TGN-073
Based on 1 Customer Validation
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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- Pureté: 99.53%
- CAS No.: 877459-36-4
- Formule: C18H16N2O3S
- Masse moléculaire:340.40
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
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.
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Animal Model:Wistar (male, 20 to 24-weeks old, 300-380 g)[1]
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Dosage:200 mg/kg
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Administration:i.p.; single dose; 30 minutes prior to MRI scanning
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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.
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Animal Model:5xFAD (Alzheimer's disease transgenic strain; 4 months old, treated until 7 months old)[2]
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Dosage:400 mg/kg
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Administration:p.o.; daily; 3 consecutive months
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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.
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Animal Model:ICR-derived (male, body weight 23g)[3]
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Dosage:200 mg/kg
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Administration:i.p.; single dose
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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
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CAS No. 877459-36-4
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Appearance Solid
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Masse moléculaire 340.40
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Formule C18H16N2O3S
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Color White to light yellow
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SMILES
O=S(C1=CC=CC=C1)(NC2=NC=CC=C2OCC3=CC=CC=C3)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
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)
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.
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.
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: ≥ 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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Pureté et documentation
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Fiche technique (283 KB)
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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)
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Instruction de manipulation (2659 KB)
Références
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. 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 |
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| 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 |
TGN-073 Related Classifications
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