MW 280.04 Da, Purity >99%. Potent NMDA receptor glycine site antagonist. Achieve your results faster with highly validated, pure and trusted compounds.
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Key facts
- CAS number
- 1184986-70-6
- Purity
- > 99%
- Form
- Solid
- Molecular weight
- 280.04 Da
- Molecular formula
- C10H4Cl2NNaO3
- PubChem identifier
- 44134672
- Nature
- Synthetic
Alternative names
AMPA 1, AMPA-selective glutamate receptor 1, GLUH1, GRIA1_HUMAN, GluA1, GluR-1, GluR-A, GluR-K1, Glutamate receptor 1, Glutamate receptor ionotropic, Glutamate receptor ionotropic AMPA 1, HBGR1, MGC133252, OTTHUMP00000160643, OTTHUMP00000165781, OTTHUMP00000224241, OTTHUMP00000224242, OTTHUMP00000224243
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MW 280.04 Da, Purity >99%. Potent NMDA receptor glycine site antagonist. Achieve your results faster with highly validated, pure and trusted compounds.
Key facts
- CAS number
- 1184986-70-6
- Purity
- > 99%
- Form
- Solid
- Molecular weight
- 280.04 Da
- Molecular formula
- C10H4Cl2NNaO3
- PubChem identifier
- 44134672
- Nature
- Synthetic
- Biochemical name
- 5,7-Dichlorokynurenic acid sodium salt
- Biological description
Potent NMDA receptor glycine site antagonist.
- Canonical SMILES
- C1=C(C=C(C2=C1NC(=CC2=O)C(=O)[O-])Cl)Cl.[Na+]
- InChI
- InChI=1S/C10H5Cl2NO3.Na/c11-4-1-5(12)9-6(2-4)13-7(10(15)16)3-8(9)14;/h1-3H,(H,13,14)(H,15,16);/q;+1/p-1
- InChIKey
- VPRPMJHKWHCUFW-UHFFFAOYSA-M
- IUPAC name
- sodium;5,7-dichloro-4-oxo-1H-quinoline-2-carboxylate
Storage
- Shipped at conditions
- Ambient - Can Ship with Ice
- Appropriate short-term storage conditions
- Ambient
- Appropriate long-term storage conditions
- Ambient
- Storage information
- Store under desiccating conditions, The product can be stored for up to 12 months
Supplementary info
- This supplementary information is collated from multiple sources and compiled automatically.
- Activity summary
Glutamate Receptor 1 (AMPA subtype) also known as GluR1 is a subunit of the AMPA receptor complex which mediates fast synaptic transmission in the central nervous system. It is an ionotropic receptor for glutamate functioning by opening ion channels to allow the flow of Na+ and Ca2+ ions across the cell membrane contributing to excitatory neurotransmission. The GluR1 subunit has a molecular mass of approximately 100 kDa. This receptor is commonly expressed in the brain regions such as the hippocampus and the cerebral cortex playing an important role in synaptic plasticity and memory formation.
- Biological function summary
The GluR1 subunit is an essential component of the AMPA receptor complex which typically forms as a tetramer. This complex modulates synaptic strength and plasticity processes critical for learning and memory. The activity of AMPA receptors including those containing GluR1 is regulated by several auxiliary proteins and is essential for post-synaptic responses. The GluR1 subunit also interacts with other proteins such as TARPs which modulate its trafficking and channel properties.
- Pathways
The GluR1-containing AMPA receptors participate significantly in the glutamatergic signaling pathway which is vital for fast excitatory synaptic transmission in the brain. This pathway also involves the NMDA receptors which work together with AMPA receptors to regulate synaptic plasticity and neuronal communication. Additionally the GluR1 interacts within the long-term potentiation (LTP) pathway contributing to the strengthening of synapses an essential mechanism underlying learning and memory.
- Associated diseases and disorders
Dysfunction in GluR1 and associated AMPA receptors has been implicated in conditions like Alzheimer's disease and epilepsy. Alzheimer's disease exhibits decreased synaptic transmission and plasticity linked to impaired GluR1 function and its interactions with NMDA receptors. In epilepsy abnormal GluR1 activity may contribute to heightened neuronal excitability and seizure propagation. Targeting GluR1 or associated pathways offers potential for therapeutic interventions in these disorders possibly through drugs such as memantine and NBQX which modulate receptor activity.
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2 product images
Chemical Structure - 5,7-Dichlorokynurenic acid sodium salt, NMDA receptor glycine site antagonist (ab120254)
2D chemical structure image of ab120254, 5,7-Dichlorokynurenic acid sodium salt, NMDA receptor glycine site antagonist
Functional Studies - 5,7-Dichlorokynurenic acid sodium salt, NMDA receptor glycine site antagonist (ab120254)
ab12416 staining cGMP in SKNSH cells treated with 5,7-Dichlorokynurenic acid sodium salt (ab120254), by ICC/IF. Decrease in cGMP expression correlates with increased concentration of 5,7-Dichlorokynurenic acid sodium salt, as described in literature.
The cells were incubated at 37°C for 20 minutes in media containing different concentrations of ab120254 (5,7-Dichlorokynurenic acid sodium salt) in DMSO. Some samples where then further incubated with 15 µM NMDA (NMDA, excitotoxic amino acid ab120052) for 5 minutes and all samples were fixed with 100% methanol for 5 minutes at -20°C 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 ab12416 (5 µg/ml) was performed overnight at 4°C in PBS containing 1% BSA and 0.1% tween. A DyLight 488 anti-rabbit polyclonal antibody (Goat Anti-Rabbit IgG H&L (DyLight® 488) preadsorbed ab96899) at 1/250 dilution was used as the secondary antibody. Nuclei were counterstained with D
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