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Submit ReviewVU 0240551
Discontinued Product
3888 has been discontinued.
View all K<sup>+</sup>/Cl<sup>-</sup> Cotransporter 2 products.
说明： KCC2 inhibitor
化学名： N-(4-Methyl-2-thiazolyl)-2-[(6-phenyl-3-pyridazinyl)thio]acetamide
纯度： ≥99% (HPLC)
生物活性 for VU 0240551
VU 0240551 is an inhibitor of the neuronal K-Cl cotransporter, KCC2 (IC50 = 560 nM for K+ uptake assay in KCC2-overexpressing cells). Exhibits selectivity over the Na-K-2Cl cotransporter, NKCCl. Also inhibits hERG and L-type Ca2+ channels.
技术数据 for VU 0240551
| 分子量 | 342.43 |
| 公式 | C16H14N4OS2 |
| 储存 | Store at +4°C |
| 纯度 | ≥99% (HPLC) |
| CAS Number | 893990-34-6 |
| PubChem ID | 7211972 |
| InChI Key | WJRWSLORVIHRNX-UHFFFAOYSA-N |
| Smiles | O=C(NC3=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.
产品说明书 for VU 0240551
参考文献 for VU 0240551
参考文献是支持产品生物活性的出版物。
Delpire et al (2009) Small-molecule screen identifies inhibitors of the neuronal K-Cl cotransporter KCC2. Proc.Natl.Acad.Sci.USA 106 5383 PMID: 19279215
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
Deisz et al (2014) Effects of VU0240551, a novel KCC2 antagonist, and DIDS on chloride homeostasis of neocortical neurons from rats and humans. Neuroscience 277 831 PMID: 25086309
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关键词: VU 0240551, VU 0240551 supplier, cotransporter, potassium, chloride, transport, KCC2, Neuronal, cotransport, SLC12A5, Na+/2Cl-/K+, NKCC1, NKCC2, inhibitors, inhibits, Ion, Pumps, K-Cl, VU0240551, epilepsy, K+/Cl-, Cotransporter, 2, 3888, Tocris Bioscience
8 篇 VU 0240551 的引用文献
引用文献是使用了 Tocris 产品的出版物。 VU 0240551 的部分引用包括：
Ferando et al (2016) Diminished KCC2 confounds synapse specificity of LTP during senescence. Nat Neurosci 19 1197 PMID: 27500406
Gagnon et al (2013) Chloride extrusion enhancers as novel therapeutics for neurological diseases. Nat Med 19 1524 PMID: 24097188
Haam et al (2012) GABA is excitatory in adult vasopressinergic neuroendocrine cells. J Neurosci 32 572 PMID: 22238092
Alfredo et al (2020) Enhancing neuronal chloride extrusion rescues α2/α3 GABAA-mediated analgesia in neuropathic pain. Nat Commun 11 869 PMID: 32054836
Doyon et al (2011) Efficacy of synaptic inhibition depends on multiple, dynamically interacting mechanisms implicated in chloride homeostasis. Purinergic Signal 7 e1002149 PMID: 21931544
Marie-Pascale et al (2021) Enhancing KCC2 activity decreases hyperreflexia and spasticity after chronic spinal cord injury. Exp Neurol 338 113605 PMID: 33453210
Yi et al (2016) Potentiation of Synaptic GluN2B NMDAR Currents by Fyn Kinase Is Gated through BDNF-Mediated Disinhibition in Spinal Pain Processing. Cell Rep 17 2753-2765 PMID: 27926876
Lavertu et al (2014) Enhancing K-Cl co-transport restores normal spinothalamic sensory coding in a neuropathic pain model. Brain 137 724 PMID: 24369380
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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.