Abarelix Acetate
(Synonyms: 阿巴瑞克乙酸盐; PPI 149 Acetate; R 3827 Acetate) 目录号 : GC35217A synthetic GnRHR antagonist
Cas No.:785804-17-3
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Abarelix is a synthetic third generation gonadotropin-releasing hormone receptor (GnRHR) antagonist (IC50 = 3.5 nM in HEK293 cells expressing the human receptor).1,2 In vivo, abarelix (200 μg/kg) decreases plasma luteinizing hormone (LH) levels six hours post-treatment in castrated rats, with levels returning to baseline within 24 hours.3 Abarelix (2 mg/kg) also transiently decreases plasma testosterone levels in intact rats, with levels returning to baseline within seven days post-treatment. Formulations containing abarelix have previously been used in the treatment of advanced prostate cancer.
1.Tan, O., and Bukulmez, O.Biochemistry, molecular biology and cell biology of gonadotropin-releasing hormone antagonistsCurr. Opin. Obstet. Gynecol.23(4)238-244(2011) 2.Jiang, G., Stalewski, J., Galyean, R., et al.GnRH antagonists: A new generation of long acting analogues incorporating p-ureido-phenylalanines at positions 5 and 6J. Med. Chem.44(3)453-467(2001) 3.Broqua, P., Riviere, P.J.-M., Conn, P.M., et al.Pharmacological profile of a new, potent, and long-acting gonadotropin-releasing hormone antagonist: DegarelixJ. Pharmacol. Exp. Ther.301(1)95-102(2002)
Cas No. | 785804-17-3 | SDF | |
别名 | 阿巴瑞克乙酸盐; PPI 149 Acetate; R 3827 Acetate | ||
Canonical SMILES | CC(O)=O.C[C@H](C(N)=O)NC([C@H]1N(C([C@H](CCCCNC(C)C)NC([C@H](CC(C)C)NC([C@@H](CC(N)=O)NC([C@H](CC2=CC=C(C=C2)O)N(C([C@H](CO)NC([C@@H](CC3=CC=CN=C3)NC([C@@H](CC4=CC=C(Cl)C=C4)NC([C@@H](CC5=CC=C6C=CC=CC6=C5)NC(C)=O)=O)=O)=O)=O)C)=O)=O)=O)=O)CCC1)=O | ||
分子式 | C74H99ClN14O16 | 分子量 | 1476.12 |
溶解度 | DMSO: ≥ 100 mg/mL (67.75 mM); Water: 25 mg/mL (16.94 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 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 0.6775 mL | 3.3873 mL | 6.7745 mL |
5 mM | 0.1355 mL | 0.6775 mL | 1.3549 mL |
10 mM | 0.0677 mL | 0.3387 mL | 0.6775 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。