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VU 0240551

VU 0240551用途

VU 0240551是神经元中钾氯共转运通道KCC2的抑制剂(在KCC2过表达的细胞中钾离子摄入实验中IC50为560nM)。

VU 0240551名称

[ CAS 号 ]:
893990-34-6

[ 中文名 ]:
VU 0240551

[ 英文名 ]:
VU 0240551

[英文别名 ]:

VU 0240551

VU 0240551生物活性

[ 描述 ]:

VU 0240551是神经元中钾氯共转运通道KCC2的抑制剂(在KCC2过表达的细胞中钾离子摄入实验中IC50为560nM)。

[ 相关类别 ]:

信号通路 >> 跨膜转运 >> 钾通道

研究领域 >> 其他

[参考文献]

[1]. Delpire E, et al. Small-molecule screen identifies inhibitors of the neuronal K-Cl cotransporter KCC2. Proc Natl Acad Sci U S A. 2009 Mar 31;106(13):5383-8.

[2]. Delpire E, et al. 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. 2012 Jul 15;22(14):4532-5.

[相关活性小分子]

VU 0240551物理化学性质

[ 分子式 ]:
C₁₆H₁₄N₄OS₂

[ 分子量 ]:
342.43900

[ 精确质量 ]:
342.06100

[ PSA ]:
124.80000

[ LogP ]:
4.28880

[ 储存条件 ]:
2-8℃

VU 0240551MSDS

详细MSDS(安全技术说明书)

VU 0240551安全信息

[ 危险品运输编码 ]:
NONH for all modes of transport

VU 0240551文献

Chloride dysregulation and inhibitory receptor blockade yield equivalent disinhibition of spinal neurons yet are differentially reversed by carbonic anhydrase blockade.

Pain 156 , 2431-7, (2015)

Synaptic inhibition plays a key role in processing somatosensory information. Blocking inhibition at the spinal level is sufficient to produce mechanical allodynia, and many neuropathic pain condition...

Efficacy of synaptic inhibition depends on multiple, dynamically interacting mechanisms implicated in chloride homeostasis.

PLoS Comput. Biol. 7 , e1002149, (2011)

Chloride homeostasis is a critical determinant of the strength and robustness of inhibition mediated by GABA(A) receptors (GABA(A)Rs). The impact of changes in steady state Cl(-) gradient is relativel...

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