TGN 020
目录号 : GC50160
TGN 020是一种选择性水通道蛋白4（AQP4）抑制剂，IC50值为3μM。
Cas No.:51987-99-6
Sample solution is provided at 25 µL, 10mM.
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TGN 020 is a selective aquaporin 4 (AQP4) inhibitor with an IC50 value of 3μM[1]. AQP4 is mainly located in the astrocyte end feet around brain blood vessels and regulates ion and water homeostasis in the brain[2]. TGN 020 is an alkyl chain-based protein degradation targeted chimeric molecule (PROTAC) linker that can be used for the synthesis of PROTAC[3].
In vitro, TGN 020 (100nM) treatment of TR-MUL5 cells for 48-72h inhibited the increase in cell volume and the production of intracellular ROS under high glucose conditions[4].
In vivo, TGN 020 (100mg/kg) was intraperitoneally injected into rats with spinal cord compression injury, which reduced spinal cord edema, inhibited glial scar formation, and promoted axon regeneration[5]. TGN 020 (200mg/kg) was intraperitoneally injected into mice with cerebral ischemia-reperfusion injury, which reduced injury-induced inflammation and cell apoptosis, improved lymphatic function, and inhibited the ERK1/2 pathway[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.
TGN 020是一种选择性水通道蛋白4（AQP4）抑制剂，IC50值为3μM[1]。AQP4主要位于脑血管周围的星形胶质细胞末足，调节大脑中的离子和水稳态[2]。TGN 020是一种基于烷基链的蛋白降解靶向嵌合分子（PROTAC）接头，可用于PROTAC的合成[3]。
在体外，TGN 020（100nM）处理TR-MUL5细胞48-72h，抑制了高糖条件下细胞体积的增加和细胞内ROS的产生[4]。
在体内，TGN 020（100mg/kg）通过腹腔注射治疗脊髓压迫损伤大鼠，减轻了脊髓水肿，抑制了神经胶质瘢痕形成，促进了轴突再生[5]。TGN 020（200mg/kg）通过腹腔注射治疗脑缺血再灌注损伤小鼠，减轻了损伤引起的炎症和细胞凋亡，改善了淋巴功能，抑制了ERK1/2通路[6]。
| Cell experiment [1]: | |
Cell lines | TR-MUL5 cells |
Preparation Method | Cells were incubated in high glucose (25mM) or physiological low glucose (5.5mM) medium for 2-3 days in the presence or absence of TGN 020 (100nM) or bevacizumab. Volume changes of TR-MUL5 and intracellular ROS levels were determined by flow cytometric analysis of ethidium fluorescence. |
Reaction Conditions | 100nM; 48-72h |
Applications | The increase in cell volume and the production of intracellular ROS under high glucose conditions were inhibited by TGN 020, and the inhibitory effect was as good as that of bevacizumab. |
| Animal experiment [2]: | |
Animal models | Sprague-Dawley rats |
Preparation Method | Animals were randomly assigned to the following three groups: Sham group which were only subject to laminectomy without compression of spinal cord, SCI group which underwent 35g impounder compression for 5min at T10, TGN 020 group which received TGN 020 (100mg/kg, i.p.) immediately followed SCI. 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. |
Dosage form | 100mg/kg; i.p. |
Applications | TGN 020 can alleviate spinal cord edema, inhibit glial scar formation, and promote axonal regeneration, conferring beneficial effects on recovery in rats. |
References: | |
| Cas No. | 51987-99-6 | SDF | |
| Canonical SMILES | O=C(NC1=NN=CS1)C2=CN=CC=C2 | ||
| 分子式 | C8H6N4OS | 分子量 | 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 | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 4.8492 mL | 24.246 mL | 48.4919 mL |
| 5 mM | 0.9698 mL | 4.8492 mL | 9.6984 mL |
| 10 mM | 0.4849 mL | 2.4246 mL | 4.8492 mL |
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动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
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| % DMSO % % Tween 80 % saline | ||||||||||
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Quality Control & SDS
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- Purity: >98.00%
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