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HC 067047

  ( 9 citations ) ( 1 Review )    
Product Datasheet
Catalog Number:4100
Chemical Name:2-Methyl-1-[3-(4-morpholinyl)propyl]-5-phenyl-N-[3-(trifluoromethyl)phenyl]-1H-pyrrole-3-carboxamide
Product Details
Citations (9)
Reviews
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.
Product Datasheets
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Citations:

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

9 Citations: Showing 1 - 9
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  1. Pharmacological activation of TRPV4 produces immediate cell damage and induction of apoptosis in human melanoma cells and HaCaT keratinocytes.
    Authors: Olivan-Viguera
    PLoS One  2018;13:e0190307
  2. 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
  3. Hypotonic stress induces RANKL via transient receptor potential melastatin 3 (TRPM3) and vaniloid 4 (TRPV4) in human PDL cells.
    Authors: Son Et al.
    J Dent Res  2015;94:473
  4. Astrocyte contributions to flow/pressure-evoked parenchymal arteriole vasoconstriction.
    Authors: Kim Et al.
    Nat Chem Biol  2015;35:8245
  5. 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
  6. Novel therapeutic strategy to prevent chemotherapy-induced persistent sensory neuropathy by TRPA1 blockade.
    Authors: Trevisan Et al.
    Cancer Res  2013;73:3120
  7. 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
  8. Hypotonicity-induced TRPV4 function in renal collecting duct cells: modulation by progressive cross-talk with Ca2+-activated K+ channels.
    Authors: Jin Et al.
    Cell Calcium  2012;51:131
  9. TRPV4 in porcine lens epithelium regulates hemichannel-mediated ATP release and Na-K-ATPase activity.
    Authors: Shahidullah Et al.
    Am J Physiol Cell Physiol  2012;302:C1751

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Average Rating: 5 (Based on 2 reviews)

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We have 2 reviews tested in 2 species: Other, Rat.

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  Excellent
   Other Jennifer Neves 01/23/2018
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Summary

Species Other
Pub Med ID 28768667
  Excellent
   Rat Jennifer Neves 01/23/2018
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Summary

Species Rat
Pub Med ID 25832173

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