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Submit ReviewCGP 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.
Sold with the permission of Novartis Pharma AG
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.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
2.2eq. NaOH | 41.46 | 100 |
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.
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 |
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
If you know of a relevant reference for CGP 78608 hydrochloride, please let us know.
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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Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
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