CGP 78608 hydrochloride

Pricing Availability   Qty
说明: Potent and selective NMDA antagonist; acts at glycine site
别名: PAMQX
化学名: [(1S)-1-[[(7-Bromo-1,2,3,4-tetrahydro-2,3-dioxo-5-quinoxalinyl)methyl]amino]ethyl]phosphonic acid hydrochloride
纯度: ≥98% (HPLC)
说明书
引用文献
评论
文献 (5)

生物活性 for CGP 78608 hydrochloride

CGP 78608 hydrochloride is a 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). Also potentiates GluN1/GluN3A-mediated glycine currents (EC50 = 26.3 nM). Anticonvulsant in vivo following systemic administration.

许可信息

Sold with the permission of Novartis Pharma AG

技术数据 for CGP 78608 hydrochloride

分子量 414.58
公式 C11H13BrN3O5P.HCl
储存 Store at RT
纯度 ≥98% (HPLC)
CAS Number 1135278-54-4
PubChem ID 24978530
InChI Key MZQQZBPMRPDKTB-JEDNCBNOSA-N
Smiles C[C@H](P(O)(O)=O)NCC1=C2NC(C(NC2=CC(Br)=C1)=O)=O.Cl

上方提供的技术数据仅供参考。批次相关数据请参见分析证书。

Tocris products are intended for laboratory research use only, unless stated otherwise.

溶解性数据 for CGP 78608 hydrochloride

溶剂 最高浓度 mg/mL 最高浓度 mM
溶解性
2.2eq. NaOH 41.46 100

制备储备液 for CGP 78608 hydrochloride

以下数据基于产品分子量 414.58。 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.

选择批次从而根据批次分子量重新计算:
浓度/溶剂体积/质量 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

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产品说明书 for CGP 78608 hydrochloride

分析证书/产品说明书
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参考文献 for CGP 78608 hydrochloride

参考文献是支持产品生物活性的出版物。

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) Antagonism of N-MthD.-aspartate receptors by σ site ligands: potency, subtype-selectivity and mechanisms of inhibition. J.Pharmacol.Exp.Ther. 282 326 PMID: 9223571

Grand et al (2018) Unmasking GluN1/GluN3A excitatory glycine NMDA receptors. Nat.Commun. 9 4769 PMID: 30425244


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关键词: CGP 78608 hydrochloride, CGP 78608 hydrochloride supplier, Potent, selective, glycine-site, NMDA, antagonists, Glutamate, Receptors, N-Methyl-D-Aspartate, iGlur, Ionotropic, CGP78608, hydrochloride, GluN1, GluN3A, potentiates, potentiators, currents, PAMQX, 1493, Tocris Bioscience

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