NS 3763

Names

[ Name ]:
NS 3763

[Synonym ]:
NS3763
5-Carboxy-2,4-dibenzamidobenzoic acid

Biological Activity

[Description]:

NS3763 is a selective and noncompetitive GLUK5 receptor antagonist with an IC50 of 1.6 µM. NS3763 does not show significant antagonistic properties on GLUK6, AMPA or NMDA receptors[1].

[Related Catalog]:

Signaling Pathways >> Neuronal Signaling >> iGluR

Research Areas >> Neurological Disease

Signaling Pathways >> Membrane Transporter/Ion Channel >> iGluR

[Target]

IC50: 1.6 µM (GLUK5 receptor)[1]

[In Vitro]

In human embryonic kidney HEK293 cells expressing homomeric GLUK5 or GLUK6 receptors, NS3763 displays selectivity for inhibition of domoate-induced increase in intracellular calcium mediated through the GLUK5 subtype (IC50 = 1.6 µM) of kainate receptors compared with the GLUK6 subtype (IC50 > 30 µM)[1]. NS3763 selectively inhibits l-glutamate- and domoate-evoked currents through GLUK5 receptors in HEK293 cells[1].

[References]

[1]. Jeppe K Christensen, et al. In vitro characterization of 5-carboxyl-2,4-di-benzamidobenzoic acid (NS3763), a noncompetitive antagonist of GLUK5 receptors. J Pharmacol Exp Ther. 2004 Jun;309(3):1003-10.

Chemical & Physical Properties

[ Density]:
1.485g/cm3

[ Boiling Point ]:
490.7ºC at 760 mmHg

[ Molecular Formula ]:
C₂₂H₁₆N₂O₆

[ Molecular Weight ]:
404.37200

[ Flash Point ]:
250.6ºC

[ Exact Mass ]:
404.10100

[ PSA ]:
132.80000

[ LogP ]:
3.73360

[ Index of Refraction ]:
1.735

Safety Information

[ Symbol ]:

GHS07, GHS09

[ Signal Word ]:
Warning

[ Hazard Statements ]:
H315-H319-H335-H410

[ Precautionary Statements ]:
P261-P273-P305 + P351 + P338-P501

[ Personal Protective Equipment ]:
dust mask type N95 (US);Eyeshields;Gloves

[ Hazard Codes ]:
Xi,N

[ Risk Phrases ]:
36/37/38-50/53

[ Safety Phrases ]:
26-36-60-61

[ RIDADR ]:
UN 3077 9/PG 3

Articles

Adenine nucleotide translocator cooperates with core cell death machinery to promote apoptosis in Caenorhabditis elegans.

Mol. Cell. Biol. 29 , 3881-93, (2009)

In Caenorhabditis elegans, the central cell-killing process is essentially controlled by the interplay of four apoptotic factors: EGL-1/BH3-only protein, CED-9/Bcl2, CED-4/Apaf1, and CED-3/caspase. In...

Neurotoxic effects of TDP-43 overexpression in C. elegans.

Hum. Mol. Genet. 19 , 3206-18, (2010)

RNA-binding protein TDP-43 has been associated with multiple neurodegenerative diseases, including amyotrophic lateral sclerosis and frontotemporal lobar dementia. We have engineered pan-neuronal expr...

Shared developmental roles and transcriptional control of autophagy and apoptosis in Caenorhabditis elegans.

J. Cell Biol. 124 , 1510-8, (2011)

Autophagy is a lysosome-mediated self-degradation process of eukaryotic cells that, depending on the cellular milieu, can either promote survival or act as an alternative mechanism of programmed cell ...

Related Compounds

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