| Size | Price | Stock | Qty |
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| 1mg |
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| Other Sizes |
| Targets |
AMPA receptor antagonist-3 targets the AMPA receptor, a subtype of ionotropic glutamate receptor that mediates fast excitatory neurotransmission in the central nervous system. AMPA receptors are composed of four subunits (GluA1-4) and are involved in synaptic plasticity, learning, and memory. By antagonizing AMPA receptors, the compound blocks glutamate-mediated excitatory neurotransmission, which can have anticonvulsant, neuroprotective, and analgesic effects.
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| ln Vitro |
AMPA receptor antagonist-3 is a selective antagonist of the AMPA receptor. It blocks glutamate-mediated excitatory neurotransmission. The compound's specific IC50 values for AMPA receptor inhibition and its selectivity over other glutamate receptor subtypes (such as NMDA and kainate receptors) are not extensively documented. It is used in neuroscience research to study the role of AMPA receptors in neurological and psychiatric disorders.
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| ln Vivo |
In vivo, AMPA receptor antagonist-3 is used in research to study the role of AMPA receptors in neurological and psychiatric disorders. As an AMPA receptor antagonist, it may have anticonvulsant, neuroprotective, and analgesic effects in animal models. Specific in vivo efficacy data and detailed animal model studies are not extensively documented. The compound is intended for research use only.
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| Enzyme Assay |
The in vitro receptor binding assay for AMPA receptor antagonist-3 typically involves measuring its affinity for the AMPA receptor using radioligand binding. Membrane preparations from cells expressing AMPA receptors are incubated with varying concentrations of the compound (typically 0.001-100 µM) and a radiolabeled ligand such as [3H]AMPA. The binding affinity is determined by competition binding analysis. The compound is dissolved in DMSO and diluted in assay buffer.
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| Cell Assay |
In vitro cellular assays for AMPA receptor antagonist-3 typically involve treating neurons or cells expressing AMPA receptors with the compound at concentrations ranging from 0.001 to 10 µM. Receptor antagonism is assessed by measuring the inhibition of AMPA-induced calcium influx using fluorescent calcium indicators or by electrophysiological recordings. Cell viability is assessed using MTT or other standard assays. The compound is dissolved in DMSO and diluted in cell culture medium.
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| Animal Protocol |
In vivo animal studies for AMPA receptor antagonist-3 typically involve administration to mice or rats via oral gavage or intraperitoneal injection at doses determined from preliminary studies. Seizure models, neuroprotection models, or pain models are used to evaluate efficacy. Seizure activity, neuroprotection, and pain-related behaviors are assessed. The compound's pharmacokinetics and pharmacodynamics are evaluated in these models.
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| ADME/Pharmacokinetics |
AMPA receptor antagonist-3 has a molecular weight of 363.39 g/mol and formula C20H20FNO4. It is soluble in DMSO and other organic solvents. Recommended storage is powder at -20°C for up to 3 years and in solvent at -80°C for up to 6 months. Detailed PK parameters such as half-life, Cmax, AUC, and bioavailability would require experimental determination.
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| Toxicity/Toxicokinetics |
AMPA receptor antagonist-3 is intended for research use only and is not approved for human therapeutic applications. As an AMPA receptor antagonist, it may affect normal excitatory neurotransmission, which could contribute to potential side effects such as sedation, cognitive impairment, or motor deficits. Standard preclinical toxicity assessments would include acute toxicity studies in rodents, repeated-dose toxicity studies, and assessment of off-target effects.
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| Additional Infomation |
AMPA receptor antagonist-3 (CAS 923272-18-8) is a selective antagonist of the AMPA receptor. It has a molecular weight of 363.39 g/mol and formula C20H20FNO4. The compound is used in neuroscience research to study the role of AMPA receptors in neurological and psychiatric disorders. AMPA receptor antagonist-3 is not approved for clinical use.
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| Molecular Formula |
C20H19N5O2S
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|---|---|
| Molecular Weight |
393.462162256241
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| Exact Mass |
393.125
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| CAS # |
923272-18-8
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| PubChem CID |
16059548
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| Appearance |
Typically exists as solid at room temperature
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| LogP |
4.2
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
28
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| Complexity |
607
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| Defined Atom Stereocenter Count |
1
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| SMILES |
C[C@@H]1CC2=CC3=C(C=C2C(=NN1C4=NN=CS4)C5=CC(=C(C=C5)N)C)OCO3
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| InChi Key |
HCOJNYUPUOBYDH-GFCCVEGCSA-N
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| InChi Code |
InChI=1S/C20H19N5O2S/c1-11-5-13(3-4-16(11)21)19-15-8-18-17(26-10-27-18)7-14(15)6-12(2)25(24-19)20-23-22-9-28-20/h3-5,7-9,12H,6,10,21H2,1-2H3/t12-/m1/s1
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| Chemical Name |
2-methyl-4-[(8R)-8-methyl-7-(1,3,4-thiadiazol-2-yl)-8,9-dihydro-[1,3]dioxolo[4,5-h][2,3]benzodiazepin-5-yl]aniline
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5416 mL | 12.7078 mL | 25.4155 mL | |
| 5 mM | 0.5083 mL | 2.5416 mL | 5.0831 mL | |
| 10 mM | 0.2542 mL | 1.2708 mL | 2.5416 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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