Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Balipodect (TAK063) 是一种高效的、口服具有活性、选择性的 PDE10A 抑制剂,IC50=0.3nM,对其他PDEs 无抑制作用。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 269 | 现货 | ||
2 mg | ¥ 397 | 现货 | ||
5 mg | ¥ 822 | 现货 | ||
10 mg | ¥ 1,080 | 现货 | ||
25 mg | ¥ 2,250 | 现货 | ||
50 mg | ¥ 3,350 | 现货 | ||
100 mg | ¥ 4,870 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 885 | 现货 |
产品描述 | Balipodect (TAK063) is a highly effective and selective PDE10A inhibitor (IC50: 0.30 nM); Its selectivity is >15000-fold over other PDEs. |
靶点活性 | PDE10A:0.3 nM |
体内活性 | TAK-063 has high brain penetration in mice. Oral administration of TAK-063 to mice elevated striatal cAMP and (cGMP) levels at 0.3 mg/kg and shows potent suppression of phencyclidine (PCP)-induced hyperlocomotion at a minimum effective dose (MED) of 0.3 mg/kg. TAK-063 is currently being evaluated in Clinicalal trials for the treatment of schizophrenia[1]. |
激酶实验 | Catalytic assay: MEK5 protein isolated from a baculovirus expression system is used to measure kinase activity utilizing PKLight ATP Detection Reagent. The assay is performed using 15 nM GST-MEK5 and 0.75 μM ATP in assay buffer consisting of 25 mM Hepes, pH 7.5, 10 mM MgCl2, 50 mM KCl, 0.2% BSA, 0.01% CHAPS, 100 μM Na3VO4, 0.5 mM DTT and 1% DMSO in the presence of varying concentrations of BIX02188. The kinase reaction mixture is incubated for 90 minutes at room temperature followed by addition of 10 μL of an ATP detection reagent for 15 minutes. The relative light unit (RLU) signal is measured and the RLU signals are converted to percent of control (POC) values for the determination of IC50 value. |
别名 | TAK063, TAK-063, TAK 063 |
分子量 | 428.42 |
分子式 | C23H17FN6O2 |
CAS No. | 1238697-26-1 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 79 mg/mL (184.4 mM)
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.3342 mL | 11.6708 mL | 23.3416 mL | 58.354 mL |
5 mM | 0.4668 mL | 2.3342 mL | 4.6683 mL | 11.6708 mL | |
10 mM | 0.2334 mL | 1.1671 mL | 2.3342 mL | 5.8354 mL | |
20 mM | 0.1167 mL | 0.5835 mL | 1.1671 mL | 2.9177 mL | |
50 mM | 0.0467 mL | 0.2334 mL | 0.4668 mL | 1.1671 mL | |
100 mM | 0.0233 mL | 0.1167 mL | 0.2334 mL | 0.5835 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。
Balipodect 1238697-26-1 Metabolism PDE TAK063 Phosphodiesterase (PDE) inhibit TAK-063 Inhibitor TAK 063 inhibitor