Kisspeptin

Kisspeptins are neuropeptides encoded by KISS1 that activate the GPR54/KISS1R receptor on GnRH neurons. They are key upstream regulators of the hypothalamic-pituitary-gonadal (HPG) axis and are used in research to stimulate GnRH/LH secretion and evaluate reproductive axis function.

— 10 mg Vial —

Reconstitute: Add 3.0 mL bacteriostatic water → ~3.33 mg/mL concentration.
Typical daily range: 100–200 mcg once daily (gradual titration).
Easy measuring: At 3.33 mg/mL, 1 unit = 0.01 mL ≈ 33.3 mcg on a U-100 insulin syringe.
Storage: Lyophilized: freeze at −20 °C; reconstituted: refrigerate at 2–8 °C, avoid freeze-thaw cycles.

Schedule: Daily subcutaneous injections for 8–12 weeks.
Cycle Length: 8–12 weeks; avoid prolonged continuous use to prevent tachyphylaxis.
Goal: Support physiological reproductive hormone signaling through upstream GnRH stimulation.

Frequency: Inject once daily subcutaneously. Conservative titration to assess individual response.

• Stimulates endogenous GnRH release leading to increased LH/FSH
• Tool for evaluating hypothalamic reproductive axis integrity
• Investigated for functional hypothalamic amenorrhea and infertility
• May help induce ovulation in certain controlled settings
• Research probe for puberty onset and reproductive neuroendocrinology

• Activates KISS1R (Gq/11-coupled GPCR) on GnRH neurons
• Increases PLCβ→IP3/DAG→intracellular Ca2+ and PKC signaling
• Triggers GnRH neuron firing and GnRH secretion → pituitary LH/FSH release

• Flushing, headache
• Nausea
• Transient changes in blood pressure/heart rate
• Abdominal discomfort
• Injection-site reactions
• In women: potential ovarian stimulation requiring monitoring

• Use lower initial doses; monitor vasomotor symptoms
• In reproductive studies, monitor LH/FSH/E2/testosterone response
• Avoid combining with other strong HPG stimulants unless protocol requires
• Use supervised protocols in female ovulation-induction contexts

• Pregnancy unless specifically indicated in fertility protocols
• Hormone-sensitive cancers
• Use caution in PCOS/high ovarian response risk contexts
• Hypersensitivity

1. Kisspeptin is required for puberty and fertility. Nat Rev Endocrinol. PubMed | DOI
2. Kisspeptin stimulates gonadotropin secretion in humans. J Clin Endocrinol Metab. PubMed | DOI
3. Kisspeptin therapy in reproductive disorders. Endocr Rev. PubMed | DOI
4. Kisspeptin and gonadotropin release: clinical potential. Trends Endocrinol Metab. PubMed | DOI