Sufugolix (TAK-013)
(Synonyms: TAK-013) 目录号 : GC32399
A gonadotropin-releasing hormone receptor antagonist
Cas No.:308831-61-0
Sample solution is provided at 25 µL, 10mM.
Sufugolix is a gonadotropin-releasing hormone (GnRH) receptor antagonist (IC50 = 0.1 nM).1 Sufugolix inhibits GnRH-induced arachidonic acid release in CHO cells expressing human recombinant or monkey recombinant GnRH (IC50s = 0.1 and 10 nM, respectively), but not the rat GnRH receptor. It inhibits luteinizing hormone (LH) release stimulated by GnRH in monkey pituitary cells ex vivo (IC50 = 36 nM).2 Sufugolix (10 and 30 mg/kg) reduces increases in plasma LH following castration in male cynomolgus monkeys and lowers serum LH, estradiol, and progesterone levels in female cynomolgus monkeys when administered at a dose of 90 mg/kg.1,2
1.Sasaki, S., Cho, N., Nara, Y., et al.Discovery of a thieno[2,3-d]pyrimidine-2,4-dione bearing a p-methoxyureidophenyl moiety at the 6-position: A highly potent and orally bioavailable non-peptide antagonist for the human luteinizing hormone-releasing hormone receptorJ. Med. Chem.46(1)113-124(2003) 2.Hara, T., Araki, H., Kusaka, M., et al.Suppression of a pituitary-ovarian axis by chronic oral administration of a novel nonpeptide gonadotropin-releasing hormone antagonist, TAK-013, in cynomolgus monkeysJ. Clin. Endocrinol. Metab.88(4)1697-1704(2003)
Kinase experiment: | The receptor-expressing CHO cells are seeded into 24-well plates at a density of 4×104 cells/well and cultured for 1 day. The cells are then incubated with [5,6,8,9,11,12,14,15-3H]arachidonic acid (11 kBq/well) for 1 day and ished with DMEM supplemented with 20 mM HEPES and 0.2% BSA. The cells are then preincubated with the compounds (Sufugolix) at 37 °C for 60 min and the reaction is started by addition of LHRH (1 nM). After incubation at37 °C for 40 min, radioactivity in the medium is measured with a liquid scintillation counter[1]. |
Animal experiment: | Monkeys: Sufugolix (10 or 30 mg/kg, 3 mL/kg, n=3 for each group) is suspended in 0.5% methylcellulose containing 1.2% citric acid, or 0.5% methylcellulose containing 1.2% citric acid alone (3 mL/kg, n=3), are administered orally. Blood samples (heparin-plasma) are collected from a femoral vein 24 h before administration and 0, 2, 4, 8, 24, and 48 h after administration. LH concentrations in the plasma are measured by bioassays using mouse testicular cells[1]. |
References: [1]. Sasaki S, et al. Discovery of a thieno[2,3-d]pyrimidine-2,4-dione bearing a p-methoxyureidophenyl moiety at the 6-position: a highly potent and orally bioavailable non-peptide antagonist for the human luteinizing hormone-releasing hormone receptor. J Med Chem. 2003 Jan 2;46(1):113-24. |
Cas No. | 308831-61-0 | SDF | |
别名 | TAK-013 | ||
Canonical SMILES | O=C(NOC)NC1=CC=C(C(S2)=C(CN(C)CC3=CC=CC=C3)C(C(N4C5=CC=CC=C5)=O)=C2N(CC6=C(F)C=CC=C6F)C4=O)C=C1 | ||
分子式 | C36H31F2N5O4S | 分子量 | 667.72 |
溶解度 | DMSO : 1.25 mg/mL (1.87 mM) | 储存条件 | Store at -20°C,unstable in solution, ready to use. |
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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。 |
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1 mg | 5 mg | 10 mg |
1 mM | 1.4976 mL | 7.4882 mL | 14.9763 mL |
5 mM | 0.2995 mL | 1.4976 mL | 2.9953 mL |
10 mM | 0.1498 mL | 0.7488 mL | 1.4976 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 | |||
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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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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: >98.00%
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