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说明： Potent and selective kainate antagonist; active enantiomer of UBP 296 (Cat. No. 2078)
化学名： (S)-1-(2-Amino-2-carboxyethyl)-3-(2-carboxybenzyl)pyrimidine-2,4-dione
纯度： ≥98% (HPLC)
生物活性 for UBP 302
UBP 302 is a potent and selective GluK1 (formally GluR5)-subunit containing kainate receptor antagonist (apparent KD = 402 nM); active enantiomer of UBP 296 (Cat. No. 2078). Displays ~ 260-fold selectivity over AMPA receptors, ~ 90-fold selectivity over recombinant human GluK2 (formally GluR6) and GluK5 (formally KA2)-containing kainate receptors and has little or no action at NMDA or group I mGlu receptors. Selectively blocks kainate receptor-mediated LTP induction in rat hippocampal mossy fibers. Also protects against soman-induced seizures and neuronal degeneration for up to 30 days when administered one hour after soman exposure.
Please refer to IUPHAR Guide to Pharmacology for the most recent naming conventions.
化合物库 for UBP 302
UBP 302 is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。
技术数据 for UBP 302
| 分子量 | 333.3 |
| 公式 | C15H15N3O6 |
| 储存 | Store at RT |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 745055-91-8 |
| PubChem ID | 6420161 |
| InChI Key | UUIYULWYHDSXHL-NSHDSACASA-N |
| Smiles | O=C(C=CN(C[C@H](N)C(O)=O)C2=O)N2CC1=CC=CC=C1C(O)=O |
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 UBP 302
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| 1eq. NaOH | 8.33 | 25 | |
| DMSO | 6.67 | 20 温和加热 |
制备储备液 for UBP 302
以下数据基于产品分子量 333.3。 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 |
|---|---|---|---|
| 0.25 mM | 12 mL | 60.01 mL | 120.01 mL |
| 1.25 mM | 2.4 mL | 12 mL | 24 mL |
| 2.5 mM | 1.2 mL | 6 mL | 12 mL |
| 12.5 mM | 0.24 mL | 1.2 mL | 2.4 mL |
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产品说明书 for UBP 302
参考文献 for UBP 302
参考文献是支持产品生物活性的出版物。
More et al (2004) Characterisation of UBP296: a novel, potent and selective kainate receptor antagonist. Neuropharmacology 47 46 PMID: 15165833
Dolman et al (2005) Synthesis and pharmacology of willardiine derivatives acting as antagonists of kainate receptors. J.Med.Chem. 48 7867 PMID: 16302825
Apland et al (2014) The Limitations of D.pam as a Treatment for Nerve Agent-Induced Seizures and Neuropathology in Rats: Comparison with UBP302. J.Pharmacol.Exp.Ther. 351 359 PMID: 25157087
If you know of a relevant reference for UBP 302, please let us know.
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关键词: UBP 302, UBP 302 supplier, Selective, potent, kainate, antagonists, Glutamate, Kainate, Receptors, iGluR, Ionotropic, UBP302, neurodegeneration, 2079, Tocris Bioscience
3 篇 UBP 302 的引用文献
引用文献是使用了 Tocris 产品的出版物。 UBP 302 的部分引用包括：
Randall et al (2011) Fast oscillatory activity induced by kainate receptor activation in the rat basolateral amygdala in vitro. Eur J Neurosci 33 914 PMID: 21255131
Caiati et al (2013) PrPC controls via protein kinase A the direction of synaptic plasticity in the immature hippocampus. J Neurosci 33 2973 PMID: 23407955
Talpalar and Kiehn (2010) Glutamatergic mechanisms for speed control and network operation in the rodent locomotor CpG. Front Neural Circuits 4 PMID: 20844601
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