1. PROTAC
  2. PROTAC Linkers
  3. TGN-020

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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CAS No. : 51987-99-6

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Customer Review

Based on 21 publication(s) in Google Scholar

Other Forms of TGN-020:

Top Publications Citing Use of Products

    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).

    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).

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    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    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

     

    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.

    Molecular Weight

    206.23

    Formula

    C8H6N4OS

    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

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

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage

    Store at room temperature 3 years

    In solvent -80°C 2 years
    -20°C 1 year
    Solvent & Solubility
    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)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 4.8490 mL 24.2448 mL 48.4896 mL
    5 mM 0.9698 mL 4.8490 mL 9.6979 mL
    View the 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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    • Molarity Calculator

    • Dilution Calculator

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

    Mass
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    Concentration
    ×
    Volume
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    Molecular Weight *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

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    Volume (final)

    V2

    In Vivo:

    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.

    • 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.

    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

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    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).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 99.97%

    References

    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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    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
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    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    Product Name:
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