Kisspeptin 234 |
| Catalog No.GC12509 |
Kisspeptin 234 is a potent kisspeptin receptor (KISS1/GPR54) antagonist composed of ten amino acids.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1145998-81-7
Sample solution is provided at 25 µL, 10mM.
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Kisspeptin 234 is a potent kisspeptin receptor (KISS1/GPR54) antagonist composed of ten amino acids[1]. By binding to GPR54, Kisspeptin 234 inhibits the stimulatory effect of kisspeptin on the hypothalamic-pituitary-gonadal (HPG) axis, reduces the release of gonadotropin-releasing hormone (GnRH) from the hypothalamus, and subsequently suppresses pituitary luteinizing hormone (LH) release[2]. Kisspeptin 234 is commonly used in research areas such as the onset of puberty, reproductive disorders (e.g., polycystic ovary syndrome), and cardiovascular diseases[3,4].
In vitro, treatment of four human endometrial cancer cell lines (RL95-2, Ishikawa, HEC-1-A, and HEC-1-B) with Kisspeptin 234 (100nM) for 24h significantly promoted cell migration ability. Treatment of RL95-2 cells with Kisspeptin 234 (100nM) for 2h significantly increased the protein expression levels of MMP-2 and MMP-9. Pretreatment of RL95-2 cells with an ERK1/2 inhibitor (U0126) for 1h, followed by co-culture with Kisspeptin 234 (100nM) for 2h, attenuated the Kisspeptin 234-stimulated upregulation of MMP-2 and MMP-9 protein expression[5]. When mouse sperm were treated with Kisspeptin 234 (50μM) during the capacitation stage for 2h, followed by in vitro fertilization, a significant reduction in the fertilization rate was observed[6].
In vivo, co-injection of Kisspeptin 234 (1nM; 1.5μL) and Kisspeptin (1nM; 1.5μL) into the third cerebral ventricle of cannula-implanted Wistar rats significantly blocked the decrease in serum ghrelin levels induced by Kisspeptin alone[7]. Intrathecal administration of Kisspeptin 234 (1nM; 3μL) to CD1 mice 10min before formalin injection significantly reduced nociceptive behaviors (such as licking, lifting, and shaking of the injected paw) in both the first phase (0-10min) and the second phase (15-45min) of the formalin test[8].
References:
[1] LEI Z, BAI X, MA J, et al. Kisspeptin-13 inhibits bleomycin-induced pulmonary fibrosis through GPR54 in mice[J]. Molecular Medicine Reports, 2019, 20(2): 1049-1056.
[2] CHEN X, YANG S, SHAW N D, et al. Kisspeptin Receptor Agonists and Antagonists: Strategies for Discovery and Implications for Human Health and Disease[J]. International Journal of Molecular Sciences, 2025, 26(10): 4890.
[3] TENA-SEMPERE M. GPR54 and kisspeptin in reproduction[J]. Human Reproduction Update, 2006, 12(5): 631-639.
[4] DINH H, KOVÁCS Z Z A, KIS M, et al. Role of the kisspeptin-KISS1R axis in the pathogenesis of chronic kidney disease and uremic cardiomyopathy[J]. GeroScience, 2024, 46(2): 2463-2488.
[5] WU H M, CHEN L H, CHIU W J, et al. Kisspeptin Regulates Cell Invasion and Migration in Endometrial Cancer[J]. Journal of the Endocrine Society, 2024, 8(3): bvae001.
[6] HSU M C, WANG J Y, LEE Y J, et al. Kisspeptin modulates fertilization capacity of mouse spermatozoa[J]. Reproduction, 2014, 147(6): 835-845.
[7] SADEGHZADEH A, BAYRAMI A, MAHMOUDI F, et al. The effects of interaction of dopaminergic and kisspeptin neural pathways on ghrelin secretion in rats[J]. Journal of Paramedical Sciences, 2018, 9(1): 29-35.
[8] SPAMPINATO S, TRABUCCO A, BIASIOTTA A, et al. Hyperalgesic activity of kisspeptin in mice[J]. Molecular Pain, 2011, 7: 1744-8069-7-90.
| Cell experiment [1]: | |
Cell lines | RL95-2, Ishikawa, HEC-1-A and HEC-1-B cells (human endometrial cancer cell lines) |
Preparation Method | Endometrial cancer cells were seeded on an uncoated porous filter in a transwell chamber containing 100nM of Kisspeptin 234. After 24h of incubation, cells on the upper side of the filter were removed and the migrated cells on the lower surface were fixed, stained with crystal violet, and counted. |
Reaction Conditions | 100nM; 24h |
Applications | Treatment with Kisspeptin 234 (100nM) significantly promoted the cell migration in the 4 cell lines. |
| Animal experiment [2]: | |
Animal models | Adult male CD1 mice |
Preparation Method | After pretreating mice with an intrathecal injection of Kisspeptin 234 (1nM; 3μL), a 10μL 5% formalin solution was subcutaneously injected into the plantar surface of the right hind paw of CD1 mice 10min later. Immediately after the injection, the mice were placed in a Plexiglas box surrounded by mirrors to allow observation of nociceptive responses, including licking, lifting, and shaking of the injected paw. Formalin scores were separated into two phases, phase I (0-10min) and phase II (15-45min). The mean behavioural score was calculated in blocks of 5min for each of the two phases. |
Dosage form | 1nM; 3μL; i.t. |
Applications | Intrathecal injection of Kisspeptin 234 at a dose of 1nM/3μL, administered 10min prior to formalin injection, significantly reduced nociceptive behaviors in both the first and second phases of the formalin test. |
References: | |
| Cas No. | 1145998-81-7 | SDF | |
| Chemical Name | (S,Z)-N'1-((6S,7Z,9R,10Z,13Z,15S,16Z,19Z,21S,22Z,24S)-9-((1H-indol-3-yl)methyl)-1-amino-15-benzyl-8,11,14,17,20,23-hexahydroxy-6-((Z)-hydroxy(((S)-1-hydroxy-1-imino-3-phenylpropan-2-yl)imino)methyl)-21-(2-hydroxy-2-iminoethyl)-1-imino-25-(1H-indol-3-yl)-2 | ||
| Canonical SMILES | C[C@](/N=C(O)/C)([H])/C(O)=N/[C@@](/C(O)=N/[C@@](/C(O)=N/[C@@](/C(O)=N/C/C(O)=N/[C@@](/C(O)=N/C/C(O)=N/[C@](/C(O)=N/[C@@](/C(O)=N/[C@@](C(O)=N)([H])CC1=CC=CC=C1)([H])CCCNC(N)=N)([H])CC2=CNC3=CC=CC=C23)([H])CC4=CC=CC=C4)([H])CC(O)=N)([H])CC5=CNC6=CC=CC=C56 | ||
| Formula | C63H78N18O13 | M.Wt | 1295.42 |
| Solubility | Soluble to 1 mg/ml in Water | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 772 μL | 3.8598 mL | 7.7195 mL |
| 5 mM | 154.4 μL | 772 μL | 1.5439 mL |
| 10 mM | 77.2 μL | 386 μL | 772 μL |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
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Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
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Average Rating: 5 (Based on Reviews and 5 reference(s) in Google Scholar.)
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