Chemical Name: 2-Methyl-1-[3-(4-morpholinyl)propyl]-5-phenyl-N-[3-(trifluoromethyl)phenyl]-1H-pyrrole-3-carboxamide
Biological ActivityHC 067047 is a 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.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
Inhibition of the cation channel TRPV4 improves bladder function in mice and rats with cyclophosphamide-induced cystitis.
Everaerts et al.
Citations for HC 067047
The citations listed below are publications that use Tocris products. Selected citations for HC 067047 include:
13 Citations: Showing 1 - 10
TRPV4 activates autonomic and behavioural warmth-defence responses in Wistar rats.
Acta Physiol ;214:275
Cell sensing and decision-making in confinement: The role of TRPM7 in a tug of war between hydraulic pressure and cross-sectional area.
Authors: Zhao Et al.
Sci Adv 2019;5:eaaw7243
TRPV4 is the temperature-sensitive ion channel of human sperm.
Authors: Mundt Et al.
Pharmacological activation of TRPV4 produces immediate cell damage and induction of apoptosis in human melanoma cells and HaCaT keratinocytes.
PLoS One 2018;13:e0190307
Functional cooperation between KCa3.1 and TRPV4 channels in bronchial smooth muscle cell proliferation associated with chronic asthma.
Front. Pharmacol 2017;8:559
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
Astrocyte contributions to flow/pressure-evoked parenchymal arteriole vasoconstriction.
Authors: Kim Et al.
Nat Chem Biol 2015;35:8245
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
Novel therapeutic strategy to prevent chemotherapy-induced persistent sensory neuropathy by TRPA1 blockade.
Authors: Trevisan Et al.
Cancer Res 2013;73:3120
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
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
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
Mechanotransductional basis of endothelial cell response to intravascular bubbles.
Authors: Klinger Et al.
Integr Biol (Camb) 2011;3:1033
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