Molecular Formula - C258H401N79O78
Molecular Weight - 5857 u
Research Category - Reproductive Health Research
Purity - 99.99%
Lab Tested - Yes
FULL CHEMICAL NAME
Kisspeptin, scientifically designated as metastin or Kiss1-derived peptide, is a family of neuropeptides encoded by the KISS1 gene, with the most studied variant being Kisspeptin-54 (KP-54), a 54-amino-acid polypeptide derived from a 145-amino-acid precursor. Its full chemical name is a complex sequence beginning with Gly-Thr-Ser-Leu-Ser-Pro-Pro-Pro-Glu-Ser-Ser-Gly-Ser-Arg-Gln-Gln-Pro-Gly-Leu-Ser-Ala-Pro-His-Ser-Arg-Gln-Ile-Pro-Ala-Pro-Gln-Gly-Ala-Val-Leu-Val-Gln-Arg-Glu-Lys-Asp-Leu-Pro-Asn-Tyr-Asn-Trp-Asn-Ser-Phe-Gly-Leu-Arg-Phe-NH2, featuring an amidated C-terminus critical for bioactivity. Shorter bioactive fragments, such as Kisspeptin-10 (KP-10: Tyr-Asn-Trp-Asn-Ser-Phe-Gly-Leu-Arg-Phe-NH2), are also widely researched due to their potency and conserved receptor-binding domain, reflecting Kisspeptin’s role as a pivotal regulator in the hypothalamic-pituitary-gonadal (HPG) axis.
ALIASES
Yes, Kisspeptin boasts several aliases reflecting its discovery and function. Originally termed ‘metastin’ due to its initial identification as a metastasis suppressor in melanoma (Lee et al., 1996), it’s also known as Kiss1 peptide, with variants like KP-54, KP-13, and KP-10 denoting specific fragment lengths (54, 13, or 10 amino acids). In research literature, it may be referenced by its gene origin, KISS1, or descriptively as ‘GnRH upstream regulator’ due to its role in gonadotropin-releasing hormone (GnRH) stimulation. These synonyms highlight its multifaceted identity across oncology and endocrinology.
EMERGING TRENDS IN RESEARCH
Emerging trends in Kisspeptin research extend its scope beyond reproduction, delving into its potential as a modulator of mood and behavior via hypothalamic circuitry, given its expression in limbic regions like the amygdala. Hypotheses suggest it may influence glucose homeostasis and insulin secretion, possibly through direct pancreatic effects or HPG axis crosstalk, as explored in rodent models. There’s also speculation about its role in puberty onset disorders and metabolic syndromes like polycystic ovary syndrome (PCOS), with studies proposing Kisspeptin analogs as diagnostic or therapeutic tools. Additionally, its anti-metastatic origins fuel interest in revisiting its tumor-suppressive properties, though these applications remain preclinical and demand extensive validation.
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Scientists are buzzing about Kisspeptin—it’s not just a fertility spark anymore! They’re guessing it could tweak your mood, maybe even steady your blood sugar, acting like a backstage boss in your brain and body. Some think it might unlock puberty puzzles or help with conditions like PCOS, and there’s a whisper it could fight cancer spread again—it’s a peptide with a wild, exciting future to explore!
NOTABLE INTERACTIONS
Kisspeptin primarily interacts with the G-protein-coupled receptor GPR54 (also Kiss1R), potently stimulating GnRH release from hypothalamic neurons, thus driving luteinizing hormone (LH) and follicle-stimulating hormone (FSH) secretion via the HPG axis. It exhibits synergistic effects with GnRH agonists and indirect modulation of steroid feedback loops (e.g., estrogen, testosterone), amplifying reproductive signaling. Emerging data suggest interactions with neuropeptide Y (NPY) and proopiomelanocortin (POMC) systems in metabolic regulation, potentially linking reproduction to energy balance. No significant direct interactions with non-endocrine systems (e.g., immune or cardiovascular) are well-documented, though its GnRH-mediated effects have broad downstream endocrine implications.
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Kisspeptin’s a social butterfly in the hormone world—it locks onto GPR54, sparking a big GnRH party in the brain that cranks out LH and FSH for reproduction! It teams up with sex hormones like estrogen and chats with appetite controllers like NPY, tying baby-making to food energy—it’s a busy connector in the body’s command center!
PREPARATION INSTRUCTIONS
In rodent studies, Kisspeptin-10 (10 nmol, intravenous) increases plasma LH levels by 3- to 5-fold within 20 minutes in rats (Matsui et al., 2004). In sheep, KP-54 (0.5 mg/kg) elevates LH by up to 10-fold and FSH by 2-fold over 2 hours (Caraty et al., 2007). Human studies show KP-10 (0.24 nmol/kg bolus) boosts LH by 2- to 3-fold in healthy men within 30 minutes (Dhillo et al., 2005), underscoring its potency as an HPG axis stimulator across species. No direct IGF-1 modulation is reported, as its effects are specific to gonadotropin pathways.
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In lab animals, Kisspeptin’s a hormone turbocharger—rats get a 3- to 5-times LH spike in minutes with a tiny shot (Matsui et al., 2004), and sheep see LH soar 10 times higher (Caraty et al., 2007)! Even in people tests, it doubles or triples LH fast—it’s like flipping a fertility switch!
CONTRAINDICATIONS OR WARNINGS FOR RESEARCH USE
Kisspeptin is designated for research use only outside approved clinical studies, with standard warnings: ‘Not for human consumption,’ ‘For laboratory use only,’ and requiring IRB/IACUC oversight. No specific contraindications beyond these are noted in preclinical literature, as toxicity is minimal at studied doses. Its potency in HPG activation warrants careful dosing in reproductive studies, but no evidence-based restrictions beyond regulatory guidelines apply.
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Kisspeptin’s a lab-only VIP—labeled ‘No humans allowed!’ unless it’s a special study, with big signs for science rules only! It’s safe in research, but its hormone powers mean scientists keep a close watch—no scary bans, just play it by the book!
PREPARATION INSTRUCTIONS
Reconstitute Kisspeptin (e.g., KP-10 or KP-54) in sterile saline or bacteriostatic water at 1 mg/mL under aseptic conditions to ensure solubility and stability. Store lyophilized powder at -20°C and reconstituted solution at 2–8°C, avoiding freeze-thaw cycles to preserve its amidated structure and bioactivity. Use within 4 weeks post-reconstitution, and handle with low-protein-binding materials to minimize adsorption losses—its small size and charge demand gentle care.
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Mix Kisspeptin with clean saltwater to make a 1 mg/mL potion—keep it super germ-free! Freeze the dry stuff at -20°C, chill the mix in the fridge, and use it within a month. Treat it gently with special tools—it’s a delicate hormone gem that hates rough shakes!
CLINICAL TRIALS AND HUMAN RESEARCH
Kisspeptin has limited clinical trial data as of February 2025. Small human studies (e.g., Dhillo et al., 2005; NCT00914823) have explored KP-10 and KP-54 for infertility and hypothalamic amenorrhea, showing LH/FSH stimulation, but no widespread therapeutic approval exists. Preclinical research dominates, with extensive rodent, sheep, and primate models evaluating its reproductive and metabolic roles.
LESS TECHNICAL EXPLANATION
Kisspeptin’s dipped its toes in human tests—like little trials for fertility boosts—but it’s mostly an animal lab star! It’s wowed rats, sheep, and monkeys, but big human stories are still cooking—think of it as a science preview, not the main show yet!
EFFECTS ON DIFFERENT TISSUE TYPES
Kisspeptin primarily affects hypothalamic GnRH neurons, driving gonadotropin secretion, and thus influences reproductive tissues (e.g., gonads) via LH/FSH. It’s expressed in limbic areas (e.g., amygdala), suggesting mood/behavior effects, and pancreatic studies hint at insulin modulation (Hauge-Evans et al., 2006). Minimal direct impact on non-reproductive tissues like liver or muscle is noted in preclinical models, though its HPG effects ripple systemically.
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Kisspeptin’s the brain’s fertility DJ—spinning GnRH tunes to spark hormones for baby-making parts! It might tweak mood in brain corners and nudge insulin in the pancreas, but it mostly skips muscles or liver—it’s a targeted love song with big echoes!
EFFICACY IN ANIMAL MODELS
In rats, KP-10 (10 nmol) raises LH 3- to 5-fold in 20 minutes (Matsui et al., 2004). In sheep, KP-54 (0.5 mg/kg) boosts LH 10-fold and FSH 2-fold (Caraty et al., 2007). In monkeys, KP-10 triggers robust GnRH pulses, advancing puberty onset (Shahab et al., 2005)—it’s a potent reproductive kickstarter!
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In animals, Kisspeptin’s a champ—rats get a 3- to 5-times LH boost fast (Matsui et al., 2004), sheep see LH soar 10 times (Caraty et al., 2007), and monkeys kickstart puberty—it’s like a hormone wake-up call!
FUTURE RESEARCH
Future Kisspeptin research may explore its therapeutic potential in infertility, PCOS, or delayed puberty, leveraging its GnRH stimulation. Its mood and metabolic roles—linking reproduction to energy balance—offer avenues for neuropsychiatric and diabetes studies. Analogs with tuned potency or half-life could enhance applications.
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What’s next for Kisspeptin? Maybe fixing fertility woes, mood swings, or sugar troubles—it could be a brain-body bridge! Scientists might cook up super-versions to make it even better—a thrilling future awaits!
HISTORY OF MODELS TESTED
Tested in rats, mice, sheep, monkeys, and human cell cultures (e.g., GnRH neurons); small human trials for fertility (Dhillo et al., 2005; Shahab et al., 2005; Caraty et al., 2007).
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Kisspeptin’s rocked rats, mice, sheep, monkeys, and lab dishes—plus a few human fertility tests! It’s a science globetrotter, but mostly shines in animal labs (Dhillo et al., 2005)!
TOXICITY DATA AVAILABLE
No formal LD50 data exists; preclinical studies report no toxicity at doses up to 1 mg/kg in rats (Matsui et al., 2004). High tolerability is observed, with no organ damage noted.
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No ‘danger limit’ yet—rats handle 1 mg/kg like pros with no harm (Matsui et al., 2004)! It’s a safety sweetheart so far!
MECHANISM OF ACTION
Kisspeptin binds GPR54, activating Gq/11 signaling, increasing intracellular calcium, and stimulating GnRH release from hypothalamic neurons. It may modulate KISS1 neuron excitability via ion channels, amplifying pulsatile secretion—no direct growth factor upregulation beyond HPG effects.
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Kisspeptin flips the GPR54 switch, sparking calcium fireworks in brain cells to unleash GnRH—like a maestro conducting a hormone symphony! It tweaks nerve signals for rhythm, focusing on fertility vibes!
METABOLIC AND PHYSIOLOGICAL EFFECTS
Boosts LH/FSH secretion, enhances reproductive axis activity, may influence glucose-stimulated insulin release (Hauge-Evans et al., 2006).
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Kisspeptin cranks up fertility hormones, revs the baby-making engine, and might nudge insulin for sugar balance—it’s a hormone multitasker (Hauge-Evans et al., 2006)!
SAFETY AND SIDE EFFECTS
Safe at studied doses (e.g., 1 mg/kg in rats); human trials note transient flushing at high doses (Dhillo et al., 2005).
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At lab doses, Kisspeptin’s chill—no big issues in rats; humans might blush a bit at high shots (Dhillo et al., 2005)!
ADMINISTRATION METHODS RECOMMENDED
Intravenous or subcutaneous injection at 1 mg/mL in saline; typical rat doses 10 nmol (Matsui et al., 2004). Store at 2–8°C post-reconstitution.
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Inject Kisspeptin in veins or under skin with saltwater mix—10 nmol for rats rocks it (Matsui et al., 2004)! Chill it in the fridge!
ADVERSE EFFECTS REPORTED
No significant adverse effects in animals at 1 mg/kg (Matsui et al., 2004); human studies note mild flushing (Dhillo et al., 2005).
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No lab oopsies—rats are fine at 1 mg/kg; humans might feel a warm flush (Matsui et al., 2004; Dhillo et al., 2005)!
KEY OBSERVATIONS FROM PEER REVIEWED STUDIES
Rats show 3- to 5-fold LH rise (Matsui et al., 2004); humans get 2- to 3-fold LH boost (Dhillo et al., 2005)—potent HPG driver!
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Kisspeptin lifts LH 3 to 5 times in rats and 2 to 3 times in people—fertility gold (Matsui et al., 2004; Dhillo et al., 2005)!
LIMITATIONS OF CURRENT RESEARCH DATA
Limited human data; preclinical focus, small samples, long-term effects unknown.
LESS TECHNICAL EXPLANATION
We’ve got baby steps in humans—mostly animal tales, tiny groups, and big ‘what ifs’ for the long haul!
RESEARCH BASED OBSERVATIONS
Stimulates reproductive axis, may modulate mood and glucose metabolism (Hauge-Evans et al., 2006).
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Kisspeptin fires up fertility, might tweak moods, and could balance sugar—cool possibilities (Hauge-Evans et al., 2006)!
SPECIFIC EFFECTS OBSERVED IN VITRO OR VIVO
In vitro: GnRH release from neurons; in vivo: 3- to 5-fold LH spike in rats (Matsui et al., 2004).
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In dishes, sparks GnRH; in rats, triples LH fast—lab magic (Matsui et al., 2004)!
TYPICAL DOSES USED IN RESEARCH
10 nmol in rats (Matsui et al., 2004); 0.24 nmol/kg in humans (Dhillo et al., 2005).
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Tiny 10 nmol shots for rats, 0.24 nmol/kg for people—hormone kicks (Matsui et al., 2004; Dhillo et al., 2005)!
UNANSWERED QUESTIONS NEEDING INVESTIGATION
Long-term safety, metabolic roles, human efficacy gaps.
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What happens years later? Sugar tweaks or people power—big mysteries!
BIOCHEMICAL PATHWAYS OR RECEPTORS TARGETED BY PEPTIDE
Targets GPR54, upregulates GnRH via calcium signaling.
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Hits GPR54, cranks GnRH with calcium sparks—hormone wizardry!
POTENTIAL RESEARCH EXPLORATIONS
Synergy with GnRH analogs, mood modulators, or metabolic agents.