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Submit ReviewUBP 310
说明： GluK1-selective kainate antagonist
化学名： (S)-1-(2-Amino-2-carboxyethyl)-3-(2-carboxy-thiophene-3-yl-methyl)-5-methylpyrimidine-2,4-dione
纯度： ≥98% (HPLC)
生物活性 for UBP 310
UBP 310 is a GluK1 (formerly GLUK5) kainate receptor antagonist (IC50 = 130 nM); also blocks recombinant homomeric GluK3 (forrmerly GLUK7) receptors. Displays 12,700-fold selectivity for GluK1 (formerly GLUK5) over GluK2 (formerly GLUK6). Exhibits no activity at mGlu group I or NMDA receptors at concentrations of up to 10 μM. Apparent KD value is 18 ± 4 nM for depression of kainate responses on the dorsal root.
Please refer to IUPHAR Guide to Pharmacology for the most recent naming conventions.
化合物库 for UBP 310
UBP 310 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 310
| 分子量 | 353.35 |
| 公式 | C14H15N3O6S |
| 储存 | Store at +4°C |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 902464-46-4 |
| PubChem ID | 6420160 |
| InChI Key | ZTAZUCRXCRXNSU-VIFPVBQESA-N |
| Smiles | CC1=CN(C[C@@H](C(O)=O)N)C(N(CC2=C(C(O)=O)SC=C2)C1=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 310
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 7.07 | 20 |
制备储备液 for UBP 310
以下数据基于产品分子量 353.35。 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 |
|---|---|---|---|
| 0.2 mM | 14.15 mL | 70.75 mL | 141.5 mL |
| 1 mM | 2.83 mL | 14.15 mL | 28.3 mL |
| 2 mM | 1.42 mL | 7.08 mL | 14.15 mL |
| 10 mM | 0.28 mL | 1.42 mL | 2.83 mL |
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产品说明书 for UBP 310
参考文献 for UBP 310
参考文献是支持产品生物活性的出版物。
Mayer et al (2006) Crystal structures of the kainate receptor GluR5 ligand binding core dimer with novel GluR5-selective antagonists. J.Neurosci. 26 2852 PMID: 16540562
Dolman et al (2007) Synthesis and pharmacological characterization of N3-substituted willardiine derivatives: Role of the substituent at the 5-position of the uracil ring in development of highly potent and selective GLUK5 kainate receptor antagonists. J.Med.Chem. 50 1558 PMID: 17348638
Perrais et al (2009) Antagonism of recombinant and native GluK3-containing kainate receptors. Neuropharmacology 56 131 PMID: 18761361
If you know of a relevant reference for UBP 310, please let us know.
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关键词: UBP 310, UBP 310 supplier, UBP310, kainate, receptors, antagonists, GLUK5, iGlu, ionotropic, glutamate, GluK1, Kainate, Receptors, 3621, Tocris Bioscience
5 篇 UBP 310 的引用文献
引用文献是使用了 Tocris 产品的出版物。 UBP 310 的部分引用包括：
Anna L et al (2021) Slow AMPA receptors in hippocampal principal cells. Cell Rep 36 109496 PMID: 34348150
Buldyrev et al (2012) Synaptic pathways that shape the excitatory drive in an OFF retinal ganglion cell. J Neurophysiol 107 1795 PMID: 22205648
Crook et al (2014) A synaptic signature for ON- and OFF-center parasol ganglion cells of the primate retina. Vis Neurosci 31 57 PMID: 24801624
Pollok and Reiner (2020) Subunit-selective iGluR antagonists can potentiate heteromeric receptor responses by blocking desensitization Proc Natl Acad Sci USA 117 25851 PMID: 32999066
Takeshi et al (2017) Kinetics of Releasable Synaptic Vesicles and Their Plastic Changes at Hippocampal Mossy Fiber Synapses. Neuron 96 1033-1040.e3 PMID: 29103807
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