MW 336.28 Da, Purity >99%. Potent, selective and competitive AMPA/kainate receptor antagonist. Neuroprotective and anticonvulsant in vivo. Water-soluble form available - please see NBQX disodium salt (ab120046).
118876-58-7
> 99%
Solid
336.28 Da
C12H8N4O6S
3272524
Synthetic
10q23del, 5 AMP activated protein kinase subunit gamma 3, 5''-AMP-activated protein kinase subunit gamma-3, AAKG3_HUMAN, ACTR-I, ACVR1A, ACVR1_HUMAN, ACVRLK 3, ACVRLK2, ALK 6, ALK-2, ALK-3, AMPA 1, AMPA 2, AMPA 3, AMPA 4, AMPA-selective glutamate receptor 1, AMPA-selective glutamate receptor 2, AMPA-selective glutamate receptor 3, AMPA-selective glutamate receptor 4, AMPK gamma 3 chain, AMPK gamma3, AMPK subunit gamma-3, AMPKG3, Activin A receptor type I, Activin A receptor type II like kinase 2, Activin A receptor type II like kinase 3, Activin receptor like kinase 6, Activin receptor type I, Activin receptor type-1, Activin receptor-like kinase 2, Activin receptor-like kinase 3, Acvrlk6, BMP type-1A receptor, BMP type-1B receptor, BMPR IB, BMR1A_HUMAN, BMR1B_HUMAN, BR 1a, BR 1b, Bmpr, Bone morphogenetic protein receptor type IA, Bone morphogenetic protein receptor type IA precursor, Bone morphogenetic protein receptor type IB, Bone morphogenetic protein receptor type-1A, Bone morphogenetic protein receptor type-1B, CD 292, CD292 antigen, CDw 293, CDw293 antigen, CFK 43a, EC 2.7.11.30, EEA3, Excitatory amino acid receptor 1, Excitatory amino acid receptor 2, Excitatory amino acid receptor 3, Excitatory amino acid receptor 4, Excitatory amino acid receptor 5, FOP, GLR 6, GLR 7, GLR5, GLUH1, GLUK3, GLUK6, GLUR4C, GRIA1_HUMAN, GRIA2_HUMAN, GRIA3_HUMAN, GRIA4_HUMAN, GRIK, GRIK1_HUMAN, GRIK2 protein, GRIK2_HUMAN, GRIK3_HUMAN, GRIK4_HUMAN, GRIK5_HUMAN, GluA 4, GluA1, GluA2, GluA3, GluK2, GluK4, GluK5, GluR 7a, GluR-1, GluR-2, GluR-3, GluR-4, GluR-5, GluR-6, GluR-7, GluR-A, GluR-B, GluR-C, GluR-D, GluR-K1, GluR-K2, GluR-K3, GluRgamma2, Glutamate ionotropic receptor AMPA type subunit 3, Glutamate receptor, Glutamate receptor 1, Glutamate receptor 2, Glutamate receptor 3, Glutamate receptor 4, Glutamate receptor 5, Glutamate receptor 6, Glutamate receptor 7, Glutamate receptor C, Glutamate receptor KA 1precursor, Glutamate receptor KA-1, Glutamate receptor KA-2, Glutamate receptor ionotrophic AMPA 3, Glutamate receptor ionotrophic AMPA 4, Glutamate receptor ionotropic, Glutamate receptor ionotropic AMPA 1, Glutamate receptor ionotropic AMPA 2, Glutamate receptor ionotropic kainate 1, Glutamate receptor ionotropic kainate 2, Glutamate receptor ionotropic kainate 3, Glutamate receptor ionotropic kainate 4, Glutamate receptor ionotropic kainate 4 precursor, Glutamate receptor subunit 3, Glutamate receptor, ionotropic kainate 5 [Precursor], Glutamate receptor, ionotropic, AMPA 3, Glutamate receptor, ionotropic, kainate 5, Glutamate receptor, ionotropic, kainate 5 (gamma 2), HBGR1, HBGR2, Human glutamate receptor GLUR5, Hydroxyalkyl protein kinase, Ionotrophic Glutamate Receptor, Ionotropic Glutamate receptor 4, KA2, MGC118086, MGC133252, MRT6, MRX94, OTTHUMP00000045951, OTTHUMP00000096569, OTTHUMP00000160643, OTTHUMP00000165781, OTTHUMP00000224241, OTTHUMP00000224242, OTTHUMP00000224243, OTTHUMP00000231881, PRKAG3, Protein kinase AMP activated gamma 3 non catalytic subunit, SKR 5, SKR1, Serine threonine protein kinase receptor R5, Serine threonine protein kinase receptor R5 precursor, Serine/threonine receptor kinase, Serine/threonine-protein kinase receptor R1, Serine/threonine-protein kinase receptor R5, TGF-B superfamily receptor type I, TSR-I, alk6tr, bA487F5.1, dJ1171F9.1, glutamate receptor form A, glutamate receptor form B, glutamate receptor form C, glutamate receptor form D, glutamate receptor form E, iGlu5, ionotropic kainate 1, ionotropic kainate 2, ionotropic kainate 3, ionotropic kainate 4, ionotropic kainate 5, zALK 6, zBMPR IA
MW 336.28 Da, Purity >99%. Potent, selective and competitive AMPA/kainate receptor antagonist. Neuroprotective and anticonvulsant in vivo. Water-soluble form available - please see NBQX disodium salt (ab120046).
118876-58-7
> 99%
Solid
336.28 Da
C12H8N4O6S
3272524
Synthetic
Soluble in DMSO to 100 mM.
2,3-Dioxo-6-nitro-7-sulfamoylbenzo(f)quinoxaline
Potent, selective and competitive AMPA/kainate receptor antagonist. Neuroprotective and anticonvulsant in vivo. Water-soluble form available - please see NBQX disodium salt (ab120046).
C1=CC2=C3C(=CC(=C2C(=C1)S(=O)(=O)N)[N+](=O)[O-])NC(=O)C(=O)N3
InChI=1S/C12H8N4O6S/c13-23(21,22)8-3-1-2-5-9(8)7(16(19)20)4-6-10(5)15-12(18)11(17)14-6/h1-4H,(H,14,17)(H,15,18)(H2,13,21,22)
UQNAFPHGVPVTAL-UHFFFAOYSA-N
6-nitro-2,3-dioxo-1,4-dihydrobenzo[f]quinoxaline-7-sulfonamide
Ambient - Can Ship with Ice
+4°C
+4°C
Store under desiccating conditions, The product can be stored for up to 12 months
This supplementary information is collated from multiple sources and compiled automatically.
Glutamate Receptor 1 (AMPA subtype) and its related proteins such as BMPR1A BMPR1B and others like GRIK2/GluK2 and GluA3 function as ionotropic glutamate receptors that mediate excitatory synaptic transmission in the central nervous system. The mass of individual components like GluA3 is approximately 100-110 kDa. These receptors including kainate subtypes are widely expressed in the brain specifically in areas involved in learning and memory such as the hippocampus and the cerebral cortex. AMPA receptors work by allowing the flow of ions particularly sodium and calcium into the cells when glutamate binds to them resulting in neuron depolarization essential for synaptic plasticity and neurotransmission.
These receptors play an important role in synaptic communication and plasticity influencing processes like learning and memory formation. The GluA3 and GluK2 subunits are integral parts of the receptor complexes that also include other subunits such as GluA4 and GluK5. These receptors dynamically regulate the synaptic strength by their assembly into tetrameric structures determining excitatory synaptic responses. The diversity in subunit composition allows for precise modulation and response to synaptic activity.
These receptors participate in key signaling cascades such as the glutamatergic and calcium signaling pathways. They directly interact with other proteins including scaffolding proteins like PSD-95 that link them to downstream effectors in these pathways. In the calcium signaling pathway the opening of these receptors leads to calcium influx which is significant for activating downstream signaling molecules including calmodulin-dependent protein kinases which modulate synaptic strength and plasticity.
The dysfunction of these receptors has a strong connection to neurological diseases like epilepsy and neurodegenerative disorders such as Alzheimer's disease. Alterations in receptor function or subunit expression particularly those involving GluA3 and GluK2 have been observed in patients with these conditions. These proteins serve as potential targets for drug development and antagonists such as NBQX are being explored for therapeutic intervention. AMPA receptor dysregulation impacts synaptic stability and plasticity contributing to the disease pathophysiology.
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2D chemical structure image of ab120045, NBQX, AMPA / kainate antagonist
A - Photomicrograph of a DCN fusiform cell filled with lucifer yellow (top) and whole cell voltage clamp recording of this fusiform cell while stimulating the LVN (bottom).
B - Photomicrograph of a DCN granule cell filled with lucifer yellow (top) and whole cell voltage clamp recording of this granule cell while stimulating the LVN (bottom)
Both cells were held at −68 mV and the LVN was stimulated at 0.3 Hz. Glutamatergic EPSCs are represented in black and are blocked by 50 μm D-AP5 and 10 μm NBQX (ab120045, traces in red). Each trace represents an average of 10–20 single traces. The arrowhead represents the artifact of stimulus that has been removed for clarity. Scale bar: (A) 50 μm, (B) 20 μm
Credit: Barker M et al. PLoS One. 2012; 7(5): e35955. 10.1371/journal.pone.0035955
Anti-MEK1 (phospho S298) antibody [EPR3338] ab96379 staining MEK1 (phospho S298) in SK-N-SH cells treated with NBQX (ab120045), by ICC/IF. Decrease in MEK1 (phospho S298) expression correlates with increased concentration of NBQX, as described in literature.
The cells were incubated at 37°C for 1h in media containing different concentrations of ab120045 (NBQX) in DMSO, fixed with 4% formaldehyde for 10 minutes at room temperature and blocked with PBS containing 10% goat serum, 0.3 M glycine, 1% BSA and 0.1% tween for 2h at room temperature. Staining of the treated cells with Anti-MEK1 (phospho S298) antibody [EPR3338] ab96379 (1/100 dilution) was performed overnight at 4°C in PBS containing 1% BSA and 0.1% tween. A DyLight 488 goat anti-rabbit polyclonal antibody (Goat Anti-Rabbit IgG H&L (DyLight® 488) preadsorbed ab96899) at 1/250 dilution was used as the secondary antibody.
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