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Submit ReviewVU 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.
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.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 19.12 | 50 |
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 |
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.
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
引用文献是使用了 Tocris 产品的出版物。 VU 0463271 的部分引用包括:
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
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
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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!
*请注意,Tocris 仅会向正规科研企业/机构地址发送文献。
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.