Catalog Number: 5380
Chemical Name: N-(3,4-Difluorophenyl)-N'-(3-methyl-1-phenyl-1H-pyrazol-5-yl)urea
Biological Activity
Selective Kir3.1/3.2 (GIRK1/2) channel activator (IC50 values are 160, 887 and 914 nM for GIRK1/2, GIRK1/4 and GIRK1/3 respectively). Exhibits no effect on GIRK2, GIRK2/3, Kir2.1 and Kv7.4 channels, and has minimal effect on a panel of other ion channels, receptors and transporters. Prevents PTZ-induced epileptic seizures in mice. Brain penetrant.
Technical Data
  • M.Wt:
  • Formula:
  • Solubility:
    Soluble to 100 mM in DMSO and to 50 mM in ethanol
  • Purity:
  • Storage:
    Store at -20°C
  • CAS No:
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Background References
  1. ML297 (VU0456810), the first potent and selective activator of the GIRK potassium channel, displays antiepileptic properties in mice.
    Kaufmann et al.
    ACS Chem.Neurosci., 2013;4:1278
  2. Discovery of 'molecular switches' within a GIRK activator scaffold that afford selective GIRK inhibitors.
    Wen et al.
    Bioorg.Med.Chem.Lett., 2013;23:4562
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