Gonadorelin acetate
(Synonyms: 醋酸戈那瑞林) 目录号 : GC34001
Gonadorelin acetate是一种促性腺激素释放激素（GnRH）的合成十肽类似物，是GnRH受体的特异性激动剂。
Cas No.:34973-08-5
Sample solution is provided at 25 µL, 10mM.
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Gonadorelin acetate is a synthetic decapeptide analog of gonadotropin-releasing hormone (GnRH) and acts as a specific agonist for the GnRH receptor[1]. By binding to the GnRH receptors in the anterior pituitary gland, Gonadorelin acetate triggers a signaling cascade that promotes the secretion of luteinizing hormone (LH) and follicle-stimulating hormone (FSH), both of which play a key role in regulating the reproductive system[2]. Gonadorelin acetate is usually used in the study of reproductive-related diseases[3][4].
In vitro, treatment of rat spinal ganglion neurons with Gonadorelin acetate (50µM; 30s-10min) significantly inhibits GABA-induced depolarization and reduces GABA-activated currents[5]. Gonadorelin acetate (1μM; 72h) significantly inhibited the proliferation, migration, and multi-lineage differentiation potential of endometrial stem cells[6].
In vivo, Gonadorelin acetate (150ng/mouse; subcutaneous injection; five days a week for three weeks) significantly reduced small intestinal polyp multiplicity and size and inhibited colon tumor formation in female ApcMin/+ mice[7].
References:
[1] Nederpelt I, Georgi V, Schiele F, et al. Characterization of 12 GnRH peptide agonists - a kinetic perspective. Br J Pharmacol. 2016;173(1):128-141.
[2] Resta C, Moustogiannis A, Chatzinikita E, et al. Gonadotropin-Releasing Hormone (GnRH)/GnRH Receptors and Their Role in the Treatment of Endometriosis. Cureus. 2023;15(4):e38136.
[3] Carel JC, Eugster EA, Rogol A, et al. Consensus statement on the use of gonadotropin-releasing hormone analogs in children. Pediatrics. 2009;123(4):e752-e762.
[4] Edi R, Cheng T. Endometriosis: Evaluation and Treatment. Am Fam Physician. 2022;106(4):397-404.
[5] Zhou XP, Wu XP, Guan BC, Li ZW. Modulatory effects of gonadorelin on GABA-induced depolarization and GABA-activated current in rat spinal ganglion neurons. Zhongguo Yao Li Xue Bao. 1996;17(1):31-34.
[6] Park SR, Cho A, Park ST, et al. Double-edged sword of gonadotropin-releasing hormone (GnRH): A novel role of GnRH in the multiple beneficial functions of endometrial stem cells. Cell Death Dis. 2018;9(8):828.
[7] Janakiram NB, Mohammed A, Brewer M, et al. Raloxifene and antiestrogenic gonadorelin inhibits intestinal tumorigenesis by modulating immune cells and decreasing stem-like cells. Cancer Prev Res (Phila). 2014;7(3):300-309.
Gonadorelin acetate是一种促性腺激素释放激素（GnRH）的合成十肽类似物，是GnRH受体的特异性激动剂[1]。Gonadorelin acetate通过与垂体前叶的GnRH受体结合，触发信号级联反应，促使黄体生成素（LH）和促卵泡激素（FSH）的分泌，这些激素在调节生殖系统方面发挥着关键作用[2]。Gonadorelin acetate通常用于生殖相关疾病研究[3][4]。
体外实验中，用50µM的Gonadorelin acetate处理大鼠脊髓神经节细胞30秒至10分钟，可显著抑制由GABA引起的去极化，并减少GABA激活的电流[5]。Gonadorelin acetate（1μM；72小时）处理子宫内膜干细胞显著抑制其增殖、迁移和多系分化潜能[6]。
体内实验中，Gonadorelin acetate (150ng/只；皮下注射；每周五天、连续三周)显著减少了雌性ApcMin/+小鼠小肠息肉的数量和大小，并抑制了结肠肿瘤的形成[7]。
| Cell experiment [1]: | |
Cell lines | Human endometrial stem cells |
Preparation Method | Human endometrial stem cells were obtained from endometrial tissues of uterine fibroid patients. Endometrial tissue was minced into small pieces, and then the small pieces were digested in DMEM containing 10% FBS and 250U/ml type I collagenase for 5h at 37°C in a rotating shaker. The digestion mixture was then filtered through a 40µm cell strainer to separate stromal like stem cells from epithelial gland fragments and undigested tissue. Isolated cells were then cultured in EBM-2 medium with EGM-2 supplements at 37°C and 5% CO2. Cells (1×104 cells per well) were seeded in 96-well plates. After 24h of incubation, the cells were treated with Gonadorelin acetate(1μM) or vehicle for 72h. The MTT assay was used to determine the anti-proliferative capacity. Cells were plated at 1×105 cells/well in 200μL of culture medium in the upper chambers of transwell permeable supports to track the migration of cells. |
Reaction Conditions | 1μM; 72h |
Applications | Gonadorelin acetate significantly inhibited the proliferation and migration of endometrial stem cells. |
| Animal experiment [2]: | |
Animal models | Female ApcMin/+ mice |
Preparation Method | Female ApcMin/+ mice were used in the efficacy study. Five-week-old mice were randomized into two groups so that average body weights in each group were equal (10 ApcMin/+ mice in each group). Mice were fed AIN-76A (control) diet for 1 week. At 6 weeks of age, animals were assigned to Group 1 (control diet) or Group 2 (control diet, Gonadorelin acetate injection). In Group 2, 150ng of Gonadorelin acetate was injected subcutaneously (five days a week, for three weeks (at 6th, 8th and 10th week). Food and water intake, animal activity, and physical changes were monitored regularly. Mice were evaluated weekly for signs of weight loss or lethargy that might indicate intestinal obstruction or anemia. After 100 days (14 weeks) of treatment, all mice were euthanized by CO2 asphyxiation. After necropsy, the entire intestinal tract was harvested, flushed with 0.9% NaCl, and opened longitudinally from the esophagus to the distal rectum. To expose the tumors, the tissue was flattened on filter paper. Tissue was briefly frozen on dry ice to aid visual scoring of tumors. The number, location, and size of visible intestinal tumors were determined under a dissection microscope. All tumors were scored and subdivided by location (duodenal, jejunal, ileal, and colorectal) and size (>2mm, 1-2, or <1mm in diameter). This procedure was completed by 2 individuals who were blinded to the experimental group and the genetic status of the mice. Fresh tissues from intestinal tumors were frozen in liquid nitrogen for molecular analysis. The remainder of the intestines was fixed in 10% neutral buffered formalin, embedded in paraffin blocks, and processed by routine hematoxylin and eosin staining. |
Dosage form | 150ng/mouse; subcutaneous injection; five days a week for three weeks |
Applications | Gonadorelin acetate significantly reduced small intestinal polyp multiplicity and size and inhibited colon tumor formation in female ApcMin/+ mice. |
References: | |
| Cas No. | 34973-08-5 | SDF | |
| 别名 | 醋酸戈那瑞林 | ||
| Canonical SMILES | O=C(N[C@@H](CO)C(N[C@H](C(NCC(N[C@@H](CC(C)C)C(N[C@@H](CCCNC(N)=N)C(N(CCC1)[C@@H]1C(NCC(N)=O)=O)=O)=O)=O)=O)CC2=CC=C(O)C=C2)=O)[C@@H](NC([C@@H](NC([C@H](CC3)NC3=O)=O)CC4=CNC=N4)=O)CC5=CNC6=C5C=CC=C6.OC(C)=O | ||
| 分子式 | C57H79N17O15 | 分子量 | 1242.34 |
| 溶解度 | DMSO : ≥ 12.5 mg/mL (10.06 mM); 25mg/ml in water | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 804.9 μL | 4.0247 mL | 8.0493 mL |
| 5 mM | 161 μL | 804.9 μL | 1.6099 mL |
| 10 mM | 80.5 μL | 402.5 μL | 804.9 μL |
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| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
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| % DMSO % % Tween 80 % saline | ||||||||||
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计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
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2.
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- Purity: >98.00%
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