| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
pIC50: AMPA receptor (10.1)[1].
AMPA (α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid) receptor, specifically TARPγ2-dependent AMPA receptors. AMPA receptor modulator-2 acts as a positive modulator of AMPA receptor function. |
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| ln Vitro |
AMPA receptor modulator-2 is a potent modulator of AMPA receptors with a pIC50 of 10.1 at TARPγ2-dependent AMPA receptors. By positively modulating AMPA receptor function, it promotes synaptic plasticity, learning, and memory formation. The compound's potent modulatory activity makes it a valuable tool for studying the role of AMPA receptors in cognitive function and neurological disorders.
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| ln Vivo |
No detailed in vivo activity data are publicly available for AMPA receptor modulator-2. As a positive modulator of AMPA receptors, its in vivo effects would be expected to be related to enhancement of glutamatergic neurotransmission. Positive AMPA receptor modulators (also known as ampakines) have been shown to improve cognitive function in animal models and are being investigated as potential treatments for cognitive impairment in Alzheimer's disease, schizophrenia, and depression.
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| Enzyme Assay |
In vitro receptor binding assays for AMPA receptor modulator-2 are performed to evaluate its affinity for AMPA receptors. Radioligand binding studies using membrane preparations from cells expressing AMPA receptors and TARPγ2 are conducted. The compound's ability to modulate AMPA receptor activity is assessed using functional assays that measure receptor-mediated ion flux or downstream signaling.
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| Cell Assay |
In vitro cell-based assays are conducted using cells expressing recombinant AMPA receptors and TARPγ2. The cells are treated with AMPA receptor modulator-2 in the presence of a sub-maximal concentration of glutamate, and receptor activity is measured by assessing ion flux or calcium mobilization. The potentiation of receptor activity is quantified to determine the compound's modulatory potency.
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| Animal Protocol |
In vivo studies would be conducted in animal models to evaluate the cognitive-enhancing effects of AMPA receptor modulator-2. The compound could be administered via various routes, and its effects on learning and memory tasks, such as the Morris water maze or novel object recognition, could be assessed.
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| ADME/Pharmacokinetics |
No detailed pharmacokinetic data are publicly available for AMPA receptor modulator-2. As a research compound, its ADME properties would be characterized in standard preclinical studies to guide in vivo experiments. The compound's ability to cross the blood-brain barrier is a key parameter for its use in CNS research.
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| Toxicity/Toxicokinetics |
No specific toxicity data are publicly available for AMPA receptor modulator-2. As a positive modulator of AMPA receptors, its toxicity profile would be expected to be related to its mechanism of action. Excessive AMPA receptor activation can lead to excitotoxicity, which could manifest as neuronal damage or seizure activity.
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| References | |
| Additional Infomation |
AMPA receptor modulator-2 is a potent and selective modulator of AMPA receptors with a pIC50 of 10.1 at TARPγ2-dependent AMPA receptors. It is used as a research tool to study the role of AMPA receptors in synaptic plasticity, learning, memory, and neurological disorders. The compound is of particular interest in the development of cognitive enhancers and potential treatments for Alzheimer's disease, schizophrenia, and depression. It is not approved for human therapeutic use and is strictly for research purposes.
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| Molecular Formula |
C15H6F6N4OS
|
|---|---|
| Molecular Weight |
404.2898
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| Exact Mass |
404.016
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| CAS # |
2034181-36-5
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| PubChem CID |
122654476
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| Appearance |
White to off-white solid powder
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| LogP |
4
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
27
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| Complexity |
602
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| Defined Atom Stereocenter Count |
0
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| SMILES |
S1C(N([H])C2C([H])=C([H])C(=C([H])C1=2)N1C(C(F)(F)F)=NC2C([H])=C([H])C(C(F)(F)F)=NC1=2)=O
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| InChi Key |
BPZAQDCXSKBMKM-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C15H6F6N4OS/c16-14(17,18)10-4-3-8-11(24-10)25(12(22-8)15(19,20)21)6-1-2-7-9(5-6)27-13(26)23-7/h1-5H,(H,23,26)
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| Chemical Name |
6-[2,5-bis(trifluoromethyl)imidazo[4,5-b]pyridin-3-yl]-3H-1,3-benzothiazol-2-one
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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: 250 mg/mL (618.37 mM)
H2O: < 0.1 mg/mL |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.14 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 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 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.08 mg/mL (5.14 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (5.14 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4735 mL | 12.3674 mL | 24.7347 mL | |
| 5 mM | 0.4947 mL | 2.4735 mL | 4.9469 mL | |
| 10 mM | 0.2473 mL | 1.2367 mL | 2.4735 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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