Cetrorelix Acetate (SB-075 acetate)
(Synonyms: 醋酸西曲瑞克; SB-75 acetate) 目录号 : GC33467
Cetrorelix Acetate (SB-075 acetate)是一种合成的促性腺激素释放激素（GnRH）拮抗剂（IC50 = 1.21nM)。
Cas No.:145672-81-7
Sample solution is provided at 25 µL, 10mM.
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Cetrorelix Acetate (SB-075 acetate) is a synthetic gonadotropin-releasing hormone (GnRH) antagonist (IC50 = 1.21nM) [1]. Cetrorelix Acetate inhibits the GnRH signaling pathway, thereby reducing the secretion of follicle-stimulating hormone (FSH) and luteinizing hormone (LH) [2-3]. Cetrorelix Acetate is used to treat premature ovulation [4].
In epithelial cells, treatment with Cetrorelix Acetate (1-20ng/mL; 10d) significantly reduced cell growth rate [5]. In HTOA cells, Cetrorelix Acetate (10nM-10μM; 24-96h) treatment showed a dose-dependent anti-proliferative effect on cells [6].
In C57BL/6J mice, Cetrorelix Acetate (5µg/kg; ip; 7d) improves superovulation efficacy in aged mice without compromising oocyte quality [7]. In CFLP male mice, Cetrorelix Acetate (2µg; 2µL; intraventricular injection; single injection) attenuates the effects of beta-amyloid 25-35 [8].
References:
[1]. Beckers T, Reiländer H, Hilgard P. Characterization of gonadotropin-releasing hormone analogs based on a sensitive cellular luciferase reporter gene assay[J]. Analytical biochemistry, 1997, 251(1): 17-23.
[2]. Britten J L, Malik M, Levy G, et al. Gonadotropin-releasing hormone (GnRH) agonist leuprolide acetate and GnRH antagonist cetrorelix acetate directly inhibit leiomyoma extracellular matrix production[J]. Fertility and sterility, 2012, 98(5): 1299-1307.
[3]. Jiang J, Gao S, Xu J. Efficacy and safety of gonadotropin-releasing hormone (GnRH) agonists triptorelin acetate and cetrorelix acetate in assisted reproduction[J]. Medical Science Monitor: International Medical Journal of Experimental and Clinical Research, 2018, 24: 7996.
[4]. Steward R G, Gill I, Williams D B, et al. Cetrorelix lowers premature luteinization rate in gonadotropin ovulation induction–intrauterine insemination cycles: a randomized-controlled clinical trial[J]. Fertility and sterility, 2011, 95(1): 434-436.
[5]. Castellón E, Clementi M, Hitschfeld C, et al. Effect of leuprolide and cetrorelix on cell growth, apoptosis, and GnRH receptor expression in primary cell cultures from human prostate carcinoma[J]. Cancer investigation, 2006, 24(3): 261-268.
[6]. Tang X, Yano T, Osuga Y, et al. Cellular mechanisms of growth inhibition of human epithelial ovarian cancer cell line by LH-releasing hormone antagonist Cetrorelix[J]. The Journal of Clinical Endocrinology & Metabolism, 2002, 87(8): 3721-3727.
[7]. Kanda A, Nobukiyo A, Sotomaru Y. Effect of Cetrorelix administration on ovarian stimulation in aged mice[J]. Experimental Animals, 2021, 70(1): 31-36.
[8]. Telegdy G, Tanaka M, Schally A V. Effects of the LHRH antagonist Cetrorelix on the brain function in mice[J]. Neuropeptides, 2009, 43(3): 229-234.
Cetrorelix Acetate (SB-075 acetate)是一种合成的促性腺激素释放激素（GnRH）拮抗剂（IC50 = 1.21nM) [1]。Cetrorelix Acetate可抑制GnRH信号通路，从而减少促卵泡激素（FSH）和促黄体生成素（LH）的分泌 [2-3]。Cetrorelix Acetate用于治疗早产排卵 [4]。
在上皮细胞中，Cetrorelix Acetate（1-20ng/mL；10d）处理显著降低细胞生长率 [5]。在HTOA细胞中，Cetrorelix Acetate（10nM-10μM；24-96h）处理显示出剂量依赖性的抗细胞增殖作用 [6]。
在C57BL/6J小鼠中，Cetrorelix Acetate（5µg/kg；ip；7d）可提高老年小鼠的超排卵效果，且不影响卵母细胞质量 [7]。在CFLP雄性小鼠中，Cetrorelix Acetate（2µg；2µL；脑室内注射；单次注射）可减弱β-淀粉样蛋白25-35的作用 [8]。
| Cell experiment [1]: | |
Cell lines | Epithelial cells |
Preparation Method | After first medium change of both cultures, cells were washed and fresh medium without FBS and supplemented with human transferrin 5mg/L, insulin 2mg/L, epidermal growth factor 10µg/L, vitamin A and E 200µg/L, hydrocortisone 10nM, sodium selenite 2µg/L, and dihydrotestosterone (DHT) 10nM was added. Then, epithelial and stromal cell cultures were set together, media were collected every 48h and cocultures maintained for 2 weeks. GnRH analogues treatments were carried out during Day 4 and 6 of co culture. Both leuprolide and Cetrorelix Acetate were used in a concentration range of 1-20ng/mL. |
Reaction Conditions | 1-20ng/mL; 10d |
Applications | Treatment with Cetrorelix Acetate significantly reduced cell growth rate. |
| Animal experiment [2]: | |
Animal models | C57BL/6J mice |
Preparation Method | To test superovulation, we used 16-week-old and 52-week-old C57BL/6J female mice as juvenile and aged mice, respectively. To prepare pseudopregnant female mice for embryo transfer, we used mature female ICR mice and vasectomized male mice. To investigate the effects of GnRH antagonists on the number of ovulated oocytes, Cetrorelix Acetate (5µg/kg) was administered intraperitoneally at approximately 5:00 PM once daily or every three days, one week prior to administration of pregnant mare serum gonadotropin and human chorionic gonadotropin. |
Dosage form | 5µg/kg; ip; 7d |
Applications | Cetrorelix Acetate improves superovulation efficacy in aged mice without compromising oocyte quality. |
References: | |
| Cas No. | 145672-81-7 | SDF | |
| 别名 | 醋酸西曲瑞克; SB-75 acetate | ||
| Canonical SMILES | N-acetyl-{2-Naph-Ala}-{Cl-Phe}-{3Py-Ala}-Ser-Tyr-{Cit}-Leu-Arg-Pro-Ala-NH2 | ||
| 分子式 | C72H96ClN17O16 | 分子量 | 1491.09 |
| 溶解度 | DMSO : 50 mg/mL (33.53 mM) | 储存条件 | -20°C, protect from light |
| 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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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 670.7 μL | 3.3533 mL | 6.7065 mL |
| 5 mM | 134.1 μL | 670.7 μL | 1.3413 mL |
| 10 mM | 67.1 μL | 335.3 μL | 670.7 μL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 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 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
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，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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Quality Control & SDS
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- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
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