| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| Other Sizes |
| Targets |
AMPA receptor antagonist-2 targets the AMPA (α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid) receptor, a subtype of ionotropic glutamate receptor that mediates fast excitatory neurotransmission in the central nervous system. AMPA receptors are involved in synaptic plasticity, learning, and memory. The compound is a non-competitive antagonist of AMPA and kainate receptors. By blocking AMPA receptors, it reduces excitatory neurotransmission and has potential applications in CNS disorders such as epilepsy, neurodegenerative diseases, and pain.
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| ln Vitro |
In vitro, AMPA receptor antagonist-2 is an antagonist of AMPA receptors, blocking glutamate-induced excitatory neurotransmission. It is a non-competitive antagonist of AMPA and kainate receptors. However, specific IC50 values and detailed in vitro activity data are not extensively reported in the available literature. The compound has potential applications in CNS disease research.
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| ln Vivo |
In vivo, AMPA receptor antagonist-2 is expected to show efficacy in animal models of CNS diseases by reducing excitatory neurotransmission. However, specific in vivo efficacy data for this compound are not extensively reported in the available literature.
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| Enzyme Assay |
In vitro enzyme/receptor binding assays for AMPA receptor antagonist-2 typically involve radioligand binding assays using rat brain membranes or cells expressing AMPA receptors. Membrane preparations are incubated with a radiolabeled AMPA receptor ligand (e.g., 3H-AMPA) and various concentrations of the compound (typically 0.001-100 μM) at 4°C for 1-2 hours. Bound radioactivity is measured by filtration and scintillation counting. The IC50 or Ki is determined from dose-response curves.
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| Cell Assay |
In vitro cellular assays for AMPA receptor antagonist-2 use primary cortical neurons or cell lines expressing AMPA receptors. Cells are cultured in appropriate media and loaded with a calcium indicator (e.g., Fluo-4). Cells are pre-treated with various concentrations of the compound (typically 0.001-100 μM) and stimulated with glutamate or AMPA. Calcium influx is measured by fluorescence imaging or plate reader. Receptor antagonism is assessed by inhibition of agonist-induced calcium responses.
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| Animal Protocol |
In vivo animal studies with AMPA receptor antagonist-2 would typically use rodent models of epilepsy, stroke, or neurodegenerative disease. The compound would be administered orally or intraperitoneally at doses of 1-30 mg/kg. Seizure activity, neuroprotection, or behavioral outcomes would be assessed. However, specific in vivo data for this compound are not extensively reported.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of AMPA receptor antagonist-2: The compound has a molecular weight of 339.35. Specific PK parameters such as oral bioavailability, half-life, and tissue distribution are not extensively reported. As a small molecule, it is expected to have moderate CNS penetration.
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| Toxicity/Toxicokinetics |
The toxicity profile of AMPA receptor antagonist-2 is not extensively reported in the available literature. As an AMPA receptor antagonist, potential side effects may include sedation, motor impairment, and cognitive effects. The compound is for research use only and not for human therapeutic use.
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| References | |
| Additional Infomation |
AMPA receptor antagonist-2 (CAS 732277-05-3, example 23) is a non-competitive antagonist of AMPA and kainate receptors with potential applications in CNS disease research. It has a molecular formula of C18H17N3O4 and a molecular weight of 339.35. The compound is available for research purposes only and is not approved for clinical use.
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| Molecular Formula |
C18H17N3O4
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|---|---|
| Molecular Weight |
339.345284223557
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| Exact Mass |
339.121
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| CAS # |
732277-05-3
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| PubChem CID |
68940818
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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 |
6
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
25
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| Complexity |
549
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| Defined Atom Stereocenter Count |
1
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| SMILES |
C[C@@H]1CC2=CC3=C(C=C2C(=NN1)C4=CC(=C(C=C4)[N+](=O)[O-])C)OCO3
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| InChi Key |
SXFGVEYSGPJCQX-LLVKDONJSA-N
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| InChi Code |
InChI=1S/C18H17N3O4/c1-10-5-12(3-4-15(10)21(22)23)18-14-8-17-16(24-9-25-17)7-13(14)6-11(2)19-20-18/h3-5,7-8,11,19H,6,9H2,1-2H3/t11-/m1/s1
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| Chemical Name |
(8R)-8-methyl-5-(3-methyl-4-nitrophenyl)-8,9-dihydro-7H-[1,3]dioxolo[4,5-h][2,3]benzodiazepine
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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 | 2.9468 mL | 14.7341 mL | 29.4681 mL | |
| 5 mM | 0.5894 mL | 2.9468 mL | 5.8936 mL | |
| 10 mM | 0.2947 mL | 1.4734 mL | 2.9468 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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