Art. -Nr.: HY-W176557

TGN-073

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TGN-073 is an orally active, blood-brain barrier-permeable aquaporin 4 (AQP4) modulator. TGN-073 increases the uptake and distribution of brain MRI tracers in the brain parenchyma and reduces the levels of insoluble amyloid β-40 and β-42. TGN-073 can be used in research related to Alzheimer's disease, dementia, traumatic brain injury and pain.

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Reinheit: 99.53%
CAS. Nr.: 877459-36-4
Formel: C₁₈H₁₆N₂O₃S
Molecular Weight:340.40

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

TGN-073 Chemical Structure

CAS. Nr.: 877459-36-4

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Biologische Aktivität
- Beschreibung
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

In Vivo

TGN-073 (200 mg/kg; i.p.; single dose; 30 minutes prior to MRI scanning) significantly enhances glymphatic transport (evidenced by up to 41% greater whole-brain contrast enhancement and regional signal increases) and increases water diffusivity in normal male Wistar rats^[1].
TGN-073 (400 mg/kg; p.o.; daily; 3 consecutive months) prevents insoluble amyloid β₄₀ and β₄₂ accumulation in the brain parenchyma of 5xFAD mice^[2].
TGN-073 (200 mg/kg; i.p.; single dose) produces a virtually complete, statistically significant block of nociceptive writhing in the acetic acid writhing test model in male ICR-derived mice^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Wistar (male, 20 to 24-weeks old, 300-380 g)^[1]
Dosage:

200 mg/kg
Administration:

i.p.; single dose; 30 minutes prior to MRI scanning
Result:

Increased prefrontal cortex signal change by 51%.
Increased cerebellum signal change by 34%.
Achieved up to 41% increase in whole-brain contrast enhancement compared to vehicle.
Increased cerebral cortex apparent diffusion coefficient (ADC).
Increased striatum ADC to 0.00074 mm²/s.
Increased whole-brain ADC to 0.00079 mm²/s.

Animal Model:

5xFAD (Alzheimer's disease transgenic strain; 4 months old, treated until 7 months old)^[2]
Dosage:

400 mg/kg
Administration:

p.o.; daily; 3 consecutive months
Result:

Decreased insoluble amyloid β₄₀ and insoluble amyloid β₄₂ in the brain parenchyma.
Showed no significant effect on soluble amyloid β₄₀ or soluble amyloid β₄₂.

Animal Model:

ICR-derived (male, body weight 23g)^[3]
Dosage:

200 mg/kg
Administration:

i.p.; single dose
Result:

Produced a virtually complete block of writhes across all 5-minute intervals (0-5, 5-10, 10-15, 15-20 minutes), with statistically significant reduction relative to vehicle.
Reduced total writhes to near-zero levels over the full 20-minute period, with statistically significant reduction relative to vehicle.

Chemical Information

CAS. Nr. 877459-36-4
Appearance Solid
Molecular Weight 340.40
Formel C₁₈H₁₆N₂O₃S
Color White to light yellow
SMILES

O=S(C1=CC=CC=C1)(NC2=NC=CC=C2OCC3=CC=CC=C3)=O
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (293.77 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

2.9377 mL

14.6886 mL

29.3772 mL

5 mM

0.5875 mL

2.9377 mL

5.8754 mL

10 mM

0.2938 mL

1.4689 mL

2.9377 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (7.34 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.

Protocol 2

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

Solubility: ≥ 2.5 mg/mL (7.34 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 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 (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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 (283 KB)
SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 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]. Alghanimy A, et al. The effect of a novel AQP4 facilitator, TGN-073, on glymphatic transport captured by diffusion MRI and DCE-MRI. PLoS One. 2023;18(3):e0282955. Published 2023 Mar 15. [Content Brief]

[2]. Ingrid L. Kwee, et al. Aquaporin4 facilitator decreases insoluble amyloid b of 5XFAD mouse brain. Alzheimer's Association. 07 December 2020.

[3]. Vincent J. et al. Aquaporin-4 facilitator TGN-073 demonstrates novel analgesic activity. bioRxiv. October 08, 2018.

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, 6 months; -20°C, 1 month. 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
DMSO	1 mM	2.9377 mL	14.6886 mL	29.3772 mL	73.4430 mL
	5 mM	0.5875 mL	2.9377 mL	5.8754 mL	14.6886 mL
	10 mM	0.2938 mL	1.4689 mL	2.9377 mL	7.3443 mL
	15 mM	0.1958 mL	0.9792 mL	1.9585 mL	4.8962 mL
	20 mM	0.1469 mL	0.7344 mL	1.4689 mL	3.6722 mL
	25 mM	0.1175 mL	0.5875 mL	1.1751 mL	2.9377 mL
	30 mM	0.0979 mL	0.4896 mL	0.9792 mL	2.4481 mL
	40 mM	0.0734 mL	0.3672 mL	0.7344 mL	1.8361 mL
	50 mM	0.0588 mL	0.2938 mL	0.5875 mL	1.4689 mL
	60 mM	0.0490 mL	0.2448 mL	0.4896 mL	1.2241 mL
	80 mM	0.0367 mL	0.1836 mL	0.3672 mL	0.9180 mL
	100 mM	0.0294 mL	0.1469 mL	0.2938 mL	0.7344 mL

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TGN-073

Membrane Transporter/Ion Channel Compound Library

Neuronal Signaling Compound Library

CNS-Penetrant Compound Library

Orally Active Compound Library

Anti-Alzheimer's Disease Compound Library

Neurodegenerative Disease-related Compound Library

Ion Channel Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

MCE Kinase Hinge Binder Fragment Library

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

TGN-073

Membrane Transporter/Ion Channel Compound Library

Neuronal Signaling Compound Library

CNS-Penetrant Compound Library

Orally Active Compound Library

Anti-Alzheimer's Disease Compound Library

Neurodegenerative Disease-related Compound Library

Ion Channel Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

MCE Kinase Hinge Binder Fragment Library

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

TGN-073 Related Classifications

HY-W176557 Related Classifications