Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Sufugolix (TAK-013) 是一种高效的、有口服活性的黄体激素释放激素(LHRH) 受体拮抗剂(IC50:0.1 nM)。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 327 | 现货 | ||
2 mg | ¥ 478 | 现货 | ||
5 mg | ¥ 822 | 现货 | ||
10 mg | ¥ 1,370 | 现货 | ||
25 mg | ¥ 2,970 | 现货 | ||
50 mg | ¥ 4,390 | 现货 | ||
100 mg | ¥ 6,290 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,190 | 现货 |
产品描述 | Sufugolix (TAK-013) is a potent and orally available luteinizing hormone-releasing hormone LHRH receptor. |
靶点活性 | LHRH:0.1 nM. |
体外活性 | Sufugolix exhibits more than 3- and 2000-fold selectivity for the human receptor over the monkey and rat receptors, respectively. Sufugolix effectively antagonizes LHRH function on CHO cells expressing the human (IC50=0.1 nM) and monkey (IC50=0.6 nM) receptors. It is observed that the cis conformer of the methoxyurea is more populated than the trans conformer by high-temperature molecular dynamics calculation during the conformational analysis of sufugolix[1]. |
体内活性 | Oral administration of sufugolix causes almost complete suppression of the plasma LH levels in castrated male cynomolgus monkeys at a 30 mg/kg dose with sufficient duration of action (more than 24 h). Sufugolix has the apparent lipophilicity to allow increased membrane permeability and consequently improve its oral absorption in monkeys. The maximum plasma concentrations of sufugolix are 0.34 μM (reached 6 h after administration) and 0.18 μM (reached 4 h after administration) at 30 and 10 mg/kg doses, respectively[1]. |
激酶实验 | 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]. |
别名 | TAK-013 |
分子量 | 667.72 |
分子式 | C36H31F2N5O4S |
CAS No. | 308831-61-0 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 25 mg/mL (37.44 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 1.4976 mL | 7.4882 mL | 14.9763 mL | 37.4408 mL |
5 mM | 0.2995 mL | 1.4976 mL | 2.9953 mL | 7.4882 mL | |
10 mM | 0.1498 mL | 0.7488 mL | 1.4976 mL | 3.7441 mL | |
20 mM | 0.0749 mL | 0.3744 mL | 0.7488 mL | 1.872 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Sufugolix 308831-61-0 Endocrinology/Hormones LHRH TAK-013 Inhibitor TAK013 TAK 013 inhibit inhibitor