CGP 78608 hydrochlorideCAS# 1135278-54-4 |
Quality Control & MSDS
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| Cas No. | 1135278-54-4 | SDF | Download SDF |
| PubChem ID | 24978530 | Appearance | Powder |
| Formula | C11H14BrClN3O5P | M.Wt | 414.58 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Synonyms | PAMQX | ||
| Solubility | Soluble to 100 mM in 2.2eq. NaOH | ||
| Chemical Name | [(1S)-1-[(7-bromo-2,3-dioxo-1,4-dihydroquinoxalin-5-yl)methylamino]ethyl]phosphonic acid;hydrochloride | ||
| SMILES | CC(NCC1=CC(=CC2=C1NC(=O)C(=O)N2)Br)P(=O)(O)O.Cl | ||
| Standard InChIKey | MZQQZBPMRPDKTB-JEDNCBNOSA-N | ||
| Standard InChI | InChI=1S/C11H13BrN3O5P.ClH/c1-5(21(18,19)20)13-4-6-2-7(12)3-8-9(6)15-11(17)10(16)14-8;/h2-3,5,13H,4H2,1H3,(H,14,16)(H,15,17)(H2,18,19,20);1H/t5-;/m0./s1 | ||
| 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 | Potent and selective NMDA antagonist that acts through the glycine site (IC50 = 5 nM). Displays > 500-fold selectivity over kainate and AMPA receptors (IC50 values are 2.7 and 3 μM respectively). Anticonvulsant in vivo following systemic administration. Also available as part of the NMDA Receptor - Glycine Site. |
CGP 78608 hydrochloride Dilution Calculator
CGP 78608 hydrochloride Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.4121 mL | 12.0604 mL | 24.1208 mL | 48.2416 mL | 60.302 mL |
| 5 mM | 0.4824 mL | 2.4121 mL | 4.8242 mL | 9.6483 mL | 12.0604 mL |
| 10 mM | 0.2412 mL | 1.206 mL | 2.4121 mL | 4.8242 mL | 6.0302 mL |
| 50 mM | 0.0482 mL | 0.2412 mL | 0.4824 mL | 0.9648 mL | 1.206 mL |
| 100 mM | 0.0241 mL | 0.1206 mL | 0.2412 mL | 0.4824 mL | 0.603 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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Synthesis, radiolabelling and biological characterization of (D)-7-iodo-N-(1-phosphonoethyl)-5-aminomethylquinoxaline-2,3-dione, a glycine-binding site antagonist of NMDA receptors.[Pubmed:10636248]
Bioorg Med Chem Lett. 2000 Jan 3;10(1):75-8.
(D)-7-Iodo-N-(1-phosphonoethyl)-5-aminomethylquinoxaline-2,3 -dione (I-PAMQX), is a potent, in vivo active antagonist acting at the glycine binding site of the NMDA receptor complex. Radioiodinated [131I]I-PAMQX was prepared with good yields and high specific activity from its 7-bromo analogue. Biodistribution studies of [131I]I-PAMQX in mice showed a relatively slow clearance from the blood. The uptake of radioactivity was highest in the kidneys, moderate in the heart, lung, liver and bones, and low in the brain.
N-phosphonoalkyl-5-aminomethylquinoxaline-2,3-diones: in vivo active AMPA and NMDA(glycine) antagonists.[Pubmed:10021939]
Bioorg Med Chem Lett. 1999 Jan 18;9(2):249-54.
N-Substituted 5-aminomethylquinoxalinediones containing carboxy or phosphonic acids yield potent and selective AMPA and/or NMDA (glycine-binding site) antagonists. Phosphonic acid derivatives are particularly water-soluble and display potent anticonvulsant effects in the electroshock-induced convulsion assay in mice.
Antagonism of N-methyl-D-aspartate receptors by sigma site ligands: potency, subtype-selectivity and mechanisms of inhibition.[Pubmed:9223571]
J Pharmacol Exp Ther. 1997 Jul;282(1):326-38.
Recent studies propose that sigma site ligands antagonize N-methyl-D-aspartate (NMDA) receptors by either direct, or indirect mechanisms of inhibition. To investigate this question further we used electrical recordings to assay actions of seventeen structurally diverse sigma site ligands on three diheteromeric subunit combinations of cloned rat NMDA receptors expressed in Xenopus oocytes: NR1a coexpressed with either NR2A, 2B or 2C. The sigma site ligands had a wide range of potency for antagonizing NMDA receptor currents. Steady-state IC50 values ranged between approximately 0.1 to >100 microM. In all cases inhibition was non-competitive with respect to glycine and glutamate. Five structurally related sigma ligands [eliprodil, haloperidol, ifenprodil, 4-phenyl-1-(4-phenylbutyl)-piperidine and trifluperidol] were strongly selective for NR1a/2B receptors. The other drugs were weakly selective or nonselective inhibitors. There was no correlation between sigma site affinity and potency of NMDA receptor antagonism for any subunit combination. Inhibition of NR1a/2B receptors by the selective antagonists was independent of voltage whereas inhibition by the weakly selective antagonists was voltage dependent. Potency of 10 sigma ligands was cross-checked on NMDA currents in cultured rat cortical neurons. There was close correspondence between the two assay systems. Our results argue that antagonism of NMDA receptor currents by the sigma ligands tested is due to direct effects on the receptor channel complex as opposed to indirect effects mediated by sigma receptors. Inhibition occurs via sites in the NMDA receptor channel pore, or via allosteric modulatory sites associated with the NR2B subunit.
