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 37 mg/mL warmed with 50ºC water bath (90.79 mM)
Water Insoluble
Ethanol Insoluble
* <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, ANA-12 prevents brain-derived neurotrophic factor (BDNF)-induced neurite outgrowth at concentrations as low as 10 nM. [1] In DRG neurons, ANA-12 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, ANA-12 (0.5 mg/kg, i.p.) shows antidepressant-like effects on lipopolysaccharide-induced depression-like behavior. [3] In male Sprague-Dawley rats, ANA-12 (3 μg/dose) blocks the effect of medial nucleus tractus solitarius (mNTS) BDNF on reducing food intake. [4] In male wild-type mice, ANA-12 reverses ethanol intake and induces D3 receptor downregulation, but is ineffective in D3R-/- mice. [5] In male CocSired rats, ANA-12 (0.5 mg/kg, i.p.) 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–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.
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.

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：

Hepatic stellate cells maintain liver homeostasis through paracrine neurotrophin-3 signaling that induces hepatocyte proliferation [ Sci Signal, 2023, 16(787):eadf6696] PubMed: 37253090
Periplaneta Americana (L.) extract activates the ERK/CREB/BDNF pathway to promote post-stroke neuroregeneration and recovery of neurological functions in rats [ J Ethnopharmacol, 2023, 10.1016/j.jep.2023.117400] PubMed: 37952730
Utility of 7,8-dihydroxyflavone in preventing astrocytic and synaptic deficits in the hippocampus elicited by PTSD [ Pharmacol Res, 2022, 176:106079] PubMed: 35026406
lncRNA BDNF-AS Attenuates Propofol-Induced Apoptosis in HT22 Cells by Modulating the BDNF/TrkB Pathway [ Mol Neurobiol, 2022, 10.1007/s12035-022-02757-y] PubMed: 35338452
Reduced BDNF expression in the auditory cortex contributed to neonatal pain-induced hearing impairment and dendritic pruning deficiency in mice [ Reg Anesth Pain Med, 2022, rapm-2022-103621] PubMed: 36384877
Atorvastatin inhibits neuronal apoptosis via activating cAMP/PKA/p-CREB/BDNF pathway in hypoxic-ischemic neonatal rats [ FASEB J, 2022, 36(4):e22263] PubMed: 35303316
[ANA- 12 inhibits spinal inflammation and alleviates acute and chronic pain in rats by targeted blocking of BDNF/TrkB signaling] [ Nan Fang Yi Ke Da Xue Xue Bao, 2022, 42(2):232-237] PubMed: 35365447
Melatonin protects inner retinal neurons of newborn mice after hypoxia-ischemia [ J Pineal Res, 2021, 71(1):e12716] PubMed: 33426650
Striatal Shati/Nat8l-BDNF pathways determine the sensitivity to social defeat stress in mice through epigenetic regulation [ Neuropsychopharmacology, 2021, 10.1038/s41386-021-01033-2] PubMed: 34099867
Striatal Shati/Nat8l-BDNF pathways determine the sensitivity to social defeat stress in mice through epigenetic regulation [ Neuropsychopharmacology, 2021, 46(9):1594-1605] PubMed: 34099867

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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