| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
AMPA receptor GluA2 subunit. ZCAN262 is an AMPA modulator that acts at an allosteric binding site on the AMPA receptor. AMPA receptors are ionotropic glutamate receptors that mediate fast excitatory neurotransmission in the central nervous system. Overactivation of AMPA receptors leads to excitotoxicity, contributing to neuronal damage in various CNS disorders. By modulating AMPA receptor activity, ZCAN262 can prevent excitotoxicity and restore neurological function. Its targeting of the GluA2 subunit suggests a specific modulatory effect.
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| ln Vitro |
In vitro, ZCAN262 has been characterized as an AMPA modulator. It prevents AMPA-mediated excitotoxicity in neuronal cell cultures. Its effects are mediated through an allosteric binding site on the AMPA receptor. It has been shown to be effective in restoring neurological function in mouse models of multiple sclerosis. The compound's in vitro activity is typically assessed using calcium flux assays or electrophysiology in cells expressing AMPA receptors. It is a research tool for studying AMPA receptor function and excitotoxicity.
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| ln Vivo |
In vivo, ZCAN262 exhibits potent effects in restoring neurological function and myelination in mouse models of multiple sclerosis. It has been studied for its potential in CNS disorder research, including stroke, epilepsy, ALS, and Alzheimer's disease. These studies suggest that ZCAN262 has disease-modifying potential in conditions where AMPA receptor overactivation contributes to pathology. The specific dosing, routes of administration, and detailed efficacy data are not provided in the available literature.
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| Enzyme Assay |
In vitro receptor binding assays for ZCAN262 involve radioligand binding to AMPA receptors. The compound is incubated with membrane preparations from cells expressing recombinant AMPA receptors (e.g., GluA2-containing receptors) and a radiolabeled AMPA receptor ligand. Displacement of the radioligand is measured to determine binding affinity (Ki). Allosteric modulation can be assessed by measuring the effect of ZCAN262 on the binding of orthosteric ligands. These assays confirm its interaction with the AMPA receptor.
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| Cell Assay |
In vitro cell-based assays for ZCAN262 are performed in neuronal cell cultures or cells expressing recombinant AMPA receptors. Calcium flux assays are commonly used, where cells are loaded with a calcium-sensitive dye, and receptor activation by AMPA or glutamate is measured as an increase in fluorescence. ZCAN262 is added prior to agonist stimulation, and the inhibition or modulation of the calcium signal is measured. Electrophysiological recordings (patch-clamp) can also be used to directly measure the modulation of AMPA receptor currents. These assays confirm its functional activity as an AMPA modulator.
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| Animal Protocol |
In vivo animal experiments with ZCAN262 have been conducted in mouse models of multiple sclerosis. In these models, mice are treated with ZCAN262, and neurological function is assessed using behavioral tests (e.g., rotarod, EAE score). Myelination is evaluated by histological analysis of spinal cord and brain tissues. The compound has also been studied in models of other CNS disorders. These experiments demonstrate its in vivo efficacy in restoring neurological function and promoting myelination.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of ZCAN262 are not detailed in the available literature. As a small molecule, it is expected to have properties suitable for CNS penetration. It targets the AMPA receptor in the brain, suggesting it crosses the blood-brain barrier. Its solubility, half-life, and bioavailability are unknown. The compound's structure as a pyrrolopyrazole suggests it may have drug-like properties, but specific PK data are not available.
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| Toxicity/Toxicokinetics |
Toxicological data for ZCAN262 are not detailed in the available literature. It is a research compound not intended for human use. No LD50 values or repeated-dose toxicity studies have been reported. Standard safety pharmacology studies have not been performed. As with all research chemicals, appropriate safety precautions should be taken when handling. Its specific toxicity profile has not been established.
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| References | |
| Additional Infomation |
ZCAN262 is an AMPA modulator that prevents AMPA-mediated excitotoxicity by targeting an allosteric binding site. It targets the AMPA receptor GluA2 subunit and exhibits potent effects in restoring neurological function and myelination in mouse models of multiple sclerosis. It is a member of the class of pyrrolopyrazoles. It is suitable for CNS disorder research, including stroke, epilepsy, ALS, and Alzheimer's disease. It is available for research use only.
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| Molecular Formula |
C19H18F2N6O
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| Molecular Weight |
384.38
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| Appearance |
White to off-white solid powder
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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 (~260.16 mM; with sonication (<80°C))
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (6.50 mM) 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; with ultrasonication.
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 and mix well. Then add 50 μL Tween-80 to the above system and mix well. Then continue to add 450 μL of physiological saline to make up 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: 2.5 mg/mL (6.50 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one),clear solution; with ultrasonication. 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 of 20% SBE-β-CD saline solution and mix well. 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: 2.5 mg/mL (6.50 mM) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one),clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6016 mL | 13.0080 mL | 26.0159 mL | |
| 5 mM | 0.5203 mL | 2.6016 mL | 5.2032 mL | |
| 10 mM | 0.2602 mL | 1.3008 mL | 2.6016 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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