MW 353.35 Da, Purity >98%. GluK1 (formerly GluR5) and GluK3 (formerly GluR7) receptor selective antagonist (Kb =10 nM and IC50 = 23 nM, respectively). IC50 values are >100 μM at recombinant human GLUA2 (formerly GluR2), GluK2 (formerly GluR6,) GluK2/GluK5 (formerly GluR6/KA2) and GluK2/GluK3 (formerly GluR6/GluR7). Selective over native AMPA receptors (Kd = 83 μM) and exhibits no activity at NMDA and Group I mGlu receptors at concentrations of up to 10 μM.
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- The Journal of neuroscience : the official journal of the Society for Neuroscience 34:7611-212014Kainate receptors mediate synaptic input to transient and sustained OFF visual pathways in primate retina.Applications:Unspecified applicationReactive species:Unspecified reactive speciesTheresa Puthussery,Kumiko A Percival,Sowmya Venkataramani,Jacqueline Gayet-Primo,Ulrike Grünert,W Rowland TaylorPubMed 24872565
- The Journal of physiology 592:1457-772014Kainate receptor subunit diversity underlying response diversity in retinal off bipolar cells.Applications:Unspecified applicationReactive species:Unspecified reactive speciesSarah H Lindstrom,David G Ryan,Jun Shi,Steven H DeVriesPubMed 24396054
- Molecular pharmacology 78:1036-452010Mapping the ligand binding sites of kainate receptors: molecular determinants of subunit-selective binding of the antagonist [3H]UBP310.Applications:Unspecified applicationReactive species:Unspecified reactive speciesPalmi T Atlason et. al.PubMed 20837679
Key facts
- CAS number
- 902464-46-4
- Purity
- > 98%
- Form
- Solid
- Molecular weight
- 353.35 Da
- Molecular formula
- C14H15N3O6S
- PubChem identifier
- 6420160
- Nature
- Synthetic
Target data
Alternative names
AMPA 1, AMPA-selective glutamate receptor 1, EEA3, Excitatory amino acid receptor 3, Excitatory amino acid receptor 5, GLR 7, GLR5, GLUH1, GRIA1_HUMAN, GRIK1_HUMAN, GRIK3_HUMAN, GluA1, GluR 7a, GluR-1, GluR-5, GluR-6, GluR-7, GluR-A, GluR-K1, Glutamate receptor, Glutamate receptor 1, Glutamate receptor 5, Glutamate receptor 7, Glutamate receptor ionotropic, Glutamate receptor ionotropic AMPA 1, Glutamate receptor ionotropic kainate 1, Glutamate receptor ionotropic kainate 3, HBGR1, Human glutamate receptor GLUR5, MGC133252, OTTHUMP00000096569, OTTHUMP00000160643, OTTHUMP00000165781, OTTHUMP00000224241, OTTHUMP00000224242, OTTHUMP00000224243, ionotropic kainate 1, ionotropic kainate 3
Recommended products
MW 353.35 Da, Purity >98%. GluK1 (formerly GluR5) and GluK3 (formerly GluR7) receptor selective antagonist (Kb =10 nM and IC50 = 23 nM, respectively). IC50 values are >100 μM at recombinant human GLUA2 (formerly GluR2), GluK2 (formerly GluR6,) GluK2/GluK5 (formerly GluR6/KA2) and GluK2/GluK3 (formerly GluR6/GluR7). Selective over native AMPA receptors (Kd = 83 μM) and exhibits no activity at NMDA and Group I mGlu receptors at concentrations of up to 10 μM.
Key facts
- CAS number
- 902464-46-4
- Purity
- > 98%
- Form
- Solid
- Molecular weight
- 353.35 Da
- Molecular formula
- C14H15N3O6S
- PubChem identifier
- 6420160
- Nature
- Synthetic
- Solubility
Soluble in DMSO to 25 mM.
- Biochemical name
- (S)-1-(2-Amino-2-carboxyethyl)-3(2-carboxythiophene-3-YL-methyl)-5-methylpyrimidine-2,4-dione
- Biological description
GluK1 (formerly GluR5) and GluK3 (formerly GluR7) receptor selective antagonist (Kb =10 nM and IC50 = 23 nM, respectively). IC50 values are >100 μM at recombinant human GLUA2 (formerly GluR2), GluK2 (formerly GluR6,) GluK2/GluK5 (formerly GluR6/KA2) and GluK2/GluK3 (formerly GluR6/GluR7). Selective over native AMPA receptors (Kd = 83 μM) and exhibits no activity at NMDA and Group I mGlu receptors at concentrations of up to 10 μM.
- Canonical SMILES
- CC1=CN(C(=O)N(C1=O)CC2=C(SC=C2)C(=O)O)CC(C(=O)O)N
- Isomeric SMILES
- CC1=CN(C(=O)N(C1=O)CC2=C(SC=C2)C(=O)O)C[C@@H](C(=O)O)N
- InChI
- InChI=1S/C14H15N3O6S/c1-7-4-16(6-9(15)12(19)20)14(23)17(11(7)18)5-8-2-3-24-10(8)13(21)22/h2-4,9H,5-6,15H2,1H3,(H,19,20)(H,21,22)/t9-/m0/s1
- InChIKey
- ZTAZUCRXCRXNSU-VIFPVBQESA-N
- IUPAC name
- 3-[[3-[(2S)-2-amino-2-carboxyethyl]-5-methyl-2,6-dioxopyrimidin-1-yl]methyl]thiophene-2-carboxylic acid
Storage
- Shipped at conditions
- Ambient - Can Ship with Ice
- Appropriate short-term storage conditions
- +4°C
- Appropriate long-term storage conditions
- +4°C
- 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 GRIK3 or GluK3 and GluK1 is an ionotropic glutamate receptor that plays a role in fast synaptic transmission in the central nervous system. This receptor exhibits a molecular mass of ~102 kDa and is widely expressed in the brain particularly in regions involved with cognitive functions like the hippocampus and cerebral cortex. The receptor mediates excitatory neurotransmission by allowing the influx of cations through its channel which gets activated upon binding glutamate a neurotransmitter.
- Biological function summary
Glutamate Receptor 1 participates in synaptic plasticity and modulating neural communication affecting processes such as learning and memory. As a part of the excitatory postsynaptic mechanisms it forms complexes with other ionotropic receptors such as NMDA receptors to regulate synaptic strength and postsynaptic currents. Through these interactions it adjusts synaptic efficacy which in turn influences neural circuit function and behavior.
- Pathways
Glutamate Receptor 1 interacts closely with the glutamatergic signaling pathway and the synaptic plasticity pathway. These pathways highlight its role in the communication between neurons and the adaptation of synapses important for memory and learning processes. Related proteins such as NMDA receptors assist in the modulation of synaptic activity providing a framework for cross-talk between various glutamate receptor types which ensures fine-tuning of synaptic transmission across neuronal networks.
- Associated diseases and disorders
Aberrations in the function of Glutamate Receptor 1 have connections to neurological conditions such as epilepsy and schizophrenia. Dysregulation of this receptor can lead to altered excitatory signals contributing to the pathophysiology of these disorders. Additionally the receptor has ties with other proteins like the aforementioned NMDA receptors in epilepsy where they collectively influence synaptic overexcitation. Understanding these interactions helps to shed light on therapeutic targets for improving neuropsychiatric conditions.
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1 product image
Chemical Structure - UBP310, GluK1 and GluK3 selective antagonist (ab120168)
2D chemical structure image of ab120168, UBP310, GluK1 and GluK3 selective antagonist
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