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V3890 Sigma

VU0240551

≥98% (HPLC)

Synonym: CID 7211972, N-(4-Methyl-2-thiazolyl)-2-[(6-phenyl-3-pyridazinyl)thio]-acetamide, SID 56405457, VU0240551-1, VU0240551-2-D4

  • CAS Number 893990-34-6

  • Empirical Formula (Hill Notation) C16H14N4OS2

  • Molecular Weight 342.44

  •  MDL number MFCD05957363

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Properties

Related Categories Bioactive Small Molecule Alphabetical Index, Bioactive Small Molecules, Cell Biology, Cell Signaling and Neuroscience, Ion Channels,
InChI Key   WJRWSLORVIHRNX-UHFFFAOYSA-N
assay   ≥98% (HPLC)
form   powder
solubility   DMSO: >20 mg/mL
storage temp.   2-8°C

Description

Biochem/physiol Actions

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.

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