- 阻害剤
- 研究分野別
- PI3K/Akt/mTOR
- Epigenetics
- Methylation
- Immunology & Inflammation
- Protein Tyrosine Kinase
- Angiogenesis
- Apoptosis
- Autophagy
- ER stress & UPR
- JAK/STAT
- MAPK
- Cytoskeletal Signaling
- Cell Cycle
- TGF-beta/Smad
- 化合物ライブラリー
- 抗体
- 新製品
- お問い合わせ
ANA-12
ANA-12 is a selective TrkB antagonist with Kd of 10 nM and 12 μM for the high and low affinity sites, respectively.
CAS No. 219766-25-3
文献中Selleckの製品使用例（44）
製品安全説明書
現在のバッチを見る：
純度：
99.97%
99.97
ANA-12関連製品
シグナル伝達経路
Trk receptor阻害剤の選択性比較
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. | ||
|---|---|---|---|
| Targets |
|
| In Vitro | ||||
| 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] | |||
|---|---|---|---|---|
| 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–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. | ||||
| 細胞実験 | 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. |
|||
| 実験結果図 | Methods | Biomarkers | 結果図 | PMID |
| Western blot | MMP-9 p-AKT / AKT |
|
29861866 | |
| In Vivo | ||
| 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] | |
|---|---|---|
| 動物実験 | 動物モデル | Adult C57BL6/129SveV F1s mice |
| 投与量 | 0.5 mg/kg | |
| 投与経路 | i.p. | |
|
化学情報
| 分子量 | 407.49 | 化学式 | C22H21N3O3S |
| CAS No. | 219766-25-3 | SDF | Download ANA-12 SDFをダウンロードする |
| Smiles | C1CCNC(=O)C(C1)NC(=O)C2=CC=CC=C2NC(=O)C3=CC4=CC=CC=C4S3 | ||
| 保管 | |||
|
In vitro |
DMSO : 37 mg/mL ( (90.79 mM)； 吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。) Water : Insoluble Ethanol : Insoluble |
モル濃度計算器 |
|
in vivo Add solvents to the product individually and in order. |
投与溶液組成計算機 | |||||
実験計算
投与溶液組成計算機(クリア溶液)
ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）
mg/kg
g
μL
匹
ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
計算結果：
投与溶媒濃度： mg/ml;
DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )
投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH2O，を加え完全に溶解させます。
投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。
注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。
技術サポート
ストックの作り方、阻害剤の保管方法、細胞実験や動物実験の際に注意すべき点など、製品を取扱う時に問い合わせが多かった質問に対しては取扱説明書でお答えしています。
他に質問がある場合は、お気軽にお問い合わせください。
* 必須
よくある質問（FAQ）
質問1:
Can you test to see if there is a vehicle (<50% DMSO) that it can be dissolved as a clear solution for injection?
回答
S7745 can be dissolved in 20% DMSO/castor oil at 10 mg/ml, and in 40% DMSO/40% PEG 300/20% ddH2O at 10 mg/ml. They are both clear solution. Please dissolve this compound in DMSO first. It dissolves in DMSO not readily, so please sonicate and warm it in water bath at about 45 degree. When it dissolves clearly, then add castor oil or PEG, then ddH2O.
納期 国内在庫品：受注日の翌日（15時までの受注分） ＊北海道、九州、沖縄への配送は受注日より２日以上 を要する場合あり 海外在庫品：受注後１〜２週間