Kisspeptin 234
目录号 : GC12509Kisspeptin 234是一种由十个氨基酸组成的有效的Kisspeptin受体（KISS1/GPR54）拮抗剂。
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.
Kisspeptin 234是一种由十个氨基酸组成的有效的Kisspeptin受体（KISS1/GPR54）拮抗剂[1]。Kisspeptin 234通过与GPR54结合抑制了kisspeptin对下丘脑-垂体-性腺（HPG）轴的刺激作用，减少了下丘脑促性腺激素释放激素（GnRH）的释放，进而抑制垂体随后释放黄体生成素（LH）[2]。Kisspeptin 234通常用于青春期启动、生殖疾病（如多囊卵巢综合征）和心血管疾病等领域的研究[3,4]。
在体外，Kisspeptin 234（100nM）处理4种人子宫内膜癌RL95-2、Ishikawa、HEC-1-A和HEC-1-B细胞系24h，显著促进了细胞的迁移能力。Kisspeptin 234（100nM）处理RL95-2细胞2h，显著提高了MMP-2和MMP-9的蛋白表达水平。使用ERK1/2抑制剂（U0126）预处理RL95-2细胞1h，再加入Kisspeptin 234（100nM）共同培养2h，削弱了由Kisspeptin 234刺激引起的MMP-2和MMP-9蛋白表达上调[5]。Kisspeptin 234（50μM）在精子获能阶段处理小鼠精子2h，随后进行体外受精，显著降低了精子的受精率[6]。
在体内，Kisspeptin 234（1nM; 1.5μL）和Kisspeptin（1nM; 1.5μL）共同注射到预植入套管的Wistar大鼠第三脑室中，显著阻断了单独注射Kisspeptin所引起的血清胃饥饿素（Ghrelin）水平下降[7]。Kisspeptin 234（1nM; 3μL）通过鞘内注射处理CD1小鼠10min，再注射福尔马林，能显著减少福尔马林测试第一时相（0-10min）和第二时相（15-45min）的伤害性行为（如舔爪、抬爪）[8]。
| 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 | |
| 化学名 | (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 | ||
| 分子式 | C63H78N18O13 | 分子量 | 1295.42 |
| 溶解度 | Soluble to 1 mg/ml in Water | 储存条件 | Store at -20°C |
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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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