NS 3763CAS# 70553-45-6 |
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Quality Control & MSDS
3D structure
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| Cas No. | 70553-45-6 | SDF | Download SDF |
| PubChem ID | 4359312 | Appearance | Powder |
| Formula | C22H16N2O6 | M.Wt | 404.38 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | Soluble to 25 mM in DMSO | ||
| Chemical Name | 4,6-dibenzamidobenzene-1,3-dicarboxylic acid | ||
| SMILES | C1=CC=C(C=C1)C(=O)NC2=CC(=C(C=C2C(=O)O)C(=O)O)NC(=O)C3=CC=CC=C3 | ||
| Standard InChIKey | UUDYZUDTQPLDDP-UHFFFAOYSA-N | ||
| Standard InChI | 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) | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | Selective non-competitive kainate receptor antagonist; displays selectivity for GLUK5 subunit-containing receptors (IC50 values are 1.6 and > 30 μM for homomeric GLUK5 and GLUK6 receptors respectively). Has minimal activity at AMPA and NMDA receptors (IC50> 30 μM). |
NS 3763 Dilution Calculator
NS 3763 Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.4729 mL | 12.3646 mL | 24.7292 mL | 49.4584 mL | 61.823 mL |
| 5 mM | 0.4946 mL | 2.4729 mL | 4.9458 mL | 9.8917 mL | 12.3646 mL |
| 10 mM | 0.2473 mL | 1.2365 mL | 2.4729 mL | 4.9458 mL | 6.1823 mL |
| 50 mM | 0.0495 mL | 0.2473 mL | 0.4946 mL | 0.9892 mL | 1.2365 mL |
| 100 mM | 0.0247 mL | 0.1236 mL | 0.2473 mL | 0.4946 mL | 0.6182 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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In vitro characterization of 5-carboxyl-2,4-di-benzamidobenzoic acid (NS3763), a noncompetitive antagonist of GLUK5 receptors.[Pubmed:14985418]
J Pharmacol Exp Ther. 2004 Jun;309(3):1003-10.
Accumulating preclinical data suggest that compounds that block the excitatory effect of glutamate on the kainate subtype of glutamate receptors may have utility for the treatment of pain, migraine, and epilepsy. In the present study, the in vitro pharmacological properties of the novel glutamate antagonist 5-carboxyl-2,4-di-benzamido-benzoic acid (NS3763) are described. 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. Furthermore, NS3763 selectively inhibits l-glutamate- and domoate-evoked currents through GLU(K5) receptors in HEK293 cells and does not significantly inhibit alpha-amino-3-hydroxy-5-methylisoxazole-4-propionic acid- or N-methyl-d-aspartate-induced currents in cultured mouse cortical neurons at 30 microM. This is the first report on a selective and noncompetitive GLU(K5) antagonist.
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