Art. -Nr.: HY-W008574

TGN-020

25 Cited Publications

Kundenbewertung

Based on 25 publication(s) in Google Scholar

TGN-020 is a selective Aquaporin 4 (AQP4) inhibitor with an IC₅₀ of 3.1 μM. TGN-020 is an alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs.TGN-020 alleviates edema and inhibits glial scar formation after spinal cord compression injury in rats.

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Reinheit: 99.97%
CAS. Nr.: 51987-99-6
Formel: C₈H₆N₄OS
Molecular Weight:206.23

Speicherung:

Store at room temperature 3 years.

In solvent -80°C, 2 years , -20°C, 1 year

TGN-020 Chemical Structure

CAS. Nr.: 51987-99-6

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (25)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

TGN-020 is a selective Aquaporin 4 (AQP4) inhibitor with an IC₅₀ of 3.1 μM^[1]^[2]. TGN-020 is an alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs^[3].TGN-020 alleviates edema and inhibits glial scar formation after spinal cord compression injury in rats^[4].

IC₅₀ & Target

Alkyl-Chain

Alle PROTAC Linkers Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
Oocyte	IC₅₀	3.1 μM Compound: 9	Inhibition of human aquaporin 4 M23 isoform expressed in Xenopus laevis oocytes Inhibition of human aquaporin 4 M23 isoform expressed in Xenopus laevis oocytes	[PMID: 18182301]

In Vitro

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.

In Vivo

TGN-020 (0.02 mg/μL; two microliter intravitreal injections) can suppress retinal edema in STZ-induced diabetic rats (nine-week-old male Wistar rats) retinas^[2].
TGN-020 (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. TGN-020 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

CAS. Nr. 51987-99-6
Appearance Solid
Molecular Weight 206.23
Formel C₈H₆N₄OS
Color White to off-white
SMILES

O=C(C1=CC=CN=C1)NC2=NN=CS2
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Store at room temperature 3 years

In solvent	-80°C	2 years
	-20°C	1 year

Publications (25)

All In Vivo Efficacy StudyHistological Imaging/StainingIFWB

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Journal Impact Factor

Adv Sci (Weinh)

Potentiating Cerebral Perfusion Normalizes Glymphatic Dynamics in Systemic Inflammation. [Abstract]

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 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 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 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).
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 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 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 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).
Brain Behav Immun

Role of AQP4 mediated glymphatic system dysfunction in postoperative neuroinflammation and cognitive dysfunction. [Abstract]

2026 May 8:106797. PMID: 42107812
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
Microchem J

2026 May 1;225:118246.
CNS Neurosci Ther

NOTCH3 Mutation Causes Glymphatic Impairment and Promotes Brain Senescence in CADASIL. [Abstract]

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

Long-Term High-Fat Diet Impairs AQP4-Mediated Glymphatic Clearance of Amyloid Beta. [Abstract]

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

Glymphatic Dysfunction in Migraine Mice Model. [Abstract]

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
Res Sq

2026 Jun 13.
Res Sq

2026 Apr 29.
SSRN

2025 Dec 9.
SSRN

2025 Nov 11.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 16.67 mg/mL (80.83 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

4.8490 mL

24.2448 mL

48.4896 mL

5 mM

0.9698 mL

4.8490 mL

9.6979 mL

10 mM

0.4849 mL

2.4245 mL

4.8490 mL

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 1.67 mg/mL (8.10 mM); Clear solution

This protocol yields a clear solution of ≥ 1.67 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 mg/mL) to 900 μL Corn oil, and mix evenly.

Working Solution

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.

Protocol 1

Add each solvent one by one: 0.5% Methyl cellulose/0.5% Tween-80 in Saline water

Solubility: 5 mg/mL (24.24 mM); Suspended solution; Need ultrasonic

Protocol 2

Add each solvent one by one: 15% Cremophor EL 85% Saline

Solubility: 25 mg/mL (121.22 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (277 KB)
SDS (392 KB)
- English - EN (392 KB)
- Français - FR (392 KB)
- Deutsch - DE (392 KB)
- Norwegian - NO (392 KB)
- Español - ES (392 KB)
- Swedish - SV (392 KB)
- Italian - IT (392 KB)
- Korean - KR (392 KB)
- Portuguese - PT (392 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	4.8490 mL	24.2448 mL	48.4896 mL	121.2239 mL
	5 mM	0.9698 mL	4.8490 mL	9.6979 mL	24.2448 mL
	10 mM	0.4849 mL	2.4245 mL	4.8490 mL	12.1224 mL
	15 mM	0.3233 mL	1.6163 mL	3.2326 mL	8.0816 mL
	20 mM	0.2424 mL	1.2122 mL	2.4245 mL	6.0612 mL
	25 mM	0.1940 mL	0.9698 mL	1.9396 mL	4.8490 mL
	30 mM	0.1616 mL	0.8082 mL	1.6163 mL	4.0408 mL
	40 mM	0.1212 mL	0.6061 mL	1.2122 mL	3.0306 mL
	50 mM	0.0970 mL	0.4849 mL	0.9698 mL	2.4245 mL
	60 mM	0.0808 mL	0.4041 mL	0.8082 mL	2.0204 mL
	80 mM	0.0606 mL	0.3031 mL	0.6061 mL	1.5153 mL

Keywords

TGN-020

25 Cited Publications

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TGN-020

Publications Citing Use of MedChemExpress (MCE) TGN-020

Alle PROTAC Linkers Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (25)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

TGN-020 Related Classifications

HY-W008574 Related Classifications