| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
The primary molecular target of TGN-073 is Aquaporin-4 (AQP4). It is a facilitator (activator) of this astroglial water channel. By enhancing the function of AQP4, TGN-073 increases the flow of fluid through the glymphatic system. The glymphatic system facilitates the clearance of waste products such as amyloid-beta (Abeta) and tau proteins, which are implicated in Alzheimer's disease. The mechanism of action involves increasing water permeability and bulk flow in the perivascular spaces. TGN-073 belongs to the Aquaporin target class.
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| ln Vitro |
In vitro activity data for TGN-073 is limited in publicly available sources. It is known to be an enhancer of AQP4, meaning it increases the water channel activity. This activity is measured in heterologous expression systems (e.g., oocytes or HEK293 cells expressing human AQP4). The compound likely increases the osmotic water permeability (Pf) of the cells. No specific EC50 or IC50 values are provided in the references. TGN-073 is not a potent inhibitor; it is an activator. It is a solid powder with a purity of ≥98% or 99.53% for research use. It is classified as a biochemical assay reagent.
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| ln Vivo |
The in vivo activity of TGN-073 has been demonstrated in a rat model. TGN-073 reveals an increase of up to 41% in glymphatic transport in the rat brain. This is a significant increase, suggesting the compound can cross the blood-brain barrier and functionally activate AQP4 channels in astrocytes. By enhancing clearance of solutes from the interstitial space, TGN-073 shows potential for the treatment of diseases characterized by protein aggregation in the brain, such as Alzheimer's, Parkinson's, and traumatic brain injury (TBI). It is a research chemical and is not FDA-approved for human use. This data is provided in research references[1].
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| Enzyme Assay |
A non-cellular assay for TGN-073 is not typical, as AQP4 is a membrane channel. However, an assay using proteoliposomes (artificial lipid membranes with purified AQP4 reconstituted) can be performed. TGN-073 is added to the external buffer. The osmotic water permeability (Pf) is measured by a stopped-flow light scattering technique. As water moves into the vesicles, they swell, and the light scattering signal decreases. The rate constant (k) is calculated. An increase in k in the presence of TGN-073 (>10 uM) compared to control indicates activation of the channel. The percentage increase is calculated. This confirms direct binding to the purified protein.
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| Cell Assay |
Cellular assays for TGN-073 are performed on primary astrocytes or AQP4-transfected cells. Cells are seeded on coverslips. They are loaded with a fluorescent dye that is sensitive to cell volume (e.g., calcein). The cells are placed in a perfusion chamber. TGN-073 is perfused over the cells. An osmotic gradient is applied (e.g., switching from isotonic to hypotonic buffer). The rate of fluorescence change, which corresponds to cell swelling (volume increase), is measured by time-lapse confocal microscopy. A faster rate of swelling in the presence of TGN-073 indicates enhanced AQP4 activity. The fold-increase over control is calculated. This assay is used to confirm activity in living cells.
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| Animal Protocol |
A standard in vivo experimental protocol for TGN-073 involves a rat model of brain solute clearance. Male Sprague-Dawley rats (250-300g) are anesthetized. A tracer molecule (e.g., fluorescent dextran or amyloid-beta peptide) is injected into the cisterna magna or the striatum. TGN-073 is dissolved in a suitable vehicle (e.g., 10% DMSO, 40% PEG300, 5% Tween-80, 45% saline) and administered intraperitoneally (IP) at a dose of 5-10 mg/kg, 30 minutes before tracer injection. The control group receives vehicle only. After 1-3 hours, the brains are harvested and sectioned. The clearance of the tracer from the brain parenchyma is quantified by fluorescence microscopy. The treated group shows up to 41% less tracer remaining in the brain compared to control, indicating increased glymphatic transport.
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| ADME/Pharmacokinetics |
The pharmacokinetics (PK) of TGN-073 has not been fully characterized in published literature. Based on its molecular weight (340.40) and LogP (estimated ~2-3), it is expected to have moderate lipophilicity and high passive permeability, suggesting it can cross the blood-brain barrier. It is likely metabolized by cytochrome P450 enzymes. The compound is soluble in DMSO (100 mg/mL) and is formulated for in vivo injection using a mixture of DMSO, PEG300, Tween-80, and saline. The compound is stable as a powder at -20degC for 3 years and in solution at -80degC for 6 months. It is a solid powder. It is for research use only.
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| Toxicity/Toxicokinetics |
Specific toxicological data for TGN-073 is not available in the references. As a research chemical, it should be handled as a potentially hazardous substance. It may cause skin and eye irritation. The acute toxicity (LD50) is not known. Standard safety precautions should be taken: wear gloves (nitrile), a lab coat, and safety goggles. Use a fume hood when weighing the powder to avoid inhalation. It is not intended for human consumption. It is a novel compound, and toxicity studies have not been published. It is stored at -20degC. It is an Aquaporin modulator.
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| References | |
| Additional Infomation |
TGN-073 is a significant research compound in the field of glymphatics and neurodegenerative disease. The glymphatic system was discovered relatively recently (2012), and there are few pharmacological tools to modulate it. TGN-073 is one of the few known enhancers of AQP4. By validating TGN-073's ability to increase clearance, researchers can use it as a probe to study whether improving waste clearance can prevent or treat Alzheimer's disease, Parkinson's disease, and normal pressure hydrocephalus. It is not a drug. It is a chemical probe and a facilitator of AQP4. It is a reference compound for aquaporin research. It is not approved by any regulatory agency. It is for research use only. It is a water channel protein stimulant.
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| Molecular Formula |
C18H16N2O3S
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| Molecular Weight |
340.40
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| Exact Mass |
340.088
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| CAS # |
877459-36-4
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| PubChem CID |
4338178
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| Appearance |
Solid powder
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
24
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| Complexity |
465
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1(COC2=CC=CN=C2NS(C2=CC=CC=C2)(=O)=O)=CC=CC=C1
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| InChi Key |
JBHHMMLJGNLVNB-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C18H16N2O3S/c21-24(22,16-10-5-2-6-11-16)20-18-17(12-7-13-19-18)23-14-15-8-3-1-4-9-15/h1-13H,14H2,(H,19,20)
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| Chemical Name |
N-(3-phenylmethoxy-2-pyridinyl)benzenesulfonamide
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~293.77 mM; with ultrasonication (<60°C))
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.34 mM)(saturation unknown) in 10% DMSO 40% PEG300 5% Tween-80 45% Saline (add these co-solvents sequentially from left to right, and one by one),clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution and add it to 400 μL PEG300, mix well; then add 50 μL Tween-80 to the above system, mix well; then continue to add 450 μL of normal saline to make up to 1 mL. Preparation of normal saline: Dissolve 0.9 g of sodium chloride in ddH₂O and make up to 100 mL to obtain a clear and transparent normal saline solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (7.34 mM)(saturation unknown) in 10% DMSO 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one),clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution and add it to 900 μL corn oil and mix well. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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