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Submit ReviewVU 0463271
说明： Potent and selective KCC2 inhibitor
化学名： N-Cyclopropyl-N-(4-methyl-2-thiazolyl)-2-[(6-phenyl-3-pyridazinyl)thio]acetamide
纯度： ≥98% (HPLC)
生物活性 for VU 0463271
VU 0463271 is a potent and selective inhibitor of the neuronal K-Cl cotransporter, KCC2 (IC50 = 61 nM); displays >100-fold selectivity versus the Na-K-2Cl cotransporter 1 (NKCC1) and no activity against a panel of 68 GPCRs, ion channels and transporters.
技术数据 for VU 0463271
| 分子量 | 382.5 |
| 公式 | C19H18N4OS2 |
| 储存 | Store at +4°C |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 1391737-01-1 |
| PubChem ID | 70690453 |
| InChI Key | DPONSKCACOZTGN-UHFFFAOYSA-N |
| Smiles | O=C(N(C4CC4)C3=NC(C)=CS3)CSC(C=C2)=NN=C2C1=CC=CC=C1 |
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 VU 0463271
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 19.12 | 50 |
制备储备液 for VU 0463271
以下数据基于产品分子量 382.5。 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 |
|---|---|---|---|
| 0.5 mM | 5.23 mL | 26.14 mL | 52.29 mL |
| 2.5 mM | 1.05 mL | 5.23 mL | 10.46 mL |
| 5 mM | 0.52 mL | 2.61 mL | 5.23 mL |
| 25 mM | 0.1 mL | 0.52 mL | 1.05 mL |
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产品说明书 for VU 0463271
参考文献 for VU 0463271
参考文献是支持产品生物活性的出版物。
Delpire et al (2012) Further optimization of the K-Cl cotransporter KCC2 antagonist ML077: development of a highly selective and more potent in vitro probe. Bioorg.Med.Chem.Lett. 22 4532 PMID: 22727639
Sivakumaran et al (2015) Selective inhibition of KCC2 leads to hyperexcitability and epileptiform discharges in hippocampal slices and in vivo. J.Neurosci. 35 8291 PMID: 26019342
If you know of a relevant reference for VU 0463271, please let us know.
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关键词: VU 0463271, VU 0463271 supplier, VU0463271, potent, selective, inhibitors, inhibits, neuronal, K-Cl, cotransporters, KCC2, K+/Cl-, Cotransporter, 2, 4719, Tocris Bioscience
5 篇 VU 0463271 的引用文献
引用文献是使用了 Tocris 产品的出版物。 VU 0463271 的部分引用包括：
Israel et al (2022) SNAP23 regulates KCC2 membrane insertion and activity following mZnR/GPR39 activation in hippocampalneurons. iScience 25 103751 PMID: 35118363
Alfonsa et al (2016) Cl- out is a novel cooperative optogenetic tool for extruding chloride from neurons Nature Communications 7 13495 PMID: 27853135
Sourav et al (2020) A Cellular Mechanism of Learning-Induced Enhancement of Synaptic Inhibition: PKC-Dependent Upregulation of KCC2 Activation. Sci Rep 10 962 PMID: 31969605
Pál et al (2015) Appearance of fast astrocytic component in voltage-sensitive dye imaging of neural activity. Mol Syst Biol 8 35 PMID: 26043770
Akiko et al (2021) CLP290 promotes the sedative effects of midazolam in neonatal rats in a KCC2-dependent manner: A laboratory study in rats. PLoS One 16 e0248113 PMID: 33711029
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该领域的文献
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*请注意，Tocris 仅会向正规科研企业/机构地址发送文献。
GABA Receptors Scientific Review
Written by Ian Martin, Norman Bowery and Susan Dunn, this review provides a history of the GABA receptor, as well as discussing the structure and function of the various subtypes and the clinical potential of receptor modulators; compounds available from Tocris are listed.