V3890
VU0240551
≥98% (HPLC)
别名:
CID 7211972, N-(4-Methyl-2-thiazolyl)-2-[(6-phenyl-3-pyridazinyl)thio]-acetamide, SID 56405457, VU0240551-1, VU0240551-2-D4
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关于此项目
经验公式（希尔记法）:
C16H14N4OS2
化学文摘社编号:
分子量:
342.44
NACRES:
NA.77
PubChem Substance ID:
UNSPSC Code:
12352200
MDL number:
产品名称
VU0240551, ≥98% (HPLC)
InChI key
WJRWSLORVIHRNX-UHFFFAOYSA-N
SMILES string
Cc1csc(NC(=O)CSc2ccc(nn2)-c3ccccc3)n1
InChI
1S/C16H14N4OS2/c1-11-9-23-16(17-11)18-14(21)10-22-15-8-7-13(19-20-15)12-5-3-2-4-6-12/h2-9H,10H2,1H3,(H,17,18,21)
assay
≥98% (HPLC)
form
powder
solubility
DMSO: >20 mg/mL
storage temp.
2-8°C
Quality Level
相关类别
Biochem/physiol Actions
VU0240551 is a potent, selective KCC2 inhibitor.
VU0240551 is a potent, selective KCC2 inhibitor. KCC2 is a potassium-chloride exchanger expressed specifically in neurons. KCC2 functions to lower intracellular chloride concentrations below the electrochemical potential of the cells, thereby increasing the hyperexcitability of the neurons. KCC2 activity enhances GABA and other inhibitory neurotransmission and is implicated in pain processing. VU0240551 was discovered in a high-throughput screen, followed by directed medicinal chemistry. VU0240551 is selective for KCC2 over NKCC1. VU0240551 binds competitively to the K+ site and binds noncompetitively to the Cl- site. VU0240551 is the only small molecule with specificity for a KCC family member.
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Mogens Andreasen et al.
Journal of neurophysiology, 117(4), 1512-1523 (2017-01-20)
The loop diuretic furosemide is known to have anticonvulsant effects, believed to be exerted through blockade of glial Na
Nicolas Doyon et al.
PLoS computational biology, 7(9), e1002149-e1002149 (2011-09-21)
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 relatively straightforward to understand, but how dynamic interplay between Cl(-) influx, diffusion
Josiane C S Mapplebeck et al.
Cell reports, 28(3), 590-596 (2019-07-18)
The behavioral features of neuropathic pain are not sexually dimorphic despite sex differences in the underlying neuroimmune signaling. This raises questions about whether neural processing is comparably altered. Here, we test whether the K+-Cl- co-transporter KCC2, which regulates synaptic inhibition
Martin Heubl et al.
Nature communications, 8(1), 1776-1776 (2017-11-28)
The K+-Cl- co-transporter KCC2 (SLC12A5) tunes the efficacy of GABAA receptor-mediated transmission by regulating the intraneuronal chloride concentration [Cl-]i. KCC2 undergoes activity-dependent regulation in both physiological and pathological conditions. The regulation of KCC2 by synaptic excitation is well documented; however
Kwan Yeop Lee et al.
Pain, 156(12), 2431-2437 (2015-07-18)
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 conditions are associated with reduced inhibition. Disinhibition of spinal neurons can arise through decreased
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