Catalog Number: 4100
Chemical Name: 2-Methyl-1-[3-(4-morpholinyl)propyl]-5-phenyl-N-[3-(trifluoromethyl)phenyl]-1H-pyrrole-3-carboxamide
Biological Activity
Potent and selective TRPV4 antagonist. Reversibly inhibits currents through mouse, human and rat TRPV4 orthologs (IC50 values are 17, 48 and 133 nM respectively). Also inhibits the endogenous TRPV4-mediated response to 4α-PDH (IC50 = 22 nM). Selective for TRPV4 over TRPV1, TRPV2, TRPV3 and TRPM8 channels.
Technical Data
  • M.Wt:
    471.51
  • Formula:
    C26H28F3N3O2
  • Solubility:
    Soluble to 100 mM in DMSO and to 25 mM in ethanol
  • Purity:
    >99%
  • Storage:
    Store at +4°C
  • CAS No:
    883031-03-6
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. Inhibition of the cation channel TRPV4 improves bladder function in mice and rats with cyclophosphamide-induced cystitis.
    Everaerts et al.
    Proc.Natl.Acad.Sci., 2010;107:19084
Citations:

The citations listed below are publications that use Tocris products. Selected citations for HC 067047 include:

4 Citations: Showing 1 - 4
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  1. Functional cooperation between KCa3.1 and TRPV4 channels in bronchial smooth muscle cell proliferation associated with chronic asthma.
    Authors: Yu
    Front. Pharmacol 2017;8:559
  2. Astrocyte contributions to flow/pressure-evoked parenchymal arteriole vasoconstriction.
    Authors: Kim Et al.
    Nat Chem Biol 2015;35:8245
  3. Intravesical TRPV4 blockade reduces repeated variate stress-induced bladder dysfunction by increasing bladder capacity and decreasing voiding frequency in male rats.
    Authors: Merrill and Vizzard
    Am J Physiol Regul Integr Comp Physiol 2014;307:R471
  4. Phosphatidylinositol-4,5-biphosphate-dependent rearrangement of TRPV4 cytosolic tails enables channel activation by physiological stimuli.
    Authors: Garcia-Elias Et al.
    Proc Natl Acad Sci U S A 2013;110:9553

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