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Tocris/CGP 78608 hydrochloride/1493/10/10 mg

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货号: 1493/10

品牌: Tocris

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Description: Potent, selective glycine-site NMDA antagonist

Alternative Names: PAMQX

Chemical Name: [(1S)-1-[[(7-Bromo-1,2,3,4-tetrahydro-2,3-dioxo-5-quinoxalinyl)methyl]amino]ethyl]phosphonic acid hydrochloride

Purity: ≥98% (HPLC)

Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity

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 Tocriset™.

Licensing Information

Sold with the permission of Novartis Pharma AG

Technical Data

M. Wt	414.58
Formula	C₁₁H₁₃BrN₃O₅P.HCl
Storage	Store at RT
Purity	≥98% (HPLC)
CAS Number	1135278-54-4
PubChem ID	24978530
InChI Key	MZQQZBPMRPDKTB-JEDNCBNOSA-N
Smiles	O=C2C(NC1=CC(Br)=CC(CN[C@@H]([P@](O)(O)=O)C)=C1N2)=O.Cl

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
Solubility	2.2eq. NaOH	41.46	100

Preparing Stock Solutions

The following data is based on the product molecular weight 414.58. Batch specific molecular weights may vary from batch to batch due to solvent 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	2.41 mL	12.06 mL	24.12 mL
5 mM	0.48 mL	2.41 mL	4.82 mL
10 mM	0.24 mL	1.21 mL	2.41 mL
50 mM	0.05 mL	0.24 mL	0.48 mL

Product Datasheets

Certificate of Analysis / Product Datasheet

Safety Datasheet

References

References are publications that support the products' biological activity.

Ametamey et al (2000) Synthesis, radiolabelling and biological characterization of (D)-7-iodo-N-(1-phosphonoethyl)l-5-aminomethylquinoxaline-2,3-dione, a glycine-binding site antagonist of NMDA receptors. Bioorg.Med.Chem.Lett. 10 75 PMID: 10636248

Auberson et al (1999) N-phosphonoalkyl-5-aminomethylquinoxaline-2,3-diones: in vivo active AMPA and NMDA(glycine) antagonists. Bioorg.Med.Chem.Lett. 9 249 PMID: 10021939

John et al (1994) Synthesis and characterisation of [¹²⁵I]-N-(N-benzylpiperidin-4-yl)-4-iodobenzamide, a new σ receptor radiopharmaceutical: high affinity binding to MCF-7 breast tumor cells. J.Med.Chem. 37 1737 PMID: 8021913

Whittemore et al (1997) Antagonistm of N-methyl-D-aspartate receptors by σ site ligands: potency, subtype-selectivity and mechanisms of inhibition. J.Pharmacol.Exp.Ther. 282 326 PMID: 9223571

Keywords: CGP 78608 hydrochloride, supplier, Potent, selective, glycine-site, NMDA, antagonists, Glutamate, Receptors, N-Methyl-D-Aspartate, iGlur, Ionotropic, CGP78608, hydrochloride, PAMQX, NMDA, Receptors, NMDA, Receptors, Tocris Bioscience

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