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Tocris/CGP 78608 hydrochloride/1493/50/50 mg

价格
¥16500.00
货号:1493/50
浏览量:127
品牌:Tocris
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商品描述
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
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

Tocris Bioscience是一家专卖生命科学研究化学、多肽和抗体的知名品牌,其产品也广销各大药厂、大学、研究机构,累计超过五万名科学研究者所采用。 Tocris bioscience是位于英国布里斯托尔的高品质试剂提供商,共有2000多种产品,主要集中在神经科学和信号传导领域,产品类型包括小分子、多肽、抗体、配体和化合物筛选文库等,主要产品包括GPCR ligands,神经传递素,离子通道调控剂,信号通路抑制剂等,这些产品被广泛选择性地用于阻断或激活生物学通路。Tocris是世界上神经科学研究领域无可争议的领导者。 Tocris Bioscience is the trading name of Tocris Cookson Ltd., which is headquartered in Bristol, UK. There are approximately 50 employees in the company. In May 2011 Tocris Bioscience was wholly acquired by R&D Systems, headquartered in Minneapolis, MN, USA.Tocris Neuramin was founded in 1982 by Professor Jeff Watkins of the Pharmacology Department at the University of Bristol, UK. Watkins' research interests focused on glutamate receptors and their involvement in the synaptic transmission processes of the mammalian central nervous system. Tocris Neuramin was founded to make standard research tools and novel probes in this field easily available to researchers, at least partly in response to the number of requests for samples Watkins was receiving at the time. Cookson Chemicals was formed in 1985 by Richard Cookson, Professor of Organic Chemistry at the University of Southampton, UK. Cookson Chemicals provided custom synthesis services as well as a range of neurochemicals to the pharmaceutical and allied industries.Tocris Cookson Ltd was incorporated in the UK in July 1994 as the result of a merger between Tocris Neuramin Ltd of Bristol, UK and Cookson Chemicals Ltd of Southampton, UK. In 2002 Tocris Cookson was awarded The Queen's Awards for Enterprise in the International Trade category and later in 2006 received nominations in five categories of the prestigious Life Science Industry Awards.In October 2005 Tocris announced the opening of new laboratories at the IO Centre, Bristol, UK. At this time, to reflect the increasingly biological nature of the products and customer base the trading name was changed to Tocris Bioscience. In January 2007 Tocris Bioscience announced the successful completion of a $40 million management buy-out (MBO) deal, providing Tocris with the ability and freedom to further develop its existing business areas and to offer additional products and services to its international client base.In May 2011 Tocris Bioscience announced that it was combining with R&D Systems. R&D Systems' products include a wide selection of biotechnology-based tools for cell biology research including proteins, antibodies, assays and kits. To learn more about the company and their products visit the R&D Systems website.In January 2014 Techne Corporation (NASDAQ: TECH) announced that it will operate under a new trade name, Bio-Techne. Over time the new name will be used to unite the company's resources and portfolio to deliver its best-in-class brands and service solutions under a new unified website. The company's major brand names, including Tocris Bioscience, will be maintained.In January 2016 Tocris Bioscience relocated to a brand new facility at the Avonbridge Trading Estate, Bristol, UK. The facility was named the Watkins Building, after Jeff Watkins, who founded Tocris Neuramin in 1982. At this time the Tocris catalog also surpassed 4000 products. 产品列表: Tocris 1000/10 ZD 7288 (10 MG) 10 MG Tocris 1000/50 ZD 7288 (50 MG) 50 MG Tocris 1001/10 Chlorisondamine diiodide (10 MG) 10 MG Tocris 1001/50 Chlorisondamine diiodide (50 MG) 50 MG Tocris 1002/10 L-745,870 trihydrochloride (10 MG) 10 MG Tocris 1002/50 L-745,870 trihydrochloride (50 MG) 50 MG Tocris 1003/10 L-741,626 (10 MG) 10 MG Tocris 1003/50 L-741,626 (50 MG) 50 MG Tocris 1004/10 L-741,742 hydrochloride (10 MG) 10 MG Tocris 1004/50 L-741,742 hydrochloride (50 MG) 50 MG Tocris 1006/10 BMY 7378 dihydrochloride (10 MG) 10 MG Tocris 1006/50 BMY 7378 dihydrochloride (50 MG) 50 MG Tocris 1007/10 N-Desmethylclozapine (10 MG) 10 MG Tocris 1007/50 N-Desmethylclozapine (50 MG) 50 MG Tocris 1009/10 E4CPG (10 MG) 10 MG Tocris 1009/50 E4CPG (50 MG) 50 MG Tocris 1014/100 QX 314 bromide (100 MG) 100 MG Tocris 1015/10 RS 16566 dihydrochloride (10 MG) 10 MG Tocris 1015/50 RS 16566 dihydrochloride (50 MG) 50 MG