[D-Lys3]-GHRP-6是一种高选择性的生长激素促分泌素受体（GHSR）拮抗剂，IC50值为0.9µM。
![[D-Lys3]-GHRP-6 Chemical Structure](https://cdn.glpbio.com/thumbs/struct/GC1/GC10161.png "[D-Lys3]-GHRP-6 Chemical Structure")
Cas No.:136054-22-3
Sample solution is provided at 25 µL, 10mM.
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[D-Lys3]-GHRP-6 is a highly selective growth-hormone secretagogue receptor (GHSR) antagonist, with an IC50 value of 0.9μM [1]. [D-Lys3]-GHRP-6 induces pronounced smooth muscle contractions in the rat fundus by interacting with 5-HT2B receptors [2]. [D-Lys3]-GHRP-6 has been widely used to alter the metabolic functions and food intake of diabetic mouse models[3].
In vitro, [D-Lys3]-GHRP-6 treatment at 100μM for 48h significantly decreased the cell viability of HECa10 cells [4]. Treatment with 100μM of [D-Lys3]-GHRP-6 for 30 minutes can block the entry and proliferation of HIV-1 virus mediated by CXCR4 in activated peripheral blood mononuclear cells (PBMC)[5]. Treatment with 1μM of [D-Lys3]-GHRP-6 for 24 hours significantly induced apoptosis of dorsal root ganglion (DRG) cells and regulated calcium ion levels[6].
In vivo, [D-Lys3]-GHRP-6 treatment via intraperitoneal injection at a dose of 20nmol/day for 14 days inhibited the growth of tumor volume in the PC3 cell-xenograft mouse model [7]. For 7 consecutive days, intravenous injection twice daily of 6mg/kg dose of [D-Lys3]-GHRP-6 significantly reduced the weight gain of growing pigs, increased the serum non-esterified fatty acids (NEFA) and insulin levels, liver glucose levels, and homeostasis model assessment of insulin resistance index (HOMA-IR) after fasting, and decreased the serum total bile acid (TBA) level[8].
References:
[1] Traebert M, Riediger T, Whitebread S, et al. Ghrelin acts on leptin‐responsive neurones in the rat arcuate nucleus[J]. Journal of neuroendocrinology, 2002, 14(7): 580-586.
[2] Depoortere I, Thijs T, Peeters T. The contractile effect of the ghrelin receptor antagonist, D-Lys3-GHRP-6, in rat fundic strips is mediated through 5-HT receptors[J]. European journal of pharmacology, 2006, 537(1-3): 160-165.
[3] Mosa R, Huang L, Li H, et al. Long-term treatment with the ghrelin receptor antagonist [d-Lys3]-GHRP-6 does not improve glucose homeostasis in nonobese diabetic MKR mice[J]. American Journal of Physiology-Regulatory, Integrative and Comparative Physiology, 2018, 314(1): R71-R83.
[4] Polowinczak-Przybylek J, Siejka A, Melen-Mucha G. D-Lys3-GHRP-6 antagonizes the effect of unacylated but not of acylated ghrelin on the growth of HECa10 murine endothelial cells[J]. Peptides, 2012, 38(2): 248-254.
[5] Patel K, Dixit V D, Lee J H, et al. Identification of ghrelin receptor blocker, D-[Lys3] GHRP-6 as a CXCR4 receptor antagonist[J]. International journal of biological sciences, 2011, 8(1): 108.
[6] Erriquez J, Bernascone S, Ciarletta M, et al. Calcium signals activated by ghrelin and D-Lys3-GHRP-6 ghrelin antagonist in developing dorsal root ganglion glial cells[J]. Cell calcium, 2009, 46(3): 197-208.
[7] Maugham M L, Seim I, Thomas P B, et al. Limited short-term effects on human prostate cancer xenograft growth and epidermal growth factor receptor gene expression by the ghrelin receptor antagonist [D-Lys3]-GHRP-6[J]. Endocrine, 2019, 64(2): 393-405.
[8] Zhang H, Yan X, Lin A, et al. Inhibition of ghrelin activity by the receptor antagonist [D-Lys3]-GHRP-6 enhances hepatic fatty acid oxidation and gluconeogenesis in a growing pig model[J]. Peptides, 2023, 166: 171041.
[D-Lys3]-GHRP-6是一种高选择性的生长激素促分泌素受体（GHSR）拮抗剂，IC50值为0.9µM [1]。[D-Lys3]-GHRP-6通过与5-HT2B受体相互作用，可诱导大鼠胃底部产生明显的平滑肌收缩[2]。[D-Lys3]-GHRP-6已被广泛用于改变糖尿病小鼠模型的代谢功能和食物摄入[3]。
在体外，使用100µM的[D-Lys3]-GHRP-6处理48小时，显著降低了HECa10细胞的活力[4]。使用100µM的[D-Lys3]-GHRP-6处理30分钟，可阻断CXCR4介导的HIV-1病毒在活化的外周血单核细胞（PBMC）中的进入和增殖[5]。使用1µM的[D-Lys3]-GHRP-6处理24小时，显著诱导了背根神经节（DRG）细胞凋亡并调节了钙离子水平[7]。
在体内，每日腹腔注射20nmol/day剂量的[D-Lys3]-GHRP-6，持续14天，抑制了PC3细胞异种移植小鼠模型中的肿瘤体积生长[7]。连续7天每日两次静脉注射6mg/kg剂量的[D-Lys3]-GHRP-6，显著减少了生长猪的体重增加，提高了空腹后的血清非酯化脂肪酸（NEFA）和胰岛素水平、肝脏葡萄糖水平以及稳态模型评估的胰岛素抵抗指数（HOMA-IR），并降低了血清总胆汁酸（TBA）水平[8]。
| Cell experiment [1]: | |
Cell lines | HECa10 cells |
Preparation Method | HECa10 cells were cultured in RPMI-1640 medium supplemented with 10% fetal calf serum (FCS) and antibiotics (penicillin 100U/ml, streptomycin 0.1mg/ml) under normal conditions (5% CO2 with 95% humidified air). HECa10 cells (5×103 cells) were plated using 96-well plates and subjected to incubation for 24h in a 5% CO2 incubator. Incubation was followed by treatment with different doses of [D-Lys3]-GHRP-6 (0.1, 1, 10, and 100μM) for 48h and cell viability was measured. |
Reaction Conditions | 0.1, 1, 10, and 100μM; 48h |
Applications | [D-Lys3]-GHRP-6 treatment decreased the cell viability of HECa10 cells in a dose-dependent manner. |
| Animal experiment [2]: | |
Animal models | NOD.CB17-Prkdcscid/Arc (NOD/SCID) mice |
Preparation Method | 1×106 PC3 cells were subcutaneously injected into the left abdomen of NOD.CB17-Prkdcscid/Arc (NOD/SCID) mice. The mice were raised under specific pathogen-free (SPF) conditions, placed in separate ventilated cages, with a room temperature of 20-23℃ and a light cycle of 12 hours of light/12 hours of darkness. When the tumor reached a volume of approximately 100mm3, the mice were divided into two groups. Subsequently, the mice were intraperitoneally injected with 20nmol per mouse of [D-Lys3]-GHRP-6 (n=4) or PBS (control) (n=5) every day for 14 days. The length and width of the subcutaneous tumors were measured twice a week, and the tumor volume was calculated as the formula: tumor volume = (length×width2)/2. |
Dosage form | 20nmol/day for 14 days; i.p. |
Applications | [D-Lys3]-GHRP-6 treatment inhibited the growth of tumor volume in the PC3 cell-xenograft mouse model. |
References: | |
| Cas No. | 136054-22-3 | SDF | |
| Canonical SMILES | NCCCC[C@@](/N=C(O)/[C@@](/N=C(O)/[C@](/N=C(O)/[C@@](/N=C(O)/[C@@](/N=C(O)/[C@](N)([H])CC1=CN=CN1)([H])CC2=CNC3=CC=CC=C23)([H])CCCCN)([H])CC4=CNC5=CC=CC=C45)([H])CC6=CC=CC=C6)([H])C(O)=N | ||
| 分子式 | C49H63N13O6 | 分子量 | 930.12 |
| 溶解度 | Soluble to 0.50 mg/ml in Water | 储存条件 | Desiccate at -20°C |
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.0751 mL | 5.3757 mL | 10.7513 mL |
| 5 mM | 215 μL | 1.0751 mL | 2.1503 mL |
| 10 mM | 107.5 μL | 537.6 μL | 1.0751 mL |
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