Name | ANA-12 |
Description | ANA-12 is a potent and selective TrkB antagonist with anxiolytic and antidepressant activity in mice. |
Cell Research | 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) |
Kinase Assay | 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. |
In vitro | 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. |
In vivo | 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。 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
Solubility Information | Ethanol : < 1 mg/mL (insoluble or slightly soluble) H2O : < 1 mg/mL (insoluble or slightly soluble) DMSO : 4.07 mg/mL (10 mM), Sonication is recommended.
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Keywords | Tropomyosin related kinase receptor | inhibit | Trk Receptor | ANA-12 | Inhibitor |
Inhibitors Related | Diosmetin | Amitriptyline hydrochloride | N-Acetyl-5-hydroxytryptamine | Selitrectinib | Sitravatinib | GW 441756 | GNF-5837 | CG 428 | Larotrectinib sulfate | SP600125 | ALE-0540 | 7,8-Dihydroxyflavone |
Related Compound Libraries | 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 |