

Jayasena and colleagues at Imperial College London conducted a comparative escalating-amount study of intravenous bolus kisspeptin-10 in healthy adult men (n = 11) and healthy adult women (n = 35), measuring serum LH, FSH, sex steroid (estradiol or testosterone), and plasma kisspeptin immunoreactivity at multiple post-injection timepoints.

The investigators reported that serum LH was significantly elevated after kisspeptin-10 administration compared with saline at all tested amounts in men, with peak LH stimulation observed 30–40 minutes after injection; FSH and testosterone were also significantly elevated [2]. The reproductive-hormone response in women varied substantially with menstrual-cycle phase, establishing the sexually dimorphic and cycle-dependent character of the human kisspeptin response and informing amount-selection for downstream fertility-medicine clinical trials.

Read the full study: The Effects of Kisspeptin-10 on Reproductive Hormone Release Show Sexual Dimorphism in Humans (JCEM 2011).

Direct Comparison Study — Narayanaswamy et al., Human Reproduction (2016)

Narayanaswamy and colleagues conducted a within-subject crossover trial directly comparing intravenous kisspeptin-10, kisspeptin-54, and gonadotropin-releasing hormone (GnRH) on gonadotropin secretion in healthy adult men. Each subject received all three peptides at matched bolus amounts on separate visits, with serial measurement of serum LH and FSH for several hours post-administration.

The investigators reported that all three peptides produced significant LH and FSH responses at the amounts studied, with kisspeptin-10 producing a more rapid onset of LH response than kisspeptin-54 due to its shorter circulatory half-life [3]. The study clarified the relative pharmacodynamic profiles of kisspeptin fragments and supports the use of kisspeptin-10 specifically when rapid, controllable GnRH stimulation is required (e.g., in trigger-shot applications in assisted reproductive technology).

Read the full study: Direct Comparison of the Effects of Intravenous Kisspeptin-10, Kisspeptin-54 and GnRH on Gonadotrophin Secretion in Healthy Men (Hum Reprod Open 2016).

Pubertal Development Study — Aamir et al., BioMed Research International (2018)

Aamir and colleagues registered a clinical trial (NCT03286517) examining how the LH response to a single intravenous bolus of kisspeptin-10 changes across Tanner stages I–V in adolescent boys, with the objective of characterizing the developmental maturation of KISS1R signaling on GnRH neurons during human pubertal transition.

The investigators reported that the LH response to kisspeptin-10 administration increased significantly across Tanner stages, with post-kisspeptin plasma testosterone levels significantly elevated by Tanner stage V (P < 0.05) [4]. The data suggest that the sensitivity of KISS1R on GnRH neurons matures during the later stages of puberty, reaching adult-equivalent responsiveness at Tanner stage V — consistent with the role of the kisspeptin–GnRH axis as the gatekeeper of pubertal initiation.

Read the full study: Changes in the Responsiveness of the Hypothalamic-Pituitary-Gonadal Axis to Kisspeptin-10 Administration during Pubertal Transition in Boys (Biomed Res Int 2018).

About the Compound

The kisspeptins are a family of hypothalamic neuropeptides cleaved from a 145-amino-acid precursor protein encoded by the KISS1 gene. Post-translational processing yields multiple bioactive fragments — kisspeptin-54 (the original “metastin” form), kisspeptin-14, kisspeptin-13, and kisspeptin-10 — all sharing the same C-terminal arginine-amidated phenylalanine (RFamide) decapeptide that is responsible for receptor binding and bioactivity. Kisspeptin-10 (sequence YNWNSFGLRF-NH2) is the minimum bioactive fragment.

Kisspeptin-10 binds with high affinity to the kisspeptin receptor (KISS1R, also known as GPR54), a G-protein-coupled receptor expressed prominently on GnRH neurons in the hypothalamus. Receptor activation triggers GnRH release into the hypothalamic-pituitary portal system, which in turn stimulates pulsatile LH and FSH secretion from anterior pituitary gonadotrophs. The kisspeptin–GnRH axis is the master regulator of pubertal initiation, ovulatory cycle timing, and adult reproductive function in humans of both sexes. The sensitivity of KISS1R signaling on GnRH neurons changes across the lifespan — quiescent in childhood, increasing through puberty, peaking in adult reproductive years, and declining with reproductive aging in both men and women.

  • CAS Number: 374675-21-5
  • Molecular Formula: C63H83N17O14
  • Molecular Weight: 1302.4 g/mol
  • Sequence: Tyr-Asn-Trp-Asn-Ser-Phe-Gly-Leu-Arg-Phe-NH2 (YNWNSFGLRF-NH2)
  • Synonyms: KP-10, kisspeptin (45–54), metastin (45–54)
  • Receptor target (in research literature): Kisspeptin receptor (KISS1R / GPR54)
  • Regulatory status (as of publication): Investigational. Not approved by the FDA, EMA, or any other regulatory authority. Multiple Phase 1 and Phase 2 clinical trials have been conducted in fertility medicine and endocrinology research.

Product Specifications

Omnix Peptides supplies Kisspeptin-10 as a sterile, lyophilized (freeze-dried) powder in a sealed glass vial intended exclusively for in vitro laboratory research. Each production lot is independently characterized using high-performance liquid chromatography (HPLC) and liquid chromatography–mass spectrometry (LC–MS) protocols.

  • Format: Lyophilized powder
  • Available strengths: 5 mg · 10 mg per vial
  • Verified Purity: >99% (HPLC, LC–MS)
  • Container: Sterile, sealed glass vial
  • Documentation: Batch-specific Certificate of Analysis (COA) available

Storage, handling, intended-use, and regulatory information are provided in the corresponding tabs on this product page.

References

  1. Chan YM, Butler JP, Sidhoum VF, Pinnell NE, Seminara SB. Kisspeptin-10 is a potent stimulator of LH and increases pulse frequency in men. J Clin Endocrinol Metab. 2011;96(8):E1228-E1236. doi:10.1210/jc.2011-0089
  2. Jayasena CN, Nijher GM, Comninos AN, et al. The effects of kisspeptin-10 on reproductive hormone release show sexual dimorphism in humans. J Clin Endocrinol Metab. 2011;96(12):E1963-E1972. doi:10.1210/jc.2011-1408
  3. Narayanaswamy S, Prague JK, Jayasena CN, et al. Investigating the KNDy hypothesis in humans by coadministration of kisspeptin, neurokinin B, and naltrexone in men. Hum Reprod Open. 2016. Direct comparison studies of intravenous kisspeptin-10, kisspeptin-54, and GnRH effects on gonadotrophin secretion in healthy men. PMC4507333
  4. Aamir S, Khan FA, Jabbar A, et al. Changes in the responsiveness of the hypothalamic-pituitary-gonadal axis to kisspeptin-10 administration during pubertal transition in boys. Biomed Res Int. 2018;2018:5860296. doi:10.1155/2018/5860296
For research use only. Not for human consumption.