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- 详细信息
- 文献和实验
- 技术资料
- CAS号:
219766-25-3
- 规格:
1mg/1mLx10mM(inDMSO)/2mg/5mg/10mg/25mg/50mg/100mg
| 规格: | 1mg | 产品价格: | ¥173.0 |
|---|---|---|---|
| 规格: | 1mLx10mM(inDMSO) | 产品价格: | ¥557.0 |
| 规格: | 2mg | 产品价格: | ¥253.0 |
| 规格: | 5mg | 产品价格: | ¥529.0 |
| 规格: | 10mg | 产品价格: | ¥848.0 |
| 规格: | 25mg | 产品价格: | ¥1536.0 |
| 规格: | 50mg | 产品价格: | ¥2544.0 |
| 规格: | 100mg | 产品价格: | ¥3664.0 |
Product Introduction
Bioactivity
| 名称 | ANA-12 |
| 描述 | ANA-12 is a potent and selective TrkB antagonist with anxiolytic and antidepressant activity in mice. |
| 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) |
| 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. |
| 体外活性 | 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。 |
| 体内活性 | 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. |
| 存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度 | Ethanol : < 1 mg/mL (insoluble or slightly soluble) H2O : < 1 mg/mL (insoluble or slightly soluble) DMSO : 4.08 mg/mL (10.01 mM), Sonication is recommended. |
| 关键字 | Tropomyosin related kinase receptor | Trkreceptor | TrkB | Trk Receptor | Inhibitor | inhibit | ANA-12 |
| 相关产品 | Larotrectinib | Tepotinib | Taletrectinib | Amitriptyline hydrochloride | NSI-189 Phosphate | N-Acetyl-5-hydroxytryptamine | GW 441756 | SP600125 | Larotrectinib sulfate | Amitriptyline | ALE-0540 | 7,8-Dihydroxyflavone |
| 相关库 | Inhibitor Library | Bioactive Compound Library | Bioactive Compounds Library Max | Kinase Inhibitor Library | NO PAINS Compound Library | Membrane Protein-targeted Compound Library | Tyrosine Kinase Inhibitor Library | Target-Focused Phenotypic Screening Library | Post-Translational Modification Compound Library |
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文献和实验共轭体系的未共用电子对与水分子易形成氢键。而吡啶、呋喃和噻吩杂原子的未共用电子对是6电子闭合共轭体系的组成部分,失去形成氢键的条件,因此难溶于水。 三、重要的杂环化合物及其衍生物 (一)吡咯、咪唑及其衍生物 吡咯存在于煤焦油和骨焦油中,为无色液体,沸点131℃。吡喀的蒸气可使浸有盐酸的松木片产生红色,称为吡咯的松木片反应。 吡咯的衍生物广泛分布于自然界,叶绿素、血红素、维生素B12及许多生物碱中都含有吡咯环。 四个吡咯环的α碳原子
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由不同种元素组成的纯净物叫做化合物。化合物一般有固定的组成。化合物的组成一般可用化学式表示。化合物具有确定的物理性质和化学性质,不同于其组成元素的性质。化合物中的元素不能用简单的机械方法或物理方法分开,而必须用化学方法才能分离。
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