TGN 020 |
カタログ番号GC50160
One-Click Copy Product Info
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TGN 020は選択的なアクアポリン4(AQP4)阻害剤であり、IC50値は3μMである。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 51987-99-6
Sample solution is provided at 25 µL, 10mM.
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TGN 020は選択的なアクアポリン4(AQP4)阻害剤であり、IC50値は3μMである[1]。AQP4は主に脳血管あたりのアストロサイトの端の足に分布し、脳の中のイオンと水ホメオスタシスを調節する[2]。TGN 020はアルキル鎖に基づいたタンパク質分解を標的としたキメラ分子(PROTAC)リンカーであり、PROTACの合成に使われることができる[3]。
体外では、TGN 020 (100nM)でTR-MUL5細胞を48-72時間処理した結果、高血糖条件下では、細胞容積の増加と、細胞内ROSの生産を阻害した[4]。
生体内では、脊髄圧迫損傷のラットに、TGN 020 (100mg/kg)を腹腔内注射した結果、脊髄浮腫を減らし、グリア瘢痕形成を阻害し、軸索再生を促進した[5]。TGN 020 (200mg/kg)を、頭部虚血-再潅流障害のマウスに腹腔内注射した結果、障害誘発の炎症と細胞アポトーシスを減らし、リンパ機能を改善し、ERK1/2経路を阻害した[6]。
References:
[1] Nishikawa Y, Oku H, Morishita S, et al. Negative impact of AQP-4 channel inhibition on survival of retinal ganglion cells and glutamate metabolism after crushing optic nerve[J]. Experimental Eye Research, 2016, 146: 118-127.
[2] Rosu G C, Catalin B, Balseanu T A, et al. Inhibition of aquaporin 4 decreases amyloid Aβ40 drainage around cerebral vessels[J]. Molecular neurobiology, 2020, 57: 4720-4734.
[3] Yuan Y, Peng W, Lei J, et al. AQP4 Endocytosis-Lysosome Degradation Mediated by MMP-9/β-DG Involved in Diabetes Cognitive Impairment[J]. Molecular Neurobiology, 2024: 1-16.
[4] Oosuka S, Kida T, Oku H, et al. Effects of an aquaporin 4 inhibitor, TGN-020, on murine diabetic retina[J]. International Journal of Molecular Sciences, 2020, 21(7): 2324.
[5] Li J, Jia Z, Xu W, et al. TGN-020 alleviates edema and inhibits astrocyte activation and glial scar formation after spinal cord compression injury in rats[J]. Life sciences, 2019, 222: 148-157.
[6] Li X, Xie Z, Zhou Q, et al. TGN-020 Alleviate Inflammation and Apoptosis After Cerebral Ischemia–Reperfusion Injury in Mice Through Glymphatic and ERK1/2 Signaling Pathway[J]. Molecular Neurobiology, 2024, 61(2): 1175-1186.
| 細胞実験[1]: | |
細胞株 | TR-MUL5細胞 |
準備方法 | TGN 020 (100nM)またはbevacizumabのある/ない状態下で、細胞を高グルコース（25mM）または生理的低血糖（5.5mM）培地に2-3日間培養した。TR-MUL5と細胞内ROSレベルの量変化は、エチジウム蛍光フローサイトメトリー分析で測定した。 |
反応条件 | 100nM；48-72時間 |
アプリケーション | 高血糖条件下で、細胞容積の増加と細胞内ROSの生成はTGN 020に阻害され、阻害作用はbevacizumabと同じ水準である。 |
| 動物実験 [2]: | |
動物モデル | Sprague-Dawleyラット |
準備方法 | 動物をランダムに下記の三つのグループに分けた：脊髄を圧迫せずに椎弓切除のみ実施した偽手術群、T10で5分間35gのインパウンダー圧縮を受けたSCIグループ、SCIの直後にTGN 020 (100mg/kg、腹腔内)を投与したTGN 020グループ。 Each group was equally and randomly assigned into four subgroups for the following experiments: (A)Spinal cord water content determination; (B)Western blotting; (C)Immunofluorescent assay, Hematoxylin-Eosin staining and Nissl staining; and (D)Locomotor function test. These rats in all groups were sacrificed 3 day or 4weeks after injury. 下記の実験のために、各グループを均一に、ランダムに4つのサブグループに分けた：（A）脊髄含水量の決定；（B）ウエスタンブロット；（C）免疫蛍光アッセイ、Hematoxylin-Eosin染色とNissl染色；（D）運動機能試験。全てのグループのラットを障害の3日後または4週間後に殺処分した。 |
投与形態 | 100mg/kg；腹腔内投与 |
アプリケーション | TGN 020は脊髄浮腫を減らし、グリア瘢痕形成を阻害し、軸索再生を促進でき、ラットの回復に有益な効果を与える。 |
References: | |
| Cas No. | 51987-99-6 | SDF | |
| Canonical SMILES | O=C(NC1=NN=CS1)C2=CN=CC=C2 | ||
| Formula | C8H6N4OS | M.Wt | 206.22 |
| 溶解度 | DMF: 100µ g/ml,DMSO: 2 mg/ml,DMSO:PBS (pH 7.2) (1:9): 100µ g/ml,Ethanol: 100µ g/ml | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 4.8492 mL | 24.246 mL | 48.4919 mL |
| 5 mM | 969.8 μL | 4.8492 mL | 9.6984 mL |
| 10 mM | 484.9 μL | 2.4246 mL | 4.8492 mL |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Quality Control & SDS
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- Purity: >98.00% Appearance: A solid
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Average Rating: 5 (Based on Reviews and 4 reference(s) in Google Scholar.)