Powder: -20°C for 3 years | In solvent: -80°C for 1 year
TAK-700 (Orteronel) 是一种有效且高度选择性的人 17, 20-裂解酶抑制剂,IC50 为 38 nM,比其他 CYP(例如 11-羟化酶和 CYP3A4)选择性高出 1000 倍以上。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 348 | 现货 | ||
2 mg | ¥ 491 | 现货 | ||
5 mg | ¥ 828 | 现货 | ||
10 mg | ¥ 1,390 | 现货 | ||
25 mg | ¥ 2,820 | 现货 | ||
50 mg | ¥ 3,970 | 现货 | ||
100 mg | ¥ 5,790 | 现货 | ||
200 mg | ¥ 7,830 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 913 | 现货 |
产品描述 | TAK-700 (Orteronel) (Orteronel) is a potent and highly selective human 17, 20-lyase inhibitor with IC50 of 38 nM, exhibits >1000-fold selectivity over other CYPs (e.g. 11-hydroxylase and CYP3A4). Phase 3. |
靶点活性 | 17, 20-lyase (human):38 nM |
体外活性 | In vitro, TAK-700 shows the potent inhibitory activity against rat and human steroid 17,20-lyase with IC50 of 54 nM and 38 nM, respectively. While other CYP isoforms including 11-hydroxylase and CYP3A4 are not significantly affected by TAK-700. [1] In microsomes expressing human CYP isoforms, TAK-700 exhibit greater inhibitory effects on 17,20-lyase with IC50 of 19 nM compared to the other CYP isoforms. [1] TAK-700 shows the inhibitory activity against monkey 17,20-lyase and 17-hydroxylase with IC50 of 27 nM and 38 nM, respectively. [2] In monkey adrenal cells, TAK-700 inhibits the ACTH stimulated production of DHEA and androstenedione with IC50 of 110 nM and 130 nM, respectively. Moreover, TAK-700 also potently inhibits DHEA production in human adrenocortical tumor line H295R cells with IC50 of 37 nM. [2] |
体内活性 | In cynomolgus monkeys, oral treatment of TAK-700 at a dose of 1 mg/kg markedly reduces serum testosterone and dehydroepiandrosterone (DHEA) levels. [1] Oral treatment of TAK-700 at a dose of 1 mg/kg results in favorable pharmacokinetic parameters with Tmax, Cmax, t1/2 and AUC0-24 hours of 1.7 hours, 0.147 μg/mL, 3.8 hours and 0.727 μg h/mL, respectively. [2] |
别名 | (S/R)-Orteronel, Orteronel |
分子量 | 307.35 |
分子式 | C18H17N3O2 |
CAS No. | 426219-18-3 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 57 mg/mL (185.5 mM)
H2O: < 1 mg/mL (insoluble or slightly soluble)
Ethanol: 8 mg/mL (26.02 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO / Ethanol | 1 mM | 3.2536 mL | 16.2681 mL | 32.5362 mL | 81.3405 mL |
5 mM | 0.6507 mL | 3.2536 mL | 6.5072 mL | 16.2681 mL | |
10 mM | 0.3254 mL | 1.6268 mL | 3.2536 mL | 8.134 mL | |
20 mM | 0.1627 mL | 0.8134 mL | 1.6268 mL | 4.067 mL | |
DMSO | 50 mM | 0.0651 mL | 0.3254 mL | 0.6507 mL | 1.6268 mL |
100 mM | 0.0325 mL | 0.1627 mL | 0.3254 mL | 0.8134 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。
TAK-700 426219-18-3 Metabolism P450 TAK 700 (S/R)-Orteronel TAK700 Orteronel Inhibitor inhibitor inhibit