ANA-12

製品コードS7745 バッチS774501

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C22H21N3O3S
分子量 407.49 CAS No. 219766-25-3
Solubility (25°C)* 体外 DMSO (warmed with 50ºC water bath) 37 mg/mL (90.79 mM)
Water Insoluble
Ethanol Insoluble
体内 （毎回新しく調製した物を用意してください）
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 ANA-12 is a selective TrkB antagonist with Kd of 10 nM and 12 μM for the high and low affinity sites, respectively.
in vitro ANA-12 binds directly and selectively to TrkB and inhibits processes downstream of TrkB without altering TrkA and TrkC functions. In nnr5 PC12-TrkB cells, this compound prevents brain-derived neurotrophic factor (BDNF)-induced neurite outgrowth at concentrations as low as 10 nM. [1] In DRG neurons, this chemical eliminates the effect of BDNF on increasing inward current. [2]
in vivo In adult C57BL6/129SveV F1s mice, ANA-12 (0.5 mg/kg, i.p.) decreases TrKB activity in the brain and reduces the anxiety- and depression-related behaviors without affecting the neuron survival. [1] In male C57BL/6 mice, this compound shows antidepressant-like effects on lipopolysaccharide-induced depression-like behavior. [3] In male Sprague-Dawley rats, this chemical blocks the effect of medial nucleus tractus solitarius (mNTS) BDNF on reducing food intake. [4] In male wild-type mice, it reverses ethanol intake and induces D3 receptor downregulation, but is ineffective in D3R-/- mice. [5] In male CocSired rats, this compound reverses the diminished self-administration of cocaine. [6]

プロトコル(参考用のみ)

キナーゼアッセイ 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–this compound bound is quantified by fluorescence at 520 ± 10 nm. Detectability range for extrapolation analysis is assessed by coating ELISA plates with bodipy–this chemical and reading fluorescence at 520 ± 10 nm.
細胞アッセイ 細胞株 nnr5 PC12–TrkA, nnr5 PC12–TrkB, and nnr5 PC12–TrkC cells
濃度 ~100 μM
反応時間 ~3 days
実験の流れ

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.
動物実験 動物モデル Adult C57BL6/129SveV F1s mice
投薬量 0.5 mg/kg
投与方法 i.p.

参考

  • http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3083767/
  • https://pubmed.ncbi.nlm.nih.gov/24611998/
  • https://pubmed.ncbi.nlm.nih.gov/25628381/
  • https://pubmed.ncbi.nlm.nih.gov/22374757/
  • https://pubmed.ncbi.nlm.nih.gov/24584330/
  • https://pubmed.ncbi.nlm.nih.gov/23242310/

カスタマーフィードバック

Data from [Data independently produced by , , Front Cell Neurosci, 2018, doi:10.3389/fncel.2018.00122]

Data from [Data independently produced by , , Am J Physiol Heart Circ Physiol, 2018, doi:10.1152/ajpheart.00245.2018]

Data from [Data independently produced by , , Neuroscience, 2018, 390:151-159]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

A Novel Gastrodin Derivative with Neuroprotection Promotes NGF-Mimic Activity by Targeting INSR and ACTN4 to Activate PI3K/Akt Signaling Pathway in PC12 Cells [ Antioxidants (Basel), 2025, 14(3)344] PubMed: 40227445
A novel synthetic 3,4,5-tri-feruloylquinic acid enhances learning and memory via neurotrophin signaling in an aging model senescence-accelerated prone 8 mice [ Geroscience, 2025, 10.1007/s11357-025-01783-7] PubMed: 40699486
Neuronal FSTL4 negatively regulates BDNF-mediated neuron-glioma interaction [ Neurochem Int, 2025, 191:106072] PubMed: 41082941
Club cell-derived brain-derived neurotrophic factor regulates murine airway mechanics and mucin production in response to IL-13 in a sex-dependent manner [ Front Physiol, 2025, 16:1578553] PubMed: 40626045
Allium Macrostemon Bge. Attenuates the Cognitive Decline of Aging Mice by Enhancing BDNF/TrkB Pathway [ Food Sci Nutr, 2025, 13(3):e70010] PubMed: 40027296
Isoform-Specific Roles of NTRK2 in Pulmonary Vascular Regeneration [ bioRxiv, 2025, 2025.05.11.653351] PubMed: 40463206
Progressive reduction of nuclear receptor Nr4a1 mediates age-dependent cognitive decline [ Alzheimers Dement, 2024, 10.1002/alz.13819] PubMed: 38605605
HDAC6-dependent deacetylation of NGF dictates its ubiquitination and maintains primordial follicle dormancy [ Theranostics, 2024, 14(6):2345-2366] PubMed: 38646645
A rare olive compound oleacein functions as a TrkB agonist and mitigates neuroinflammation both in vitro and in vivo [ Cell Commun Signal, 2024, 22(1):309] PubMed: 38835076
Exercise-conditioned plasma ameliorates postoperative cognitive dysfunction by activating hippocampal cholinergic circuit and enhancing BDNF/TrkB signaling [ Cell Commun Signal, 2024, 22(1):551] PubMed: 39558340

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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