Chemical Name: 2-Methyl-1-[3-(4-morpholinyl)propyl]-5-phenyl-N-[3-(trifluoromethyl)phenyl]-1H-pyrrole-3-carboxamide
Biological ActivityPotent 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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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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Reviews for HC 067047
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HC067047 (1µM) was used to demonstrate that TRPV4 channels contribute to pressure-induced membrane depolarization, intracellular [Ca2+] elevation, and constriction in neonatal pig renal preglomerular arteries.