TGN 020 |
Katalog-Nr.GC50160
One-Click Copy Product Info
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TGN 020 ist ein selektiver Aquaporin 4 (AQP4)-Inhibitor mit einem IC50-Wert von 3,1 μM.
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 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.
| Cell experiment [1]: | |
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Cell lines |
TR-MUL5 cells |
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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. |
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Reaction Conditions |
100nM; 48-72h |
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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]: | |
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Animal models |
Sprague-Dawley rats |
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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. |
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Dosage form |
100mg/kg; i.p. |
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Applications |
TGN 020 can alleviate spinal cord edema, inhibit glial scar formation, and promote axonal regeneration, conferring beneficial effects on recovery in rats. |
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References: |
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| Cas No. | 51987-99-6 | SDF | |
| Canonical SMILES | O=C(NC1=NN=CS1)C2=CN=CC=C2 | ||
| Formula | C8H6N4OS | M.Wt | 206.22 |
| Löslichkeit | 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 |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
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.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 4 reference(s) in Google Scholar.)