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Merck
CN

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.

别名:

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

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关于此项目

经验公式(希尔记法):
C29H24BrN3O4
化学文摘社编号:
分子量:
558.42
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
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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

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.

Packaging

Packaged under inert gas

Other Notes

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

Legal Information

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

Disclaimer

Toxicity: Regulatory Review (Z)

存储类别

11 - Combustible Solids

wgk

WGK 2

flash_point_f

Not applicable

flash_point_c

Not applicable


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相关内容

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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