Goserelin acetate
(Synonyms: 醋酸戈舍瑞林; ICI-118630 acetate) 目录号 : GC36180
A synthetic GNRH agonist
Cas No.:145781-92-6
Sample solution is provided at 25 µL, 10mM.
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Goserelin is a synthetic gonadotropin-releasing hormone (GNRH) agonist that binds to the GNRH receptor (GNRHR; Ki = 1.6 nM, in CHO cells expressing the human receptor).1 It binds to mouse pituitary αT3-1 cells and human placenta (Kds = 2 and 580 nM, respectively) and increases intracellular calcium in αT3-1 cells.2 Goserelin induces testosterone production in vitro within 4 h in rat Leydig cells (ED50 = 83 nM) but decreases testosterone plasma level in vivo in rats over a period of 2 to 24 weeks.3,4 It inhibits tumor growth in a DU145 human prostate carcinoma mouse xenograft model when administered at a dose of 100 μg per day.5 Formulations containing goserelin have been used in the treatment of hormone-dependent breast and prostate cancers, as well as endometriosis and uterine fibroids.
1.Nederpelt, I., Georgi, V., Schiele, F., et al.Characterization of 12 GnRH peptide agonists - a kinetic perspectiveBr. J. Pharmacol.173(1)128-141(2016) 2.Chatzaki, E., Bax, C.M., Eidne, K.A., et al.The expression of gonadotropin-releasing hormone and its receptor in endometrial cancer, and its relevance as an autocrine growth factorCancer Res.56(9)2059-2065(1996) 3.Sullivan, M.H., and Cooke, B.A.The role of calcium in luteinizing hormone-releasing hormone agonist (ICI 118630)-stimulated steroidogenesis in rat Leydig cellsBiochem. J.218(2)621-624(1984) 4.Ward, J.A., Furr, B.J., Valcaccia, B., et al.Prolonged suppression of rat testis function by a depot formulation of Zoladex, a GnRH agonistJ. Androl.10(6)478-486(1989) 5.Dondi, D., Moretti, R.M., Montagnani, M.M., et al.Growth-inhibitory effects of luteinizing hormone-releasing hormone (LHRH) agonists on xenografts of the DU 145 human androgen-independent prostate cancer cell line in nude miceInt. J. Cancer76(4)506-511(1998)
| Cas No. | 145781-92-6 | SDF | |
| 别名 | 醋酸戈舍瑞林; ICI-118630 acetate | ||
| Canonical SMILES | O=C(N[C@H](C(N[C@@H](CC1=CC=C(O)C=C1)C(N[C@H](COC(C)(C)C)C(N[C@@H](CC(C)C)C(N[C@@H](CCCNC(N)=N)C(N2CCC[C@H]2C(NNC(N)=O)=O)=O)=O)=O)=O)=O)CO)[C@@H](NC([C@H](CC3=CN=CN3)NC([C@@H](N4)CCC4=O)=O)=O)CC5=CNC6=C5C=CC=C6.CC(O)=O | ||
| 分子式 | C61H88N18O16 | 分子量 | 1329.46 |
| 溶解度 | DMSO: ≥ 28 mg/mL (21.06 mM) | 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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| 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 | 0.7522 mL | 3.7609 mL | 7.5219 mL |
| 5 mM | 0.1504 mL | 0.7522 mL | 1.5044 mL |
| 10 mM | 0.0752 mL | 0.3761 mL | 0.7522 mL |
| 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。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet