Determine the necessary mass, volume, or concentration for preparing a solution.
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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SKU | Size | Availability | Price | Qty |
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G275579-10mg | 10mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $118.90 | |
G275579-50mg | 50mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $494.90 |
Selective non-competitive AMPA antagonist
Synonyms | 4-{13-methyl-4,6-dioxa-11,12-diazatricyclo[7.5.0.0^{3,7}]tetradeca-1(9),2,7,10,12-pentaen-10-yl}aniline | CHEBI:79560 | GYKI52466 | Gyki-52466 | GTPL4210 | 1-(p-Aminophenyl)-4-methyl-7,8-methylenedioxy-5H-2,3-benzodiazepine hydrochloride | NCGC00015463-03 |
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Specifications & Purity | Moligand™, ≥99% |
Biochemical and Physiological Mechanisms | Selective non-competitive AMPA receptor antagonist (IC 50 values are 10-20, approx. 450 and >50 μM for AMPA- , kainate- and NMDA-induced responses, respectively). |
Storage Temp | Room temperature,Desiccated |
Shipped In | Normal |
Grade | Moligand™ |
Action Type | ANTAGONIST |
Mechanism of action | Antagonist of GluA1;Antagonist of GluA2;Antagonist of GluA3;Antagonist of GluA4 |
Note | Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour. Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details. |
Product Description | Store at Room Temperature. Store under desiccating conditions. The product can be stored for up to 12 months. |
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Mechanism of Action | Action Type | target ID | Target Name | Target Type | Target Organism | Binding Site Name | References |
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IUPAC Name | 4-(8-methyl-9H-[1,3]dioxolo[4,5-h][2,3]benzodiazepin-5-yl)aniline |
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INCHI | InChI=1S/C17H15N3O2/c1-10-6-12-7-15-16(22-9-21-15)8-14(12)17(20-19-10)11-2-4-13(18)5-3-11/h2-5,7-8H,6,9,18H2,1H3 |
InChi Key | LFBZZHVSGAHQPP-UHFFFAOYSA-N |
Canonical SMILES | CC1=NN=C(C2=CC3=C(C=C2C1)OCO3)C4=CC=C(C=C4)N |
Isomeric SMILES | CC1=NN=C(C2=CC3=C(C=C2C1)OCO3)C4=CC=C(C=C4)N |
PubChem CID | 3538 |
Molecular Weight | 329.79 |
PubChem CID | 3538 |
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CAS Registry No. | 102771-26-6 |
ChEMBL Ligand | CHEMBL275006 |
Wikipedia | GYKI-52,466 |
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Solubility | Soluble in 1eq. HCl to 10mM and in DMSO to 25 mM (with heating) |
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Pictogram(s) | GHS07 |
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Signal | Warning |
Hazard Statements | H315:Causes skin irritation H319:Causes serious eye irritation H335:May cause respiratory irritation |
Precautionary Statements | P261:Avoid breathing dust/fume/gas/mist/vapors/spray. P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses if present and easy to do - continue rinsing. P280:Wear protective gloves/protective clothing/eye protection/face protection. P302+P352:IF ON SKIN: wash with plenty of water. P321:Specific treatment (see ... on this label). P405:Store locked up. P501:Dispose of contents/container to ... P264:Wash hands [and …] thoroughly after handling. P271:Use only outdoors or in a well-ventilated area. P304+P340:IF INHALED: Remove person to fresh air and keep comfortable for breathing. P403+P233:Store in a well-ventilated place. Keep container tightly closed. P362+P364:Take off contaminated clothing and wash it before reuse. P264+P265:Wash hands [and …] thoroughly after handling. Do not touch eyes. P337+P317:If eye irritation persists: Get medical help. P332+P317:If skin irritation occurs: Get medical help. P319:Get medical help if you feel unwell. |
1. Sasaki T et al.. (2012) Application of an optogenetic byway for perturbing neuronal activity via glial photostimulation.. Proc Natl Acad Sci U S A, 109 (50): (20720-5). [PMID:23185019] |
2. Srivastava R et al.. (2012) Cocaine-taking and cocaine-seeking behaviors in rats remain stable after systemic administration of GYKI 52466: a non-competitive AMPA receptor antagonist.. Neurosci Lett, 508 (2): (106-9). [PMID:22206835] |
3. Hartung H et al.. (2011) Nitric oxide donors enhance the frequency dependence of dopamine release in nucleus accumbens.. Neuropsychopharmacology, 36 (9): (1811-22). [PMID:21508928] |
4. Threlfell S et al.. (2012) Striatal dopamine release is triggered by synchronized activity in cholinergic interneurons.. Neuron, 75 (58-64). [PMID:22794260] |
5. Platt NJ et al.. (2012) Striatal dopamine transmission is subtly modified in human A53Ta-synuclein overexpressing mice.. PLoS One, 7 (5): (e36397). [PMID:22570709] |
6. Threlfell S et al.. (2010) Striatal muscarinic receptors promote activity dependence of dopamine transmission via distinct receptor subtypes on cholinergic interneurons in ventral versus dorsal striatum.. J Neurosci, 30 (9): (3398-408). [PMID:20203199] |