| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| Other Sizes |
Purity: ≥98%
| Targets |
CX546 targets AMPA receptors, which are ionotropic glutamate receptors important for synaptic transmission and plasticity in the brain. It acts as a positive allosteric modulator, enhancing the activity of AMPA receptors without directly acting as a conventional agonist. It binds specifically to the agonist-bound non-desensitized receptor, and most likely destabilizes the desensitized receptor conformation.
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|---|---|
| ln Vitro |
CX546 is a positive modulator of AMPA receptors. It enhances the activity of AMPA receptors, which are important for synaptic transmission and plasticity in the brain. It binds specifically to the agonist-bound non-desensitized receptor, and most likely destabilizes the desensitized receptor conformation. It exhibits specificity for different combinations of receptor subunits and TARP variants.
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| ln Vivo |
In cultured rat entorhinal/hippocampal slices, treatment with ampakine CX614 (intraperitoneal injection) raises brain-derived neurotrophic factor (BDNF) mRNA and protein levels considerably and reversibly [1].
CX546 has been investigated for its potential in treating schizophrenia, reversing respiratory depression, relieving pain, promoting neurogenesis, and improving synaptic plasticity. It has demonstrated antipsychotic action by restoring prepulse inhibition. It has shown significant efficacy in reversing respiratory depression caused by sedative drugs like opioids and barbiturates without reducing the analgesic effects. Systemic administration of CX546 has reduced mechanical hypersensitivity and depressive features of pain in animal models. |
| Enzyme Assay |
CX546 is evaluated in cell-free receptor binding assays to determine its affinity for AMPA receptors. Radioligand binding displacement assays are performed using membrane preparations expressing AMPA receptor subunits. Competition binding experiments are conducted with increasing concentrations of CX546 and a fixed concentration of a labeled reference ligand.
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| Cell Assay |
CX546 is assessed in cell-based electrophysiological assays using neurons or cells expressing AMPA receptors. The compound's ability to modulate AMPA receptor activity is measured by assessing its effects on excitatory postsynaptic currents and receptor kinetics. It enhances excitatory postsynaptic currents at cerebellar parallel fiber to Purkinje cell synapses.
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| Animal Protocol |
CX546 is administered in animal models to evaluate its antipsychotic, analgesic, and cognitive-enhancing effects. It has been studied in models of schizophrenia, pain, and respiratory depression. Efficacy is assessed using behavioral tests and physiological measurements.
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| ADME/Pharmacokinetics |
CX546 has a molecular weight of 247.29 and a molecular formula of C14H17NO3. It has a CAS number of 215923-54-9. The compound is soluble in DMSO. It should be stored under recommended conditions.
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| Toxicity/Toxicokinetics |
No detailed toxicity data is available for CX546. The compound is for research use only and is not intended for human therapeutic use. It is an investigational compound that has been proposed as a treatment for schizophrenia. Its safety profile has not been extensively characterized in the available literature.
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| References |
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| Additional Infomation |
CX546 is an ampakine drug that was initially developed by Cortex Pharmaceuticals. It is a positive allosteric modulator of AMPA receptors. The compound has a CAS number of 215923-54-9. It has been proposed as a treatment for schizophrenia. It is not approved for clinical use.
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| Molecular Formula |
C14H17NO3MOLECULARWEIGHT
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|---|---|
| Molecular Weight |
247.2897
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| Exact Mass |
247.121
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| CAS # |
215923-54-9
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| Related CAS # |
215923-54-9
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| PubChem CID |
2890
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| Appearance |
White to off-white solid powder
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| Density |
1.215g/cm3
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| Boiling Point |
422.8ºC at 760 mmHg
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| Flash Point |
209.5ºC
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| Vapour Pressure |
2.34E-07mmHg at 25°C
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| Index of Refraction |
1.573
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| LogP |
2.021
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
18
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| Complexity |
301
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
LJUNPHMOGNFFOS-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C14H17NO3/c16-14(15-6-2-1-3-7-15)11-4-5-12-13(10-11)18-9-8-17-12/h4-5,10H,1-3,6-9H2
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| Chemical Name |
2,3-dihydro-1,4-benzodioxin-6-yl(piperidin-1-yl)methanone
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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 (~404.38 mM)
Ethanol : ~100 mg/mL (~404.38 mM) H2O : ~2 mg/mL (~8.09 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (10.11 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 25.0 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: ≥ 2.5 mg/mL (10.11 mM) (saturation unknown) 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. 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 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: ≥ 2.5 mg/mL (10.11 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: ≥ 2.5 mg/mL (10.11 mM) (saturation unknown) in 10% EtOH + 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 25.0 mg/mL clear EtOH stock solution to 400 μL of PEG300 and mix evenly; then add 50 μL of Tween-80 to the above solution and mix evenly; then add 450 μL of 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 5: ≥ 2.5 mg/mL (10.11 mM) (saturation unknown) in 10% EtOH + 90% (20% SBE-β-CD in 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 EtOH 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. Solubility in Formulation 6: ≥ 2.5 mg/mL (10.11 mM) (saturation unknown) in 10% EtOH + 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 EtOH stock solution to 900 μL of corn oil and mix evenly. Solubility in Formulation 7: 2 mg/mL (8.09 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. Solubility in Formulation 8: 4 mg/mL (16.18 mM) in 20% HP-β-CD in Saline (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.0438 mL | 20.2192 mL | 40.4384 mL | |
| 5 mM | 0.8088 mL | 4.0438 mL | 8.0877 mL | |
| 10 mM | 0.4044 mL | 2.0219 mL | 4.0438 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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