Abcam, ab120168, UBP310, GluK1 and GluK3 selective antagonist

Size: 10mg / 50mg
MW 353.35 Da, Purity >98%. GluK1 (formerly GluR5) and GluK3 (formerly GluR7) receptor selective antagonist (K b =10 nM and IC 50 = 23 nM, respectively). IC 50 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 (K d = 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:SolidSee storage information,
Molecular weight:353.35 Da,
Molecular formula:C14H15N3O6S,
PubChem: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

Properties and Storage Information:
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 Information:
This supplementary information is collated from multiple sources and compiled automatically.
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.
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.