Synonym
NS3763; NS 3763; NS-3763.
IUPAC/Chemical Name
4,6-dibenzamidobenzene-1,3-dicarboxylic acid
InChi Key
UUDYZUDTQPLDDP-UHFFFAOYSA-N
InChi Code
InChI=1S/C22H16N2O6/c25-19(13-7-3-1-4-8-13)23-17-12-18(16(22(29)30)11-15(17)21(27)28)24-20(26)14-9-5-2-6-10-14/h1-12H,(H,23,25)(H,24,26)(H,27,28)(H,29,30)
SMILES Code
O=C(C1=C(NC(C2=CC=CC=C2)=O)C=C(NC(C3=CC=CC=C3)=O)C(C(O)=O)=C1)O
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
Biological target:
NS3763 is a selective and noncompetitive GLUK5 receptor antagonist with an IC50 of 1.6 µM.
In vitro activity:
In functional assays in human embryonic kidney (HEK)293 cells expressing homomeric GLU(K5) or GLU(K6) receptors, NS3763 is shown to display selectivity for inhibition of domoate-induced increase in intracellular calcium mediated through the GLU(K5) subtype (IC(50) = 1.6 microM) of kainate receptors compared with the GLU(K6) subtype (IC(50) > 30 microM). NS3763 inhibits the GLU(K5)-mediated response in a noncompetitive manner and does not inhibit [(3)H]alpha-amino-3-hydroxy-5-tertbutylisoxazole-4-propionic acid binding to GLU(K5) receptors.
Reference: J Pharmacol Exp Ther. 2004 Jun;309(3):1003-10. https://pubmed.ncbi.nlm.nih.gov/14985418/
Preparing Stock Solutions
The following data is based on the
product
molecular weight
404.38
Batch specific molecular weights may vary
from batch to batch
due to the degree of hydration, which will
affect the solvent
volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass |
1 mg |
5 mg |
10 mg |
| 1 mM |
1.15 mL |
5.76 mL |
11.51 mL |
| 5 mM |
0.23 mL |
1.15 mL |
2.3 mL |
| 10 mM |
0.12 mL |
0.58 mL |
1.15 mL |
| 50 mM |
0.02 mL |
0.12 mL |
0.23 mL |
Formulation protocol:
Christensen JK, Varming T, Ahring PK, Jørgensen TD, Nielsen EØ. 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. doi: 10.1124/jpet.103.062794. Epub 2004 Feb 25. PMID: 14985418.
In vitro protocol:
Christensen JK, Varming T, Ahring PK, Jørgensen TD, Nielsen EØ. 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. doi: 10.1124/jpet.103.062794. Epub 2004 Feb 25. PMID: 14985418.
1: Lv Q, Liu Y, Han D, Xu J, Zong YY, Wang Y, Zhang GY. Neuroprotection of GluK1 kainate receptor agonist ATPA against ischemic neuronal injury through inhibiting GluK2 kainate receptor-JNK3 pathway via GABA(A) receptors. Brain Res. 2012 May 25;1456:1-13. doi: 10.1016/j.brainres.2012.03.050. Epub 2012 Mar 28. PubMed PMID: 22516108.
2: Qi SH, Liu Y, Wang WW, Wang M, Zhang GY. Neuroprotection of ethanol against cerebral ischemia/reperfusion induced brain injury through GABA receptor activation. Brain Res. 2009 Jun 18;1276:151-8. doi: 10.1016/j.brainres.2009.04.040. Epub 2009 May 3. PubMed PMID: 19406109.
3: Xu J, Liu Y, Zhang GY. Neuroprotection of GluR5-containing kainate receptor activation against ischemic brain injury through decreasing tyrosine phosphorylation of N-methyl-D-aspartate receptors mediated by Src kinase. J Biol Chem. 2008 Oct 24;283(43):29355-66. doi: 10.1074/jbc.M800393200. Epub 2008 Aug 4. PubMed PMID: 18678878; PubMed Central PMCID: PMC2662022.
4: Platel JC, Heintz T, Young S, Gordon V, Bordey A. Tonic activation of GLUK5 kainate receptors decreases neuroblast migration in whole-mounts of the subventricular zone. J Physiol. 2008 Aug 15;586(16):3783-93. doi: 10.1113/jphysiol.2008.155879. Epub 2008 Jun 19. PubMed PMID: 18565997; PubMed Central PMCID: PMC2538932.
5: Christensen JK, Paternain AV, Selak S, Ahring PK, Lerma J. A mosaic of functional kainate receptors in hippocampal interneurons. J Neurosci. 2004 Oct 13;24(41):8986-93. PubMed PMID: 15483117.
6: Christensen JK, Varming T, Ahring PK, Jørgensen TD, Nielsen EØ. 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. Epub 2004 Feb 25. PubMed PMID: 14985418.
