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Merck

454586

NMDAR2C/2D Inhibitor, DQP-1105

The NMDAR2C/2D Inhibitor, DQP-1105 controls the biological activity of NMDAR2C/2D. This small molecule/inhibitor is primarily used for Neuroscience applications.

Synonym(s):

NMDAR2C/2D Inhibitor, DQP-1105, NMDA Antagonist IV, DQP-1105

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About This Item

Empirical Formula (Hill Notation):
C29H24BrN3O4
CAS Number:
Molecular Weight:
558.42
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
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Product Name

NMDAR2C/2D Inhibitor, DQP-1105, The NMDAR2C/2D Inhibitor, DQP-1105 controls the biological activity of NMDAR2C/2D. This small molecule/inhibitor is primarily used for Neuroscience applications.

SMILES string

O=C(O)CCC(N1N=C(C2=C(C3=CC=CC=C3)C4=C(NC2=O)C=CC(C)=C4)CC1C5=CC=C(Br)C=C5)=O

assay

≥97% (HPLC)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
protect from light

color

yellow-white

solubility

DMSO: 10 mg/mL, pale yellow

shipped in

ambient

storage temp.

−20°C

Quality Level

Disclaimer

Toxicity: Regulatory Review (Z)

General description

A dihydroquinilone-pyrazoline NMDA antagonist, which is selective for NMDA receptors that are comprised of recombinant subunits GluN1/GluN2C (IC50 = 5.4 µM) and GluN1/GluN2D (2.2 µM) over GluN1/GluN2B (206 µM) and GluN1/ClucN2A (undetectable) in Xenopus oocytes. Similar selectivity is observed in whole-cell HEK patch-clamp assays with IC50 values for GluN2C and GluN2D that are at least 50-fold lower than those for recombinant GluN2A, GluN2B, GluA1, or GluK2-containing receptors. It inhibits NMDA by blocking a conformational change necessary for channel opening and is non-competitive with co-agonists, glutamate and glycine.

Other Notes

Acker, T., et al. 2011. Mol. Pharmacol.80, 782.

Packaging

Packaged under inert gas

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Storage Class

11 - Combustible Solids

wgk

WGK 2

flash_point_f

Not applicable

flash_point_c

Not applicable


Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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Related Content

Glutamate is an excitatory neurotransmitter found in the synaptic vesicles of glutamatergic synapses. The post-synaptic neurons in these synapses contain ionotropic and metabotropic glutamate receptors. Glutamate binds to AMPA (α-amino-3-hydroxy-5- methylisoxazole-4-propionic acid) subtype glutamate receptors, leading to sodium influx into the post-synaptic cell and resulting in neuronal excitability and synaptic transmission. The NMDA (N-methyl-d-aspartate) subtype glutamate receptors, on the other hand, regulate synaptic plasticity, and can influence learning and memory. The metabotropic g-protein coupled mGluRs modulate downstream calcium signaling pathways and indirectly influence the synapse’s excitability. The synaptic architecture includes intracellular scaffolding proteins (PSD-95, GRIP), intercellular cell adhesion molecules (NCAMs, N-Cadherins), and a variety of signaling proteins (CaMKII/PKA, PP1/PP2B). Processes critical for synaptic transmission and plasticity are influenced by these molecules and their interactions. When the function of these molecules is disrupted, it leads to synaptic dysfunction and degeneration, and can contribute to dementia as seen in Alzheimer’s disease.

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