Powder: -20°C for 3 years | In solvent: -80°C for 1 year
ANA-12 是一种选择性TrkB 拮抗剂,对高亲和力和低亲和力位点的IC50分别为45.6 nM 和41.1 μM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 197 | 现货 | ||
2 mg | ¥ 297 | 现货 | ||
5 mg | ¥ 662 | 现货 | ||
10 mg | ¥ 1,060 | 现货 | ||
25 mg | ¥ 1,920 | 现货 | ||
50 mg | ¥ 3,180 | 现货 | ||
100 mg | ¥ 4,580 | 现货 | ||
500 mg | ¥ 9,530 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 697 | 现货 |
产品描述 | ANA-12 is a potent and selective TrkB antagonist with anxiolytic and antidepressant activity in mice. |
靶点活性 | TrkB:10 nM(Kd) |
体外活性 | 在雄性Sprague-Dawley大鼠中,ANA-12(3 μg/次)阻断内侧核孤束核(mNTS)BDNF对减少食物摄入的作用.在雄性C57BL/6小鼠中,ANA-12(0.5 mg/kg,腹膜内)显示对脂多糖诱导的抑郁样行为的抗抑郁作用.在雄性野生型小鼠中,ANA-12逆转乙醇摄入并诱导D3受体下调,但在D3R -/- 小鼠中无效. |
体内活性 | 在nnr5 PC12-TrkB细胞中,ANA-12在低至10 nM的浓度下阻止脑源性神经营养因子(BDNF)诱导的神经突生长。ANA-12可选择性直接与TrkB受体结合,抑制TrkB下游通路,而不改变TrkA和TrkC功能。ANA-12在DRG神经元中,消除了BDNF对增加内向电流的作用。 |
激酶实验 | ANA-12 Binding assay: Maxisorp ELISA 96-well plates are coated with various concentrations of Trk BECD -Fc, 20 mg/ml BSA, or 1 mg/mL IgG-Fc (polyclonal anti-TrkB) in a carbonate buffer (pH 9.6) overnight at 4°C. Plates are saturated with 0.5% BSA in PBS for 2 hours at room temperature and extensively washed in PBS-Tween 0.05%. Bodipy–ANA-12 is then incubated in 0.5% PBS-BSA for 1 hour at room temperature before the addition of BDNF in 0.5% PBS-BSA for another hour. After extensive washes in PBS-Tween 0.05%, the amount of bodipy–ANA-12 bound is quantified by fluorescence at 520 ± 10 nm. Detectability range for extrapolation analysis is assessed by coating ELISA plates with bodipy–ANA-12 and reading fluorescence at 520 ± 10 nm. |
细胞实验 | Modulation of neurite outgrowth by molecules is assessed in nnr5 PC12–TrkB, –TrkA, and –TrkC cells after addition of BDNF (1 nM), NGF (2 nM), and NT-3 (10 nM), respectively. The number of cells bearing neurites longer than 2 cells in diameter in each counting field is microscopically determined (2 fields per well, 3 wells per condition). Counting is performed blind each 24 hours for 3 days. (Only for Reference) |
别名 | ANA 12, ANA12 |
分子量 | 407.49 |
分子式 | C22H21N3O3S |
CAS No. | 219766-25-3 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
H2O: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 35 mg/mL (85.9 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.454 mL | 12.2702 mL | 24.5405 mL | 61.3512 mL |
5 mM | 0.4908 mL | 2.454 mL | 4.9081 mL | 12.2702 mL | |
10 mM | 0.2454 mL | 1.227 mL | 2.454 mL | 6.1351 mL | |
20 mM | 0.1227 mL | 0.6135 mL | 1.227 mL | 3.0676 mL | |
50 mM | 0.0491 mL | 0.2454 mL | 0.4908 mL | 1.227 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。
ANA-12 219766-25-3 Tyrosine Kinase/Adaptors Trk receptor Tropomyosin related kinase receptor inhibit Trk Receptor ANA 12 ANA12 Inhibitor inhibitor