Catalog Number: 5106
Chemical Name: 3-([1,4'-Bipiperidin]-1'-ylmethyl)-7-bromo-N-(1-phenylcyclopropyl)-2-[3-(trifluoromethyl)phenyl]-4-quinolinecarboxamide
Biological Activity
Potent and selective TRPV4 antagonist (IC50 values are 2 and 40 nM for rat and human receptors, respectively); inhibits Ca2+ influx through TRPV4 channels. Prevents and reverses pulmonary edema after myocardial infarction in vivo models. Selective over a panel of ~200 human receptors, channels and enzymes. Orally active.
Technical Data
  • M.Wt:
    691.62
  • Formula:
    C37H38BrF3N4O
  • Solubility:
    Soluble to 20 mM in 1eq. HCl and to 50 mM in DMSO
  • Storage:
    Store at +4°C
  • CAS No:
    1336960-13-4
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.
Additional Information
Licensing Caveats:
Sold for research purposes under agreement from GlaxoSmithKline
Background References
  1. An orally active TRPV4 channel blocker prevents and resolves pulmonary edema induced by heart failure.
    Thorneloe et al.
    Sci.Transl.Med., 2012;4:159
  2. Discovery of GSK2193874: an orally active, potent, and selective blocker of transient receptor potential vanilloid 4.
    Cheung et al.
    ACS Med.Chem.Lett., 2017;8:549

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