TGN-020 sodium
Based on 21 publication(s) in Google Scholar
TGN-020 sodium is a selective Aquaporin 4 (AQP4) inhibitor with an IC50 of 3.1 μM. TGN-020 sodium is an alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs. TGN-020 sodium alleviates edema and inhibits glial scar formation after spinal cord compression injury in rats.
For research use only. We do not sell to patients.
- Purity: 99.96%
- CAS No.: 1313731-99-5
- Formula: C8H5N4NaOS
- Molecular Weight:228.21
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Storage:
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) TGN-020 sodium
More- Adv Sci (Weinh). 2025 Oct 5:e03576. [Abstract]
- J Adv Res. 2025 May 20:S2090-1232(25)00316-9. [Abstract]
- J Adv Res. 2024 Feb:56:125-136. [Abstract]
- Fluids Barriers CNS. 2025 Apr 14;22(1):37. [Abstract]
- Transl Psychiatry. 2023 Oct 6;13(1):310. [Abstract]
- Neurosci Bull. 2025 Nov 18. [Abstract]
- Neurosci Bull. 2022 Feb;38(2):181-199. [Abstract]
- Chin Med. 2023 Oct 10;18(1):128. [Abstract]
- CNS Neurosci Ther. 2025 Jan;31(1):e70140. [Abstract]
- Inflammation. 2025 Apr;48(2):713-729. [Abstract]
- J Cereb Blood Flow Metab. 2024 Aug;44(8):1450-1466. [Abstract]
- Mol Neurobiol. 2025 Jan;62(1):1079-1093. [Abstract]
- Mol Neurobiol. 2024 Feb;61(2):1175-1186. [Abstract]
- Biochim Biophys Acta Mol Cell Res. 2024 Oct 21;1872(1):119866. [Abstract]
- Dis Model Mech. 2023 Oct 1;16(10):dmm050206. [Abstract]
- Neuroscience. 2023 Sep 15:528:64-74. [Abstract]
- Photodiagnosis Photodyn Ther. 2024 Dec:50:104364. [Abstract]
- Behav Brain Res. 2024 Aug 28:115220. [Abstract]
- J Stroke Cerebrovasc Dis. 2022 Aug;31(8):106570. [Abstract]
- SSRN. 2025 Dec 9.
- SSRN. 2025 Nov 11.
Customer Validation & Images
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In Vivo Efficacy Study
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Histological Imaging/Staining
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WB
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WB
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IF
All PROTAC Linkers Isoforms
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Biological Activity
PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein. PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
TGN-020 sodium (100 mg/kg; ip; single dose immediately followed SCI) promotes functional recovery at days 3, 7, 14, 21, and 28, as well as reduces the degree of edema and inhibits the expression of AQP4, GFAP, PCNA at days 3 after SCI[4].
TGN-020 sodium inhibits the glial scar formation and upregulates GAP-43 expression in adult female Sprague-Dawley rats (180-220 g, 9-10 weeks old) with SCI[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1313731-99-5
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Appearance Solid
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Molecular Weight 228.21
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Formula C8H5N4NaOS
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Color White to off-white
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SMILES
O=C(C1=CC=CN=C1)[N-]C2=NN=CS2.[Na+]
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Publications (21)
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Journal Impact Factor
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Most Recent
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Adv Sci (Weinh)
2025 Oct 5:e03576. PMID: 41047470 -
J Adv Res
Aquaporin 4 and its isoforms regulation ameliorate AQP4 Mis-localization-induced glymphatic dysfunction in ischemic stroke. [Abstract]2025 May 20:S2090-1232(25)00316-9. PMID: 40403843
TGN-020 sodium purchased from MedChemExpress. Usage Cited in: J Adv Res. 2025 May 20:S2090-1232(25)00316-9. [Abstract]
TGN-020 (0.1 mg/20 g, administered via intraperitoneal injection every 12 h). Representative T2WI and DWI images of three distinct mouse groups.
TGN-020 sodium purchased from MedChemExpress. Usage Cited in: J Adv Res. 2025 May 20:S2090-1232(25)00316-9. [Abstract]
Schematic of intracerebral injection procedure in mice. Representative fluorescence microscopy images show Ovalbumin (45-kDa, red) inflow into CSF at 30- and 60-minute. The white arrow indicates the residual tracer deposition. Scale bar: 1000 μm. Quantification of Ovalbumin inflow at 30- and 60-minute in brain sections (n = 4 mice per group).
TGN-020 sodium purchased from MedChemExpress. Usage Cited in: J Adv Res. 2025 May 20:S2090-1232(25)00316-9. [Abstract]
TGN-020 (0.1 mg/20 g, administered via intraperitoneal injection every 12 h). Representative Western blot bands and densitometric quantification of AQP4-M1 and AQP4-M23 in the peri-infarction area (n = 6 per group).
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J Adv Res
Matrix metalloproteinase-9 inhibition prevents aquaporin-4 depolarization-mediated glymphatic dysfunction in Parkinson's disease. [Abstract]2024 Feb:56:125-136. PMID: 36940850
TGN-020 sodium purchased from MedChemExpress. Usage Cited in: J Adv Res. 2024 Feb:56:125-136. [Abstract]
TGN-020 (100 mg/kg, i.p.,on the third day) Representative immunoblot bands and densitometric quantification of TH, GFAP, AQP4-M1, AQP4-M23, and AQP4-M23/M1 (n = 6 per group).
TGN-020 sodium purchased from MedChemExpress. Usage Cited in: J Adv Res. 2024 Feb:56:125-136. [Abstract]
TGN-020 (100 mg/kg, i.p., on the third day).Representative 20 × magnification immunofluorescence images of AQP4 (red) and GFAP (green) in the striatum and SN. White dotted squares show the colocalization of AQP4 with astrocyte endfeet.
TGN-020 sodium purchased from MedChemExpress. Usage Cited in: J Adv Res. 2024 Feb:56:125-136. [Abstract]
Quantification of the mean intensity of A594 penetration into the whole brain parenchyma in both Saline and MPTP groups after inhibition of TGN-020 (100 mg/kg, i.p., on the third day) (n = 4–5 per group).
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Fluids Barriers CNS
Reactive astrocyte-derived exosomes enhance intracranial lymphatic drainage in mice after intracranial hemorrhage. [Abstract]2025 Apr 14;22(1):37. PMID: 40229887 -
Transl Psychiatry
Melatonin alleviates depression-like behaviors and cognitive dysfunction in mice by regulating the circadian rhythm of AQP4 polarization. [Abstract]2023 Oct 6;13(1):310. PMID: 37802998 -
Neurosci Bull
Agomelatine Targets Aquaporin-4 Polarization to Rescue Glymphatic Dysfunction in Parkinson's Disease. [Abstract]2025 Nov 18. PMID: 41251938 -
Neurosci Bull
Digoxin Ameliorates Glymphatic Transport and Cognitive Impairment in a Mouse Model of Chronic Cerebral Hypoperfusion. [Abstract]2022 Feb;38(2):181-199. PMID: 34704235 -
Chin Med
Isoforskolin modulates AQP4-SPP1-PIK3C3 related pathway for chronic obstructive pulmonary disease via cAMP signaling. [Abstract]2023 Oct 10;18(1):128. PMID: 37817209 -
CNS Neurosci Ther
2025 Jan;31(1):e70140. PMID: 39853935 -
Inflammation
Neuroprotective Effects of AER-271 in a tMCAO Mouse Model: Modulation of Autophagy, Apoptosis, and Inflammation. [Abstract]2025 Apr;48(2):713-729. PMID: 39117789 -
J Cereb Blood Flow Metab
Long-term isoflurane anesthesia induces cognitive deficits via AQP4 depolarization mediated blunted glymphatic inflammatory proteins clearance. [Abstract]2024 Aug;44(8):1450-1466. PMID: 38443763 -
Mol Neurobiol
2025 Jan;62(1):1079-1093. PMID: 38958889 -
Mol Neurobiol
TGN-020 Alleviate Inflammation and Apoptosis After Cerebral Ischemia-Reperfusion Injury in Mice Through Glymphatic and ERK1/2 Signaling Pathway. [Abstract]2024 Feb;61(2):1175-1186. PMID: 37695472 -
Biochim Biophys Acta Mol Cell Res
Involvement of aquaporins in Shiga toxin-induced swelling and water transport dysfunction in human renal microvascular endothelial cells. [Abstract]2024 Oct 21;1872(1):119866. PMID: 39442808 -
Dis Model Mech
Glycosphingolipids are linked to elevated neurotransmission and neurodegeneration in a Drosophila model of Niemann Pick type C. [Abstract]2023 Oct 1;16(10):dmm050206. PMID: 37815467 -
Neuroscience
2023 Sep 15:528:64-74. PMID: 37516436 -
Photodiagnosis Photodyn Ther
Photobiomodulation reduces spinal cord edema by decreasing the expression of AQP4 in the astrocytes of male spinal cord injury rats via the JAK2/STAT3 signaling pathway. [Abstract]2024 Dec:50:104364. PMID: 39401645 -
Behav Brain Res
AQP4 is upregulated in schizophrenia and Its inhibition attenuates MK-801-induced schizophrenia-like behaviors in mice. [Abstract]2024 Aug 28:115220. PMID: 39214422 -
J Stroke Cerebrovasc Dis
Downregulation of NF-κB by Shp-1 Alleviates Cerebral Venous Sinus Thrombosis-Induced Brain Edema Via Suppression of AQP4. [Abstract]2022 Aug;31(8):106570. PMID: 35636226 -
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Solvent & Solubility
H2O : 3.33 mg/mL (14.59 mM; ultrasonic and warming and heat to 60°C)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 5 mg/mL (21.91 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 5 mg/mL (21.91 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: Saline
Solubility: 10 mg/mL (43.82 mM); Clear solution; Need ultrasonic
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
Purity & Documentation
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Data Sheet (278 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Vincent J Huber, et al. Identification of aquaporin 4 inhibitors using in vitro and in silico methods. Bioorg Med Chem. 2009 Jan 1;17(1):411-7. [Content Brief]
[2]. Shou Oosuka, et al. Effects of an Aquaporin 4 Inhibitor, TGN-020, on Murine Diabetic Retina. Int J Mol Sci. 2020 Mar 27;21(7):2324. [Content Brief]
[3]. An S, et al. Small-molecule PROTACs: An emerging and promising approach for the development of targeted therapy drugs. EBioMedicine. 2018 Oct;36:553-562. [Content Brief]
[4]. Jian Li, et al. TGN-020 alleviates edema and inhibits astrocyte activation and glial scar formation after spinal cord compression injury in rats. Life Sci. 2019 Apr 1;222:148-157. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O | 1 mM | 4.3819 mL | 21.9095 mL | 43.8189 mL | 109.5473 mL |
| 5 mM | 0.8764 mL | 4.3819 mL | 8.7638 mL | 21.9095 mL | |
| 10 mM | 0.4382 mL | 2.1909 mL | 4.3819 mL | 10.9547 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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