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AB120168

UBP310, GluK1 and GluK3 selective antagonist

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(3 Publications)

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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Chemical Structure - UBP310, GluK1 and GluK3 selective antagonist (AB120168)
  • Chemical Structure

Lab

Chemical Structure - UBP310, GluK1 and GluK3 selective antagonist (AB120168)

2D chemical structure image of ab120168, UBP310, GluK1 and GluK3 selective antagonist

Key facts

CAS number

902464-46-4

Purity

>98%

Form

Solid

form

Molecular weight

353.35 Da

Molecular formula

C<sub>1</sub><sub>4</sub>H<sub>1</sub><sub>5</sub>N<sub>3</sub>O<sub>6</sub>S

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

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Secondary Antibodies

AB150113

Goat Anti-Mouse IgG H&L (Alexa Fluor® 488)

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AB120045

NBQX, AMPA / kainate antagonist

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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
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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.
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Product protocols

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Publications (3)

Recent publications for all applications. Explore the full list and refine your search

The Journal of neuroscience : the official journal of the Society for Neuroscience 34:7611-21 PubMed24872565

2014

Kainate receptors mediate synaptic input to transient and sustained OFF visual pathways in primate retina.

Applications

Unspecified application

Species

Unspecified reactive species

Theresa Puthussery,Kumiko A Percival,Sowmya Venkataramani,Jacqueline Gayet-Primo,Ulrike Grünert,W Rowland Taylor

The Journal of physiology 592:1457-77 PubMed24396054

2014

Kainate receptor subunit diversity underlying response diversity in retinal off bipolar cells.

Applications

Unspecified application

Species

Unspecified reactive species

Sarah H Lindstrom,David G Ryan,Jun Shi,Steven H DeVries

Molecular pharmacology 78:1036-45 PubMed20837679

2010

Mapping the ligand binding sites of kainate receptors: molecular determinants of subunit-selective binding of the antagonist [3H]UBP310.

Applications

Unspecified application

Species

Unspecified reactive species

Palmi T Atlason,Caroline L Scholefield,Richard J Eaves,M Belen Mayo-Martin,David E Jane,Elek Molnár
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