2. PROTAC
  3. PROTAC Linkers
  4. 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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TGN-020 Chemical Structure

TGN-020 Chemical Structure

CAS No. : 51987-99-6

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Customer Review

Based on 9 publication(s) in Google Scholar

Other Forms of TGN-020:

TGN-020 Related Antibodies

Top Publications Citing Use of Products

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PEG Linkers Alkyl-Chain Linkers Alkyl/ether Linkers

  • 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

 

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.

TGN-020 Related Antibodies
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

206.22

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
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 16.67 mg/mL (80.84 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 4.8492 mL 24.2460 mL 48.4919 mL
5 mM 0.9698 mL 4.8492 mL 9.6984 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, 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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
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

×
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:  15% Cremophor EL    85% Saline

    Solubility: 25 mg/mL (121.23 mM); Suspended solution; Need ultrasonic

  • Protocol 2

    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% MC  0.5% Tween-80

    Solubility: 5 mg/mL (24.25 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: 99.52%

COA (250 KB) HNMR (112 KB) RP-HPLC (187 KB)

Handling Instructions (2659 KB)
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, 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 4.8492 mL 24.2460 mL 48.4919 mL 121.2298 mL
5 mM 0.9698 mL 4.8492 mL 9.6984 mL 24.2460 mL
10 mM 0.4849 mL 2.4246 mL 4.8492 mL 12.1230 mL
15 mM 0.3233 mL 1.6164 mL 3.2328 mL 8.0820 mL
20 mM 0.2425 mL 1.2123 mL 2.4246 mL 6.0615 mL
25 mM 0.1940 mL 0.9698 mL 1.9397 mL 4.8492 mL
30 mM 0.1616 mL 0.8082 mL 1.6164 mL 4.0410 mL
40 mM 0.1212 mL 0.6061 mL 1.2123 mL 3.0307 mL
50 mM 0.0970 mL 0.4849 mL 0.9698 mL 2.4246 mL
60 mM 0.0808 mL 0.4041 mL 0.8082 mL 2.0205 mL
80 mM 0.0606 mL 0.3031 mL 0.6061 mL 1.5154 mL
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TGN-020 Related Classifications

Help & FAQs
  • 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.

Keywords:

TGN-02051987-99-6TGN020TGN 020PROTAC LinkersAquaporin 4AQP4edemaglialscarInhibitorinhibitorinhibit

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